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A curated database of glucokinase modulators
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Compound ID Compound ID/Name Type Year of publication Scaffold Name Molecular Weight XLOGP3 Group/Institution Molecular Formula Article Title PubChem ID Index
AM-2394 AM-2394 GKA: Systemic 2016 Urea,Pyridine 423.47 1.81 Amgen Inc. & Array BioPharma (USA) C22H25N5O4 Dransfield, P. J. et al. Novel Series of Potent Glucokinase Activators Leading to the Discovery of AM-2394. ACS Med. Chem. Lett. (2016) 71603585 11
AMG-1694 AMG-1694 GK-GKRP disruptor 2014 Sulfoxide/Sulfone derivatives 533.63 3.29 Amgen Inc. (USA) C23H30F3N3O4S2 Ashton, K. S. et al. Small molecule disruptors of the Glucokinase-Glucokinase regulatory protein interaction: 1. Discovery of a novel tool compound for in vivo proof-of-concept. J. Med. Chem. (2014) 66582747 1476
AMG-3969 AMG-3969 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives 522.46 3.1 Amgen Inc. (USA) C21H20F6N4O3S St. Jean, D. J. et al. Small molecule disruptors of the Glucokinase-Glucokinase regulatory protein interaction: 2. Leveraging structure-based drug design to identify analogues with improved pharmacokinetic profiles. J. Med. Chem. (2014) 73053709 1477
Astra_Zeneca_s_GKA22 Astra Zeneca's GKA22 GKA: Systemic 2005 Benzamide,Pyridine 426.49 3.93 AstraZeneca (UK) C22H22N2O5S McKerrecher, D. et al. Discovery, synthesis and biological evaluation of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2005) 9954194 3
Astra_Zeneca_s_GKA50 Astra Zeneca's GKA50 GKA: Systemic 2006 Benzamide,Pyridine 464.51 4.16 AstraZeneca (UK) C26H28N2O6 McKerrecher, D. et al. Design of a potent, soluble glucokinase activator with excellent in vivo efficacy. Bioorganic Med. Chem. Lett. (2006) 11340230 4
Banyu_s_Compound_A Banyu's Compound A GKA: Systemic 2004 Thiazole/Thiadiazole,Benzamide 349.41 2.59 Banyu Tsukuba Research Institute (JAPAN) C14H12FN5OS2 Kamata, K., Mitsuya, M., Nishimura, T., Eiki, J. & Nagata, Y. Structural Basis for Allosteric Regulation of the Monomeric Allosteric Enzyme Human Glucokinase. Structure 12, 429–438 (2004) 449003 1
Dorzagliatin_HMS5552 Dorzagliatin (Sinogliatin/HMS5552) GKA: Systemic 2017 462.93 1.6 Hua Medicine (Shanghai, CHINA) C22H27ClN4O5 Wang, P. et al. Effects of a Novel Glucokinase Activator, HMS5552, on Glucose Metabolism in a Rat Model of Type 2 Diabetes Mellitus. J. Diabetes Res. (2017) 76641559 12
GKA10-2b GKA10-2b GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 432.51 3.66 Banyu Tsukuba Research Institute (JAPAN) C20H20N2O5S2 Iino, T. et al. Structure-activity relationships of 3,5-disubstituted benzamides as glucokinase activators with potent in vivo efficacy. Bioorganic Med. Chem. (2009) 11154711 218
GKA10-5a GKA10-5a GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 458.55 4.13 Banyu Tsukuba Research Institute (JAPAN) C22H22N2O5S2 Iino, T. et al. Structure-activity relationships of 3,5-disubstituted benzamides as glucokinase activators with potent in vivo efficacy. Bioorganic Med. Chem. (2009) 23093036 219
GKA10-5b GKA10-5b GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 460.52 2.91 Banyu Tsukuba Research Institute (JAPAN) C21H20N2O6S2 Iino, T. et al. Structure-activity relationships of 3,5-disubstituted benzamides as glucokinase activators with potent in vivo efficacy. Bioorganic Med. Chem. (2009) 45270647 220
GKA10-5c GKA10-5c GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 476.57 3.67 Banyu Tsukuba Research Institute (JAPAN) C22H24N2O6S2 Iino, T. et al. Structure-activity relationships of 3,5-disubstituted benzamides as glucokinase activators with potent in vivo efficacy. Bioorganic Med. Chem. (2009) 45268096 221
GKA10-5d GKA10-5d GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 462.54 3.14 Banyu Tsukuba Research Institute (JAPAN) C21H22N2O6S2 Iino, T. et al. Structure-activity relationships of 3,5-disubstituted benzamides as glucokinase activators with potent in vivo efficacy. Bioorganic Med. Chem. (2009) 23093050 222
GKA10-5e GKA10-5e GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 474.55 3.27 Banyu Tsukuba Research Institute (JAPAN) C22H22N2O6S2 Iino, T. et al. Structure-activity relationships of 3,5-disubstituted benzamides as glucokinase activators with potent in vivo efficacy. Bioorganic Med. Chem. (2009) 45270633 223
GKA10-5f GKA10-5f GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 492.57 2.63 Banyu Tsukuba Research Institute (JAPAN) C22H24N2O7S2 Iino, T. et al. Structure-activity relationships of 3,5-disubstituted benzamides as glucokinase activators with potent in vivo efficacy. Bioorganic Med. Chem. (2009) 10458369 224
GKA10-5g GKA10-5g GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 448.51 2.61 Banyu Tsukuba Research Institute (JAPAN) C20H20N2O6S2 Iino, T. et al. Structure-activity relationships of 3,5-disubstituted benzamides as glucokinase activators with potent in vivo efficacy. Bioorganic Med. Chem. (2009) 45270655 225
GKA10-5h GKA10-5h GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 434.49 2.18 Banyu Tsukuba Research Institute (JAPAN) C19H18N2O6S2 Iino, T. et al. Structure-activity relationships of 3,5-disubstituted benzamides as glucokinase activators with potent in vivo efficacy. Bioorganic Med. Chem. (2009) 10252364 226
GKA10-5i GKA10-5i GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 474.55 3.15 Banyu Tsukuba Research Institute (JAPAN) C22H22N2O6S2 Iino, T. et al. Structure-activity relationships of 3,5-disubstituted benzamides as glucokinase activators with potent in vivo efficacy. Bioorganic Med. Chem. (2009) 9982344 227
GKA10-5j GKA10-5j GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 474.55 3.15 Banyu Tsukuba Research Institute (JAPAN) C22H22N2O6S2 Iino, T. et al. Structure-activity relationships of 3,5-disubstituted benzamides as glucokinase activators with potent in vivo efficacy. Bioorganic Med. Chem. (2009) 45268085 228
GKA10-5k GKA10-5k GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 462.54 2.97 Banyu Tsukuba Research Institute (JAPAN) C21H22N2O6S2 Iino, T. et al. Structure-activity relationships of 3,5-disubstituted benzamides as glucokinase activators with potent in vivo efficacy. Bioorganic Med. Chem. (2009) 10004541 229
GKA10-5l GKA10-5l GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 502.48 3.35 Banyu Tsukuba Research Institute (JAPAN) C20H17F3N2O6S2 Iino, T. et al. Structure-activity relationships of 3,5-disubstituted benzamides as glucokinase activators with potent in vivo efficacy. Bioorganic Med. Chem. (2009) 45268959 230
GKA10-5m GKA10-5m GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 476.57 3.57 Banyu Tsukuba Research Institute (JAPAN) C22H24N2O6S2 Iino, T. et al. Structure-activity relationships of 3,5-disubstituted benzamides as glucokinase activators with potent in vivo efficacy. Bioorganic Med. Chem. (2009) 23093081 231
GKA10-5n GKA10-5n GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 459.54 2.63 Banyu Tsukuba Research Institute (JAPAN) C21H21N3O5S2 Iino, T. et al. Structure-activity relationships of 3,5-disubstituted benzamides as glucokinase activators with potent in vivo efficacy. Bioorganic Med. Chem. (2009) 45268088 232
GKA10-5o GKA10-5o GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 447.53 2.35 Banyu Tsukuba Research Institute (JAPAN) C20H21N3O5S2 Iino, T. et al. Structure-activity relationships of 3,5-disubstituted benzamides as glucokinase activators with potent in vivo efficacy. Bioorganic Med. Chem. (2009) 23092965 233
GKA10-5p GKA10-5p GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 475.58 3.33 Banyu Tsukuba Research Institute (JAPAN) C22H25N3O5S2 Iino, T. et al. Structure-activity relationships of 3,5-disubstituted benzamides as glucokinase activators with potent in vivo efficacy. Bioorganic Med. Chem. (2009) 10073655 234
GKA10-5q GKA10-5q GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 473.57 3.09 Banyu Tsukuba Research Institute (JAPAN) C22H23N3O5S2 Iino, T. et al. Structure-activity relationships of 3,5-disubstituted benzamides as glucokinase activators with potent in vivo efficacy. Bioorganic Med. Chem. (2009) 45272367 235
GKA10-5r GKA10-5r GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 446.54 3.26 Banyu Tsukuba Research Institute (JAPAN) C21H22N2O5S2 Iino, T. et al. Structure-activity relationships of 3,5-disubstituted benzamides as glucokinase activators with potent in vivo efficacy. Bioorganic Med. Chem. (2009) 10095113 236
GKA10-5s GKA10-5s GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 476.52 3.26 Banyu Tsukuba Research Institute (JAPAN) C21H20N2O7S2 Iino, T. et al. Structure-activity relationships of 3,5-disubstituted benzamides as glucokinase activators with potent in vivo efficacy. Bioorganic Med. Chem. (2009) 10254402 237
GKA10-5t GKA10-5t GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 489.56 3.01 Banyu Tsukuba Research Institute (JAPAN) C22H23N3O6S2 Iino, T. et al. Structure-activity relationships of 3,5-disubstituted benzamides as glucokinase activators with potent in vivo efficacy. Bioorganic Med. Chem. (2009) 10005759 238
GKA10-5u GKA10-5u GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 503.59 3.19 Banyu Tsukuba Research Institute (JAPAN) C23H25N3O6S2 Iino, T. et al. Structure-activity relationships of 3,5-disubstituted benzamides as glucokinase activators with potent in vivo efficacy. Bioorganic Med. Chem. (2009) 239
GKA10-6b GKA10-6b GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 460.52 2.91 Banyu Tsukuba Research Institute (JAPAN) C21H20N2O6S2 Iino, T. et al. Structure-activity relationships of 3,5-disubstituted benzamides as glucokinase activators with potent in vivo efficacy. Bioorganic Med. Chem. (2009) 45273248 240
GKA10-6c GKA10-6c GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 476.57 3.67 Banyu Tsukuba Research Institute (JAPAN) C22H24N2O6S2 Iino, T. et al. Structure-activity relationships of 3,5-disubstituted benzamides as glucokinase activators with potent in vivo efficacy. Bioorganic Med. Chem. (2009) 45267234 242
GKA10-6g GKA10-6g GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 448.51 2.61 Banyu Tsukuba Research Institute (JAPAN) C20H20N2O6S2 Iino, T. et al. Structure-activity relationships of 3,5-disubstituted benzamides as glucokinase activators with potent in vivo efficacy. Bioorganic Med. Chem. (2009) 11662332 244
GKA10-6i GKA10-6i GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 474.55 3.15 Banyu Tsukuba Research Institute (JAPAN) C22H22N2O6S2 Iino, T. et al. Structure-activity relationships of 3,5-disubstituted benzamides as glucokinase activators with potent in vivo efficacy. Bioorganic Med. Chem. (2009) 45271457 246
GKA10-6j GKA10-6j GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 474.55 3.15 Banyu Tsukuba Research Institute (JAPAN) C22H22N2O6S2 Iino, T. et al. Structure-activity relationships of 3,5-disubstituted benzamides as glucokinase activators with potent in vivo efficacy. Bioorganic Med. Chem. (2009) 45268085 248
GKA10-7b GKA10-7b GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 460.52 2.91 Banyu Tsukuba Research Institute (JAPAN) C21H20N2O6S2 Iino, T. et al. Structure-activity relationships of 3,5-disubstituted benzamides as glucokinase activators with potent in vivo efficacy. Bioorganic Med. Chem. (2009) 45270647 241
GKA10-7c GKA10-7c GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 476.57 3.67 Banyu Tsukuba Research Institute (JAPAN) C22H24N2O6S2 Iino, T. et al. Structure-activity relationships of 3,5-disubstituted benzamides as glucokinase activators with potent in vivo efficacy. Bioorganic Med. Chem. (2009) 45268096 243
GKA10-7g GKA10-7g GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 448.51 2.61 Banyu Tsukuba Research Institute (JAPAN) C20H20N2O6S2 Iino, T. et al. Structure-activity relationships of 3,5-disubstituted benzamides as glucokinase activators with potent in vivo efficacy. Bioorganic Med. Chem. (2009) 45270655 245
GKA10-7i GKA10-7i GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 474.55 3.15 Banyu Tsukuba Research Institute (JAPAN) C22H22N2O6S2 Iino, T. et al. Structure-activity relationships of 3,5-disubstituted benzamides as glucokinase activators with potent in vivo efficacy. Bioorganic Med. Chem. (2009) 45271479 247
GKA10-7j GKA10-7j GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 474.55 3.15 Banyu Tsukuba Research Institute (JAPAN) C22H22N2O6S2 Iino, T. et al. Structure-activity relationships of 3,5-disubstituted benzamides as glucokinase activators with potent in vivo efficacy. Bioorganic Med. Chem. (2009) 45269833 249
GKA1-10 GKA1-10 GKA: Systemic 2005 Thiazole/Thiadiazole,Urea,Pyridine 332.42 3.1 OSI Pharmaceuticals (USA); Prosidion Limited (UK) C16H20N4O2S Castelhano, A. L. et al. Glucokinase-activating ureas. Bioorganic Med. Chem. Lett. (2005) 44389920 23
GKA1-11 GKA1-11 GKA: Systemic 2005 Thiazole/Thiadiazole,Urea,Pyridine 366.87 4.06 OSI Pharmaceuticals (USA); Prosidion Limited (UK) C16H19ClN4O2S Castelhano, A. L. et al. Glucokinase-activating ureas. Bioorganic Med. Chem. Lett. (2005) 44389928 24
GKA1-12 GKA1-12 GKA: Systemic 2005 Thiazole/Thiadiazole,Urea,Pyridine 411.32 4.12 OSI Pharmaceuticals (USA); Prosidion Limited (UK) C16H19BrN4O2S Castelhano, A. L. et al. Glucokinase-activating ureas. Bioorganic Med. Chem. Lett. (2005) 44389929 25
GKA11-21a GKA11-21a GKA: Systemic 2009 Sulfoxide/Sulfone derivatives,Quinoline/Quinazoline 395.43 2.83 Banyu Tsukuba Research Institute (JAPAN) C19H17N5O3S Iino, T. et al. Discovery and structure-activity relationships of a novel class of quinazoline glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 11718171 255
GKA11-21b GKA11-21b GKA: Systemic 2009 Quinoline/Quinazoline 353.33 3.79 Banyu Tsukuba Research Institute (JAPAN) C18H13F2N5O Iino, T. et al. Discovery and structure-activity relationships of a novel class of quinazoline glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 11610032 256
GKA11-21c GKA11-21c GKA: Systemic 2009 Quinoline/Quinazoline 353.33 3.79 Banyu Tsukuba Research Institute (JAPAN) C18H13F2N5O Iino, T. et al. Discovery and structure-activity relationships of a novel class of quinazoline glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 23160266 257
GKA11-21d GKA11-21d GKA: Systemic 2009 Sulfoxide/Sulfone derivatives,Quinoline/Quinazoline 413.43 2.93 Banyu Tsukuba Research Institute (JAPAN) C19H16FN5O3S Iino, T. et al. Discovery and structure-activity relationships of a novel class of quinazoline glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 11589677 258
GKA11-21e GKA11-21e GKA: Systemic 2009 Sulfoxide/Sulfone derivatives,Quinoline/Quinazoline 429.88 3.45 Banyu Tsukuba Research Institute (JAPAN) C19H16ClN5O3S Iino, T. et al. Discovery and structure-activity relationships of a novel class of quinazoline glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 11647637 259
GKA11-21f GKA11-21f GKA: Systemic 2009 Sulfoxide/Sulfone derivatives,Quinoline/Quinazoline 409.46 3.19 Banyu Tsukuba Research Institute (JAPAN) C20H19N5O3S Iino, T. et al. Discovery and structure-activity relationships of a novel class of quinazoline glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 23160272 260
GKA11-21g GKA11-21g GKA: Systemic 2009 Sulfoxide/Sulfone derivatives,Quinoline/Quinazoline 409.46 3.19 Banyu Tsukuba Research Institute (JAPAN) C20H19N5O3S Iino, T. et al. Discovery and structure-activity relationships of a novel class of quinazoline glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 23160260 261
GKA11-21h GKA11-21h GKA: Systemic 2009 Quinoline/Quinazoline 356.38 3.67 Banyu Tsukuba Research Institute (JAPAN) C20H16N6O Iino, T. et al. Discovery and structure-activity relationships of a novel class of quinazoline glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 23160348 262
GKA11-21i GKA11-21i GKA: Systemic 2009 Pyridine,Quinoline/Quinazoline 318.33 2.85 Banyu Tsukuba Research Institute (JAPAN) C17H14N6O Iino, T. et al. Discovery and structure-activity relationships of a novel class of quinazoline glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 45483594 263
GKA11-21j GKA11-21j GKA: Systemic 2009 Pyrazine,Quinoline/Quinazoline 319.32 1.78 Banyu Tsukuba Research Institute (JAPAN) C16H13N7O Iino, T. et al. Discovery and structure-activity relationships of a novel class of quinazoline glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 23160279 264
GKA11-21k GKA11-21k GKA: Systemic 2009 Pyrimidine,Quinoline/Quinazoline 319.32 2.2 Banyu Tsukuba Research Institute (JAPAN) C16H13N7O Iino, T. et al. Discovery and structure-activity relationships of a novel class of quinazoline glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 23160304 265
GKA11-21l GKA11-21l GKA: Systemic 2009 Pyridine,Quinoline/Quinazoline 336.32 2.95 Banyu Tsukuba Research Institute (JAPAN) C17H13FN6O Iino, T. et al. Discovery and structure-activity relationships of a novel class of quinazoline glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 23160287 266
GKA11-21m GKA11-21m GKA: Systemic 2009 Pyridine,Quinoline/Quinazoline 352.78 3.48 Banyu Tsukuba Research Institute (JAPAN) C17H13ClN6O Iino, T. et al. Discovery and structure-activity relationships of a novel class of quinazoline glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 45483616 267
GKA11-21n GKA11-21n GKA: Systemic 2009 Pyridine,Quinoline/Quinazoline 397.23 3.54 Banyu Tsukuba Research Institute (JAPAN) C17H13BrN6O Iino, T. et al. Discovery and structure-activity relationships of a novel class of quinazoline glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 45483579 268
GKA11-21o GKA11-21o GKA: Systemic 2009 Pyridine,Quinoline/Quinazoline 389.41 2.31 Banyu Tsukuba Research Institute (JAPAN) C20H19N7O2 Iino, T. et al. Discovery and structure-activity relationships of a novel class of quinazoline glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 45483589 269
GKA11-21p GKA11-21p GKA: Systemic 2009 Pyridine,Quinoline/Quinazoline 348.36 1.97 Banyu Tsukuba Research Institute (JAPAN) C18H16N6O2 Iino, T. et al. Discovery and structure-activity relationships of a novel class of quinazoline glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 23160263 270
GKA11-25a GKA11-25a GKA: Systemic 2009 Sulfoxide/Sulfone derivatives,Quinoline/Quinazoline 427.45 3.23 Banyu Tsukuba Research Institute (JAPAN) C20H18FN5O3S Iino, T. et al. Discovery and structure-activity relationships of a novel class of quinazoline glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 11690454 271
GKA11-25b GKA11-25b GKA: Systemic 2009 Sulfoxide/Sulfone derivatives,Quinoline/Quinazoline 399.4 2.91 Banyu Tsukuba Research Institute (JAPAN) C18H14FN5O3S Iino, T. et al. Discovery and structure-activity relationships of a novel class of quinazoline glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 45483603 272
GKA11-25c GKA11-25c GKA: Systemic 2009 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives,Quinoline/Quinazoline 431.46 3.85 Banyu Tsukuba Research Institute (JAPAN) C18H14FN5O3S2 Iino, T. et al. Discovery and structure-activity relationships of a novel class of quinazoline glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 45483611 273
GKA11-25d GKA11-25d GKA: Systemic 2009 Pyridine,Sulfoxide/Sulfone derivatives,Quinoline/Quinazoline 410.42 3.55 Banyu Tsukuba Research Institute (JAPAN) C20H15FN4O3S Iino, T. et al. Discovery and structure-activity relationships of a novel class of quinazoline glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 45483612 274
GKA11-25e GKA11-25e GKA: Systemic 2009 Sulfoxide/Sulfone derivatives,Quinoline/Quinazoline 411.41 2.54 Banyu Tsukuba Research Institute (JAPAN) C19H14FN5O3S Iino, T. et al. Discovery and structure-activity relationships of a novel class of quinazoline glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 23160298 275
GKA11-25f GKA11-25f GKA: Systemic 2009 Pyrazine,Sulfoxide/Sulfone derivatives,Quinoline/Quinazoline 411.41 2.48 Banyu Tsukuba Research Institute (JAPAN) C19H14FN5O3S Iino, T. et al. Discovery and structure-activity relationships of a novel class of quinazoline glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 11711284 276
GKA11-25g GKA11-25g GKA: Systemic 2009 Pyrazine,Sulfoxide/Sulfone derivatives,Quinoline/Quinazoline 425.44 2.88 Banyu Tsukuba Research Institute (JAPAN) C20H16FN5O3S Iino, T. et al. Discovery and structure-activity relationships of a novel class of quinazoline glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 23160316 277
GKA11-25h GKA11-25h GKA: Systemic 2009 Pyrazine,Sulfoxide/Sulfone derivatives,Quinoline/Quinazoline 445.85 3.44 Banyu Tsukuba Research Institute (JAPAN) C19H13ClFN5O3S Iino, T. et al. Discovery and structure-activity relationships of a novel class of quinazoline glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 23160285 278
GKA1-13 GKA1-13 GKA: Systemic 2005 Thiazole/Thiadiazole,Urea,Pyridine 333.41 2.51 OSI Pharmaceuticals (USA); Prosidion Limited (UK) C15H19N5O2S Castelhano, A. L. et al. Glucokinase-activating ureas. Bioorganic Med. Chem. Lett. (2005) 44389936 26
GKA11-4 GKA11-4 GKA: Systemic 2009 Thiazole/Thiadiazole,Quinoline/Quinazoline 341.41 2.69 Banyu Tsukuba Research Institute (JAPAN) C14H11N7S2 Iino, T. et al. Discovery and structure-activity relationships of a novel class of quinazoline glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 11501028 250
GKA1-14 GKA1-14 GKA: Systemic 2005 Thiazole/Thiadiazole,Urea,Pyridine 348.42 2.56 OSI Pharmaceuticals (USA); Prosidion Limited (UK) C16H20N4O3S Castelhano, A. L. et al. Glucokinase-activating ureas. Bioorganic Med. Chem. Lett. (2005) 136132253 27
GKA11-5 GKA11-5 GKA: Systemic 2009 Thiazole/Thiadiazole,Quinoline/Quinazoline 355.44 3.09 Banyu Tsukuba Research Institute (JAPAN) C15H13N7S2 Iino, T. et al. Discovery and structure-activity relationships of a novel class of quinazoline glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 11660390 251
GKA1-15 GKA1-15 GKA: Systemic 2005 Thiazole/Thiadiazole,Urea,Sulfoxide/Sulfone derivatives 414.93 3.39 OSI Pharmaceuticals (USA); Prosidion Limited (UK) C16H19ClN4O3S2 Castelhano, A. L. et al. Glucokinase-activating ureas. Bioorganic Med. Chem. Lett. (2005) 44389908 28
GKA11-6 GKA11-6 GKA: Systemic 2009 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives,Quinoline/Quinazoline 412.49 3.95 Banyu Tsukuba Research Institute (JAPAN) C19H16N4O3S2 Iino, T. et al. Discovery and structure-activity relationships of a novel class of quinazoline glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 45483613 252
GKA1-16 GKA1-16 GKA: Systemic 2005 Thiazole/Thiadiazole,Urea 403.85 5.71 OSI Pharmaceuticals (USA); Prosidion Limited (UK) C17H17ClF3N3OS Castelhano, A. L. et al. Glucokinase-activating ureas. Bioorganic Med. Chem. Lett. (2005) 44389913 29
GKA11-7 GKA11-7 GKA: Systemic 2009 Thiazole/Thiadiazole,Quinoline/Quinazoline 352.39 4.81 Banyu Tsukuba Research Institute (JAPAN) C18H13FN4OS Iino, T. et al. Discovery and structure-activity relationships of a novel class of quinazoline glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 45483614 253
GKA1-17 GKA1-17 GKA: Systemic 2005 Thiazole/Thiadiazole,Urea 360.86 4.54 OSI Pharmaceuticals (USA); Prosidion Limited (UK) C17H17ClN4OS Castelhano, A. L. et al. Glucokinase-activating ureas. Bioorganic Med. Chem. Lett. (2005) 44389942 30
GKA11-8 GKA11-8 GKA: Systemic 2009 Thiazole/Thiadiazole,Quinoline/Quinazoline 352.39 4.81 Banyu Tsukuba Research Institute (JAPAN) C18H13FN4OS Iino, T. et al. Discovery and structure-activity relationships of a novel class of quinazoline glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 45483615 254
GKA1-18 GKA1-18 GKA: Systemic 2005 Thiazole/Thiadiazole,Urea 420.96 4.57 OSI Pharmaceuticals (USA); Prosidion Limited (UK) C20H25ClN4O2S Castelhano, A. L. et al. Glucokinase-activating ureas. Bioorganic Med. Chem. Lett. (2005) 44389947 31
GKA1-19 GKA1-19 GKA: Systemic 2005 Thiazole/Thiadiazole,Urea 427.95 6.35 OSI Pharmaceuticals (USA); Prosidion Limited (UK) C22H22ClN3O2S Castelhano, A. L. et al. Glucokinase-activating ureas. Bioorganic Med. Chem. Lett. (2005) 44389877 32
GKA1-20 GKA1-20 GKA: Systemic 2005 Thiazole/Thiadiazole,Urea 384.32 5.81 OSI Pharmaceuticals (USA); Prosidion Limited (UK) C17H19Cl2N3OS Castelhano, A. L. et al. Glucokinase-activating ureas. Bioorganic Med. Chem. Lett. (2005) 44389882 33
GKA1-21 GKA1-21 GKA: Systemic 2005 Thiazole/Thiadiazole,Urea 432.74 5.61 OSI Pharmaceuticals (USA); Prosidion Limited (UK) C16H16BrClFN3OS Castelhano, A. L. et al. Glucokinase-activating ureas. Bioorganic Med. Chem. Lett. (2005) 44389894 34
GKA1-22 GKA1-22 GKA: Systemic 2005 Thiazole/Thiadiazole,Urea 365.88 4.79 OSI Pharmaceuticals (USA); Prosidion Limited (UK) C17H20ClN3O2S Castelhano, A. L. et al. Glucokinase-activating ureas. Bioorganic Med. Chem. Lett. (2005) 44389900 35
GKA12-25 GKA12-25 GKA: Systemic 2009 Pyridine,Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 437.94 2.81 Pfizer Global Research & Development (USA) C20H24ClN3O4S Pfefferkorn, J. A. et al. Pyridones as glucokinase activators: Identification of a unique metabolic liability of the 4-sulfonyl-2-pyridone heterocycle. Bioorganic Med. Chem. Lett. (2009) 54587333 280
GKA12-26 GKA12-26 GKA: Systemic 2009 Pyridine,Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 417.52 2.83 Pfizer Global Research & Development (USA) C21H27N3O4S Pfefferkorn, J. A. et al. Pyridones as glucokinase activators: Identification of a unique metabolic liability of the 4-sulfonyl-2-pyridone heterocycle. Bioorganic Med. Chem. Lett. (2009) 54584389 281
GKA12-27 GKA12-27 GKA: Systemic 2009 Pyridine,Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 431.55 3.27 Pfizer Global Research & Development (USA) C22H29N3O4S Pfefferkorn, J. A. et al. Pyridones as glucokinase activators: Identification of a unique metabolic liability of the 4-sulfonyl-2-pyridone heterocycle. Bioorganic Med. Chem. Lett. (2009) 54580432 282
GKA12-28 GKA12-28 GKA: Systemic 2009 Pyridine,Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 429.53 3.02 Pfizer Global Research & Development (USA) C22H27N3O4S Pfefferkorn, J. A. et al. Pyridones as glucokinase activators: Identification of a unique metabolic liability of the 4-sulfonyl-2-pyridone heterocycle. Bioorganic Med. Chem. Lett. (2009) 54584390 283
GKA12-29 GKA12-29 GKA: Systemic 2009 Pyridine,Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 443.56 3.38 Pfizer Global Research & Development (USA) C23H29N3O4S Pfefferkorn, J. A. et al. Pyridones as glucokinase activators: Identification of a unique metabolic liability of the 4-sulfonyl-2-pyridone heterocycle. Bioorganic Med. Chem. Lett. (2009) 54580433 284
GKA1-23 GKA1-23 GKA: Systemic 2005 Thiazole/Thiadiazole,Urea 392.9 4 OSI Pharmaceuticals (USA); Prosidion Limited (UK) C18H21ClN4O2S Castelhano, A. L. et al. Glucokinase-activating ureas. Bioorganic Med. Chem. Lett. (2005) 11639763 36
GKA12-30 GKA12-30 GKA: Systemic 2009 Pyridine,Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 417.52 2.38 Pfizer Global Research & Development (USA) C21H27N3O4S Pfefferkorn, J. A. et al. Pyridones as glucokinase activators: Identification of a unique metabolic liability of the 4-sulfonyl-2-pyridone heterocycle. Bioorganic Med. Chem. Lett. (2009) 54582448 285
GKA12-31 GKA12-31 GKA: Systemic 2009 Pyridine,Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 465.99 3.61 Pfizer Global Research & Development (USA) C22H28ClN3O4S Pfefferkorn, J. A. et al. Pyridones as glucokinase activators: Identification of a unique metabolic liability of the 4-sulfonyl-2-pyridone heterocycle. Bioorganic Med. Chem. Lett. (2009) 76152153 286
GKA12-32 GKA12-32 GKA: Systemic 2009 Pyridine,Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 445.57 3.18 Pfizer Global Research & Development (USA) C23H31N3O4S Pfefferkorn, J. A. et al. Pyridones as glucokinase activators: Identification of a unique metabolic liability of the 4-sulfonyl-2-pyridone heterocycle. Bioorganic Med. Chem. Lett. (2009) 54583427 287
GKA12-33 GKA12-33 GKA: Systemic 2009 Pyridine,Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 465.99 4.1 Pfizer Global Research & Development (USA) C22H28ClN3O4S Pfefferkorn, J. A. et al. Pyridones as glucokinase activators: Identification of a unique metabolic liability of the 4-sulfonyl-2-pyridone heterocycle. Bioorganic Med. Chem. Lett. (2009) 54584391 288
GKA12-34 GKA12-34 GKA: Systemic 2009 Pyridine,Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 405.51 2.4 Pfizer Global Research & Development (USA) C20H27N3O4S Pfefferkorn, J. A. et al. Pyridones as glucokinase activators: Identification of a unique metabolic liability of the 4-sulfonyl-2-pyridone heterocycle. Bioorganic Med. Chem. Lett. (2009) 54585342 289
GKA12-35 GKA12-35 GKA: Systemic 2009 Pyridine,Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 417.52 2.72 Pfizer Global Research & Development (USA) C21H27N3O4S Pfefferkorn, J. A. et al. Pyridones as glucokinase activators: Identification of a unique metabolic liability of the 4-sulfonyl-2-pyridone heterocycle. Bioorganic Med. Chem. Lett. (2009) 54582449 290
GKA12-36 GKA12-36 GKA: Systemic 2009 Pyridine,Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 445.57 3.81 Pfizer Global Research & Development (USA) C23H31N3O4S Pfefferkorn, J. A. et al. Pyridones as glucokinase activators: Identification of a unique metabolic liability of the 4-sulfonyl-2-pyridone heterocycle. Bioorganic Med. Chem. Lett. (2009) 54585344 291
GKA12-37 GKA12-37 GKA: Systemic 2009 Pyridine,Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 481.56 3.2 Pfizer Global Research & Development (USA) C23H29F2N3O4S Pfefferkorn, J. A. et al. Pyridones as glucokinase activators: Identification of a unique metabolic liability of the 4-sulfonyl-2-pyridone heterocycle. Bioorganic Med. Chem. Lett. (2009) 54582450 292
GKA12-38 GKA12-38 GKA: Systemic 2009 Pyridine,Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 433.52 1.23 Pfizer Global Research & Development (USA) C21H27N3O5S Pfefferkorn, J. A. et al. Pyridones as glucokinase activators: Identification of a unique metabolic liability of the 4-sulfonyl-2-pyridone heterocycle. Bioorganic Med. Chem. Lett. (2009) 54582451 293
GKA12-39 GKA12-39 GKA: Systemic 2009 Pyridine,Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 439.53 2.67 Pfizer Global Research & Development (USA) C23H25N3O4S Pfefferkorn, J. A. et al. Pyridones as glucokinase activators: Identification of a unique metabolic liability of the 4-sulfonyl-2-pyridone heterocycle. Bioorganic Med. Chem. Lett. (2009) 54586308 294
GKA1-24 GKA1-24 GKA: Systemic 2005 Thiazole/Thiadiazole,Urea 378.88 3.7 OSI Pharmaceuticals (USA); Prosidion Limited (UK) C17H19ClN4O2S Castelhano, A. L. et al. Glucokinase-activating ureas. Bioorganic Med. Chem. Lett. (2005) 44389932 37
GKA12-40 GKA12-40 GKA: Systemic 2009 Pyridine,Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 417.52 2.9 Pfizer Global Research & Development (USA) C21H27N3O4S Pfefferkorn, J. A. et al. Pyridones as glucokinase activators: Identification of a unique metabolic liability of the 4-sulfonyl-2-pyridone heterocycle. Bioorganic Med. Chem. Lett. (2009) 54585345 295
GKA12-41 GKA12-41 GKA: Systemic 2009 Pyridine,Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 485.52 3.79 Pfizer Global Research & Development (USA) C22H26F3N3O4S Pfefferkorn, J. A. et al. Pyridones as glucokinase activators: Identification of a unique metabolic liability of the 4-sulfonyl-2-pyridone heterocycle. Bioorganic Med. Chem. Lett. (2009) 54581443 296
GKA12-42 GKA12-42 GKA: Systemic 2009 Pyridine,Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 458.36 3.08 Pfizer Global Research & Development (USA) C19H21Cl2N3O4S Pfefferkorn, J. A. et al. Pyridones as glucokinase activators: Identification of a unique metabolic liability of the 4-sulfonyl-2-pyridone heterocycle. Bioorganic Med. Chem. Lett. (2009) 54580435 297
GKA12-43 GKA12-43 GKA: Systemic 2009 Pyrazine,Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 416.49 1.59 Pfizer Global Research & Development (USA) C20H24N4O4S Pfefferkorn, J. A. et al. Pyridones as glucokinase activators: Identification of a unique metabolic liability of the 4-sulfonyl-2-pyridone heterocycle. Bioorganic Med. Chem. Lett. (2009) 54583428 298
GKA12-44 GKA12-44 GKA: Systemic 2009 Pyrazine,Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 430.52 1.94 Pfizer Global Research & Development (USA) C21H26N4O4S Pfefferkorn, J. A. et al. Pyridones as glucokinase activators: Identification of a unique metabolic liability of the 4-sulfonyl-2-pyridone heterocycle. Bioorganic Med. Chem. Lett. (2009) 54585346 299
GKA12-45 GKA12-45 GKA: Systemic 2009 Pyrazine,Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 466.98 2.58 Pfizer Global Research & Development (USA) C21H27ClN4O4S Pfefferkorn, J. A. et al. Pyridones as glucokinase activators: Identification of a unique metabolic liability of the 4-sulfonyl-2-pyridone heterocycle. Bioorganic Med. Chem. Lett. (2009) 54581444 300
GKA12-46 GKA12-46 GKA: Systemic 2009 Pyrazine,Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 404.48 1.43 Pfizer Global Research & Development (USA) C19H24N4O4S Pfefferkorn, J. A. et al. Pyridones as glucokinase activators: Identification of a unique metabolic liability of the 4-sulfonyl-2-pyridone heterocycle. Bioorganic Med. Chem. Lett. (2009) 44224189 301
GKA12-47 GKA12-47 GKA: Systemic 2009 Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 406.5 2.26 Pfizer Global Research & Development (USA) C19H26N4O4S Pfefferkorn, J. A. et al. Pyridones as glucokinase activators: Identification of a unique metabolic liability of the 4-sulfonyl-2-pyridone heterocycle. Bioorganic Med. Chem. Lett. (2009) 54582452 302
GKA12-48 GKA12-48 GKA: Systemic 2009 Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 420.53 2.28 Pfizer Global Research & Development (USA) C20H28N4O4S Pfefferkorn, J. A. et al. Pyridones as glucokinase activators: Identification of a unique metabolic liability of the 4-sulfonyl-2-pyridone heterocycle. Bioorganic Med. Chem. Lett. (2009) 44224190 303
GKA12-49 GKA12-49 GKA: Systemic 2009 Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 418.51 2.04 Pfizer Global Research & Development (USA) C20H26N4O4S Pfefferkorn, J. A. et al. Pyridones as glucokinase activators: Identification of a unique metabolic liability of the 4-sulfonyl-2-pyridone heterocycle. Bioorganic Med. Chem. Lett. (2009) 54587334 304
GKA1-25 GKA1-25 GKA: Systemic 2005 Thiazole/Thiadiazole,Urea,Pyridine 361.85 3.8 OSI Pharmaceuticals (USA); Prosidion Limited (UK) C16H16ClN5OS Castelhano, A. L. et al. Glucokinase-activating ureas. Bioorganic Med. Chem. Lett. (2005) 44389933 38
GKA12-50 GKA12-50 GKA: Systemic 2009 Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 432.54 2.39 Pfizer Global Research & Development (USA) C21H28N4O4S Pfefferkorn, J. A. et al. Pyridones as glucokinase activators: Identification of a unique metabolic liability of the 4-sulfonyl-2-pyridone heterocycle. Bioorganic Med. Chem. Lett. (2009) 54585347 305
GKA12-51 GKA12-51 GKA: Systemic 2009 Thiazole/Thiadiazole,Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 423.55 3 Pfizer Global Research & Development (USA) C19H25N3O4S2 Pfefferkorn, J. A. et al. Pyridones as glucokinase activators: Identification of a unique metabolic liability of the 4-sulfonyl-2-pyridone heterocycle. Bioorganic Med. Chem. Lett. (2009) 54581445 306
GKA1-26 GKA1-26 GKA: Systemic 2005 Thiazole/Thiadiazole,Urea,Sulfoxide/Sulfone derivatives 427.95 3.44 OSI Pharmaceuticals (USA); Prosidion Limited (UK) C16H14ClN3O3S3 Castelhano, A. L. et al. Glucokinase-activating ureas. Bioorganic Med. Chem. Lett. (2005) 44389937 39
GKA12-7 GKA12-7 GKA: Systemic 2009 Pyridine,Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 403.5 2.47 Pfizer Global Research & Development (USA) C20H25N3O4S Pfefferkorn, J. A. et al. Pyridones as glucokinase activators: Identification of a unique metabolic liability of the 4-sulfonyl-2-pyridone heterocycle. Bioorganic Med. Chem. Lett. (2009) 54581442 279
GKA1-27 GKA1-27 GKA: Systemic 2005 Thiazole/Thiadiazole,Urea,Sulfoxide/Sulfone derivatives 427.95 3.41 OSI Pharmaceuticals (USA); Prosidion Limited (UK) C16H14ClN3O3S3 Castelhano, A. L. et al. Glucokinase-activating ureas. Bioorganic Med. Chem. Lett. (2005) 44389938 40
GKA1-28 GKA1-28 GKA: Systemic 2005 Thiazole/Thiadiazole,Urea,Sulfoxide/Sulfone derivatives 472.4 3.47 OSI Pharmaceuticals (USA); Prosidion Limited (UK) C16H14BrN3O3S3 Castelhano, A. L. et al. Glucokinase-activating ureas. Bioorganic Med. Chem. Lett. (2005) 44389874 41
GKA1-29 GKA1-29 GKA: Systemic 2005 Thiazole/Thiadiazole,Urea,Sulfoxide/Sulfone derivatives 473.39 2.86 OSI Pharmaceuticals (USA); Prosidion Limited (UK) C15H13BrN4O3S3 Castelhano, A. L. et al. Glucokinase-activating ureas. Bioorganic Med. Chem. Lett. (2005) 44389875 42
GKA1-3 GKA1-3 GKA: Systemic 2005 Thiazole/Thiadiazole,Urea,Sulfoxide/Sulfone derivatives 379.5 3.1 OSI Pharmaceuticals (USA); Prosidion Limited (UK) C17H21N3O3S2 Castelhano, A. L. et al. Glucokinase-activating ureas. Bioorganic Med. Chem. Lett. (2005) 44389921 16
GKA1-30 GKA1-30 GKA: Systemic 2005 Thiazole/Thiadiazole,Urea,Sulfoxide/Sulfone derivatives 411.88 2.83 OSI Pharmaceuticals (USA); Prosidion Limited (UK) C16H14ClN3O4S2 Castelhano, A. L. et al. Glucokinase-activating ureas. Bioorganic Med. Chem. Lett. (2005) 44389885 43
GKA1-31 GKA1-31 GKA: Systemic 2005 Thiazole/Thiadiazole,Urea,Sulfoxide/Sulfone derivatives 415.91 2.64 OSI Pharmaceuticals (USA); Prosidion Limited (UK) C16H18ClN3O4S2 Castelhano, A. L. et al. Glucokinase-activating ureas. Bioorganic Med. Chem. Lett. (2005) 44389889 44
GKA1-32 GKA1-32 GKA: Systemic 2005 Thiazole/Thiadiazole,Urea,Sulfoxide/Sulfone derivatives 415.91 2.47 OSI Pharmaceuticals (USA); Prosidion Limited (UK) C16H18ClN3O4S2 Castelhano, A. L. et al. Glucokinase-activating ureas. Bioorganic Med. Chem. Lett. (2005) 44389903 45
GKA13-2a GKA13-2a GKA: Systemic 2009 Pyridine,Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 478.56 2.91 Banyu Tsukuba Research Institute (JAPAN) C25H26N4O4S Takahashi, K. et al. The design and optimization of a series of 2-(pyridin-2-yl)-1H-benzimidazole compounds as allosteric glucokinase activators. Bioorganic Med. Chem. (2009) 46226729 307
GKA13-2b GKA13-2b GKA: Systemic 2009 Pyridine,Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 464.54 2.54 Banyu Tsukuba Research Institute (JAPAN) C24H24N4O4S Takahashi, K. et al. The design and optimization of a series of 2-(pyridin-2-yl)-1H-benzimidazole compounds as allosteric glucokinase activators. Bioorganic Med. Chem. (2009) 11605090 308
GKA13-2c GKA13-2c GKA: Systemic 2009 Pyridine,Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 450.51 2.36 Banyu Tsukuba Research Institute (JAPAN) C23H22N4O4S Takahashi, K. et al. The design and optimization of a series of 2-(pyridin-2-yl)-1H-benzimidazole compounds as allosteric glucokinase activators. Bioorganic Med. Chem. (2009) 46226671 309
GKA13-2d GKA13-2d GKA: Systemic 2009 Pyridine,Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 478.56 2.94 Banyu Tsukuba Research Institute (JAPAN) C25H26N4O4S Takahashi, K. et al. The design and optimization of a series of 2-(pyridin-2-yl)-1H-benzimidazole compounds as allosteric glucokinase activators. Bioorganic Med. Chem. (2009) 46226674 310
GKA1-33 GKA1-33 GKA: Systemic 2005 Thiazole/Thiadiazole,Urea,Sulfoxide/Sulfone derivatives 429.94 2.83 OSI Pharmaceuticals (USA); Prosidion Limited (UK) C17H20ClN3O4S2 Castelhano, A. L. et al. Glucokinase-activating ureas. Bioorganic Med. Chem. Lett. (2005) 44389905 46
GKA13-3a GKA13-3a GKA: Systemic 2009 Pyridine,Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 476.55 2.61 Banyu Tsukuba Research Institute (JAPAN) C25H24N4O4S Takahashi, K. et al. The design and optimization of a series of 2-(pyridin-2-yl)-1H-benzimidazole compounds as allosteric glucokinase activators. Bioorganic Med. Chem. (2009) 46226685 311
GKA13-3b GKA13-3b GKA: Systemic 2009 Pyridine,Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 478.52 2.72 Banyu Tsukuba Research Institute (JAPAN) C24H22N4O5S Takahashi, K. et al. The design and optimization of a series of 2-(pyridin-2-yl)-1H-benzimidazole compounds as allosteric glucokinase activators. Bioorganic Med. Chem. (2009) 44555462 312
GKA13-3c GKA13-3c GKA: Systemic 2009 Pyridine,Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 491.56 2.33 Banyu Tsukuba Research Institute (JAPAN) C25H25N5O4S Takahashi, K. et al. The design and optimization of a series of 2-(pyridin-2-yl)-1H-benzimidazole compounds as allosteric glucokinase activators. Bioorganic Med. Chem. (2009) 46226704 313
GKA13-3d GKA13-3d GKA: Systemic 2009 Pyridine,Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 477.54 2.15 Banyu Tsukuba Research Institute (JAPAN) C24H23N5O4S Takahashi, K. et al. The design and optimization of a series of 2-(pyridin-2-yl)-1H-benzimidazole compounds as allosteric glucokinase activators. Bioorganic Med. Chem. (2009) 46226705 314
GKA13-3e GKA13-3e GKA: Systemic 2009 Pyridine,Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 512.6 2.46 Banyu Tsukuba Research Institute (JAPAN) C24H24N4O5S2 Takahashi, K. et al. The design and optimization of a series of 2-(pyridin-2-yl)-1H-benzimidazole compounds as allosteric glucokinase activators. Bioorganic Med. Chem. (2009) 11649204 315
GKA13-3f GKA13-3f GKA: Systemic 2009 Pyridine,Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 492.55 2.2 Banyu Tsukuba Research Institute (JAPAN) C25H24N4O5S Takahashi, K. et al. The design and optimization of a series of 2-(pyridin-2-yl)-1H-benzimidazole compounds as allosteric glucokinase activators. Bioorganic Med. Chem. (2009) 46226734 316
GKA13-3g GKA13-3g GKA: Systemic 2009 Pyridine,Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 490.53 1.97 Banyu Tsukuba Research Institute (JAPAN) C25H22N4O5S Takahashi, K. et al. The design and optimization of a series of 2-(pyridin-2-yl)-1H-benzimidazole compounds as allosteric glucokinase activators. Bioorganic Med. Chem. (2009) 11562233 317
GKA13-3h GKA13-3h GKA: Systemic 2009 Pyridine,Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 492.5 2.53 Banyu Tsukuba Research Institute (JAPAN) C24H20N4O6S Takahashi, K. et al. The design and optimization of a series of 2-(pyridin-2-yl)-1H-benzimidazole compounds as allosteric glucokinase activators. Bioorganic Med. Chem. (2009) 44555463 318
GKA13-3i GKA13-3i GKA: Systemic 2009 Pyridine,Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 505.55 2.14 Banyu Tsukuba Research Institute (JAPAN) C25H23N5O5S Takahashi, K. et al. The design and optimization of a series of 2-(pyridin-2-yl)-1H-benzimidazole compounds as allosteric glucokinase activators. Bioorganic Med. Chem. (2009) 11504344 319
GKA13-3j GKA13-3j GKA: Systemic 2009 Pyridine,Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 462.56 3.57 Banyu Tsukuba Research Institute (JAPAN) C25H26N4O3S Takahashi, K. et al. The design and optimization of a series of 2-(pyridin-2-yl)-1H-benzimidazole compounds as allosteric glucokinase activators. Bioorganic Med. Chem. (2009) 46226682 320
GKA13-3k GKA13-3k GKA: Systemic 2009 Pyridine,Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 459.52 2.93 Banyu Tsukuba Research Institute (JAPAN) C24H21N5O3S Takahashi, K. et al. The design and optimization of a series of 2-(pyridin-2-yl)-1H-benzimidazole compounds as allosteric glucokinase activators. Bioorganic Med. Chem. (2009) 46226690 321
GKA13-3l GKA13-3l GKA: Systemic 2009 Pyridine,Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 475.52 2.85 Banyu Tsukuba Research Institute (JAPAN) C23H21N7O3S Takahashi, K. et al. The design and optimization of a series of 2-(pyridin-2-yl)-1H-benzimidazole compounds as allosteric glucokinase activators. Bioorganic Med. Chem. (2009) 46226664 322
GKA1-4 GKA1-4 GKA: Systemic 2005 Thiazole/Thiadiazole,Urea,Sulfoxide/Sulfone derivatives 448.48 3.43 OSI Pharmaceuticals (USA); Prosidion Limited (UK) C17H19F3N4O3S2 Castelhano, A. L. et al. Glucokinase-activating ureas. Bioorganic Med. Chem. Lett. (2005) 44389935 17
GKA14-12 GKA14-12 GKA: Systemic 2009 Benzamide 357.41 2.54 Chinese Academy of Sciences (Shanghai, CHINA) C17H16FN5OS Zhang, L. et al. Benzamide derivatives as dual-action hypoglycemic agents that inhibit glycogen phosphorylase and activate glucokinase. Bioorganic Med. Chem. (2009) 44263455 323
GKA14-13a GKA14-13a GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide 360.43 3.48 Chinese Academy of Sciences (Shanghai, CHINA) C16H13FN4OS2 Zhang, L. et al. Benzamide derivatives as dual-action hypoglycemic agents that inhibit glycogen phosphorylase and activate glucokinase. Bioorganic Med. Chem. (2009) 44263456 324
GKA14-13b GKA14-13b GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide 374.46 3.88 Chinese Academy of Sciences (Shanghai, CHINA) C17H15FN4OS2 Zhang, L. et al. Benzamide derivatives as dual-action hypoglycemic agents that inhibit glycogen phosphorylase and activate glucokinase. Bioorganic Med. Chem. (2009) 44263457 325
GKA14-13c GKA14-13c GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide 361.42 2.89 Chinese Academy of Sciences (Shanghai, CHINA) C15H12FN5OS2 Zhang, L. et al. Benzamide derivatives as dual-action hypoglycemic agents that inhibit glycogen phosphorylase and activate glucokinase. Bioorganic Med. Chem. (2009) 44263458 326
GKA14-13d GKA14-13d GKA: Systemic 2009 Benzamide,Pyridine 354.4 3.38 Chinese Academy of Sciences (Shanghai, CHINA) C18H15FN4OS Zhang, L. et al. Benzamide derivatives as dual-action hypoglycemic agents that inhibit glycogen phosphorylase and activate glucokinase. Bioorganic Med. Chem. (2009) 44263459 327
GKA14-13e GKA14-13e GKA: Systemic 2009 Benzamide,Pyrimidine 383.44 3.53 Chinese Academy of Sciences (Shanghai, CHINA) C19H18FN5OS Zhang, L. et al. Benzamide derivatives as dual-action hypoglycemic agents that inhibit glycogen phosphorylase and activate glucokinase. Bioorganic Med. Chem. (2009) 44263460 328
GKA14-13f GKA14-13f GKA: Systemic 2009 Benzamide 357.41 1.99 Chinese Academy of Sciences (Shanghai, CHINA) C17H16FN5OS Zhang, L. et al. Benzamide derivatives as dual-action hypoglycemic agents that inhibit glycogen phosphorylase and activate glucokinase. Bioorganic Med. Chem. (2009) 44263461 329
GKA14-13g GKA14-13g GKA: Systemic 2009 Benzamide 371.43 2.08 Chinese Academy of Sciences (Shanghai, CHINA) C18H18FN5OS Zhang, L. et al. Benzamide derivatives as dual-action hypoglycemic agents that inhibit glycogen phosphorylase and activate glucokinase. Bioorganic Med. Chem. (2009) 44263462 330
GKA14-13h GKA14-13h GKA: Systemic 2009 Benzamide 410.39 4.11 Chinese Academy of Sciences (Shanghai, CHINA) C18H14F4N4OS Zhang, L. et al. Benzamide derivatives as dual-action hypoglycemic agents that inhibit glycogen phosphorylase and activate glucokinase. Bioorganic Med. Chem. (2009) 44263463 331
GKA14-13i GKA14-13i GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide 413.41 5.05 Chinese Academy of Sciences (Shanghai, CHINA) C17H11F4N3OS2 Zhang, L. et al. Benzamide derivatives as dual-action hypoglycemic agents that inhibit glycogen phosphorylase and activate glucokinase. Bioorganic Med. Chem. (2009) 44263464 332
GKA14-13j GKA14-13j GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide 427.44 5.45 Chinese Academy of Sciences (Shanghai, CHINA) C18H13F4N3OS2 Zhang, L. et al. Benzamide derivatives as dual-action hypoglycemic agents that inhibit glycogen phosphorylase and activate glucokinase. Bioorganic Med. Chem. (2009) 44263465 333
GKA14-13k GKA14-13k GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide 414.4 4.46 Chinese Academy of Sciences (Shanghai, CHINA) C16H10F4N4OS2 Zhang, L. et al. Benzamide derivatives as dual-action hypoglycemic agents that inhibit glycogen phosphorylase and activate glucokinase. Bioorganic Med. Chem. (2009) 44263466 334
GKA14-13l GKA14-13l GKA: Systemic 2009 Benzamide 367.4 2.94 Chinese Academy of Sciences (Shanghai, CHINA) C18H14FN5OS Zhang, L. et al. Benzamide derivatives as dual-action hypoglycemic agents that inhibit glycogen phosphorylase and activate glucokinase. Bioorganic Med. Chem. (2009) 44263467 335
GKA14-13m GKA14-13m GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide 370.42 3.88 Chinese Academy of Sciences (Shanghai, CHINA) C17H11FN4OS2 Zhang, L. et al. Benzamide derivatives as dual-action hypoglycemic agents that inhibit glycogen phosphorylase and activate glucokinase. Bioorganic Med. Chem. (2009) 44263468 336
GKA14-13n GKA14-13n GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide 384.45 4.28 Chinese Academy of Sciences (Shanghai, CHINA) C18H13FN4OS2 Zhang, L. et al. Benzamide derivatives as dual-action hypoglycemic agents that inhibit glycogen phosphorylase and activate glucokinase. Bioorganic Med. Chem. (2009) 44263469 337
GKA14-13o GKA14-13o GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide 371.41 3.29 Chinese Academy of Sciences (Shanghai, CHINA) C16H10FN5OS2 Zhang, L. et al. Benzamide derivatives as dual-action hypoglycemic agents that inhibit glycogen phosphorylase and activate glucokinase. Bioorganic Med. Chem. (2009) 44263470 338
GKA14-13p GKA14-13p GKA: Systemic 2009 Benzamide,Pyrimidine 393.44 3.93 Chinese Academy of Sciences (Shanghai, CHINA) C20H16FN5OS Zhang, L. et al. Benzamide derivatives as dual-action hypoglycemic agents that inhibit glycogen phosphorylase and activate glucokinase. Bioorganic Med. Chem. (2009) 44263471 339
GKA14-13q GKA14-13q GKA: Systemic 2009 Benzamide 360.38 3.32 Chinese Academy of Sciences (Shanghai, CHINA) C17H14F2N4OS Zhang, L. et al. Benzamide derivatives as dual-action hypoglycemic agents that inhibit glycogen phosphorylase and activate glucokinase. Bioorganic Med. Chem. (2009) 44263472 340
GKA14-13r GKA14-13r GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide 363.4 4.26 Chinese Academy of Sciences (Shanghai, CHINA) C16H11F2N3OS2 Zhang, L. et al. Benzamide derivatives as dual-action hypoglycemic agents that inhibit glycogen phosphorylase and activate glucokinase. Bioorganic Med. Chem. (2009) 44263473 341
GKA14-13s GKA14-13s GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide 364.39 3.67 Chinese Academy of Sciences (Shanghai, CHINA) C15H10F2N4OS2 Zhang, L. et al. Benzamide derivatives as dual-action hypoglycemic agents that inhibit glycogen phosphorylase and activate glucokinase. Bioorganic Med. Chem. (2009) 44263474 342
GKA14-13t GKA14-13t GKA: Systemic 2009 Benzamide,Pyridine 357.38 4.16 Chinese Academy of Sciences (Shanghai, CHINA) C18H13F2N3OS Zhang, L. et al. Benzamide derivatives as dual-action hypoglycemic agents that inhibit glycogen phosphorylase and activate glucokinase. Bioorganic Med. Chem. (2009) 44263475 343
GKA14-13u GKA14-13u GKA: Systemic 2009 Benzamide 397.4 5.07 Chinese Academy of Sciences (Shanghai, CHINA) C20H13F2N3O2S Zhang, L. et al. Benzamide derivatives as dual-action hypoglycemic agents that inhibit glycogen phosphorylase and activate glucokinase. Bioorganic Med. Chem. (2009) 44263476 344
GKA14-13v GKA14-13v GKA: Systemic 2009 Benzamide 372.42 3.19 Chinese Academy of Sciences (Shanghai, CHINA) C18H17FN4O2S Zhang, L. et al. Benzamide derivatives as dual-action hypoglycemic agents that inhibit glycogen phosphorylase and activate glucokinase. Bioorganic Med. Chem. (2009) 44263477 345
GKA14-13w GKA14-13w GKA: Systemic 2009 Benzamide 372.42 3.19 Chinese Academy of Sciences (Shanghai, CHINA) C18H17FN4O2S Zhang, L. et al. Benzamide derivatives as dual-action hypoglycemic agents that inhibit glycogen phosphorylase and activate glucokinase. Bioorganic Med. Chem. (2009) 44263478 346
GKA14-13x GKA14-13x GKA: Systemic 2009 Benzamide 402.44 3.16 Chinese Academy of Sciences (Shanghai, CHINA) C19H19FN4O3S Zhang, L. et al. Benzamide derivatives as dual-action hypoglycemic agents that inhibit glycogen phosphorylase and activate glucokinase. Bioorganic Med. Chem. (2009) 44263479 347
GKA14-14a GKA14-14a GKA: Systemic 2009 328.38 2.18 Chinese Academy of Sciences (Shanghai, CHINA) C18H21FN4O Zhang, L. et al. Benzamide derivatives as dual-action hypoglycemic agents that inhibit glycogen phosphorylase and activate glucokinase. Bioorganic Med. Chem. (2009) 28336011 348
GKA14-14b GKA14-14b GKA: Systemic 2009 381.37 3.74 Chinese Academy of Sciences (Shanghai, CHINA) C19H19F4N3O Zhang, L. et al. Benzamide derivatives as dual-action hypoglycemic agents that inhibit glycogen phosphorylase and activate glucokinase. Bioorganic Med. Chem. (2009) 4002132 349
GKA14-14c GKA14-14c GKA: Systemic 2009 331.36 2.96 Chinese Academy of Sciences (Shanghai, CHINA) C18H19F2N3O Zhang, L. et al. Benzamide derivatives as dual-action hypoglycemic agents that inhibit glycogen phosphorylase and activate glucokinase. Bioorganic Med. Chem. (2009) 2264867 350
GKA14-14d GKA14-14d GKA: Systemic 2009 338.38 2.58 Chinese Academy of Sciences (Shanghai, CHINA) C19H19FN4O Zhang, L. et al. Benzamide derivatives as dual-action hypoglycemic agents that inhibit glycogen phosphorylase and activate glucokinase. Bioorganic Med. Chem. (2009) 27150838 351
GKA14-14e GKA14-14e GKA: Systemic 2009 391.41 2.9 Chinese Academy of Sciences (Shanghai, CHINA) C20H23F2N3O3 Zhang, L. et al. Benzamide derivatives as dual-action hypoglycemic agents that inhibit glycogen phosphorylase and activate glucokinase. Bioorganic Med. Chem. (2009) 44263480 352
GKA14-15a GKA14-15a GKA: Systemic 2009 Benzamide 376.41 4.09 Chinese Academy of Sciences (Shanghai, CHINA) C22H20N2O4 Zhang, L. et al. Benzamide derivatives as dual-action hypoglycemic agents that inhibit glycogen phosphorylase and activate glucokinase. Bioorganic Med. Chem. (2009) 984599 353
GKA14-15b GKA14-15b GKA: Systemic 2009 Benzamide 376.41 3.53 Chinese Academy of Sciences (Shanghai, CHINA) C22H20N2O4 Zhang, L. et al. Benzamide derivatives as dual-action hypoglycemic agents that inhibit glycogen phosphorylase and activate glucokinase. Bioorganic Med. Chem. (2009) 138884 354
GKA14-15c GKA14-15c GKA: Systemic 2009 Benzamide 376.41 3.66 Chinese Academy of Sciences (Shanghai, CHINA) C22H20N2O4 Zhang, L. et al. Benzamide derivatives as dual-action hypoglycemic agents that inhibit glycogen phosphorylase and activate glucokinase. Bioorganic Med. Chem. (2009) 295310 355
GKA1-5 GKA1-5 GKA: Systemic 2005 Thiazole/Thiadiazole,Urea,Sulfoxide/Sulfone derivatives 413.94 4.06 OSI Pharmaceuticals (USA); Prosidion Limited (UK) C17H20ClN3O3S2 Castelhano, A. L. et al. Glucokinase-activating ureas. Bioorganic Med. Chem. Lett. (2005) 44389949 18
GKA15-1 GKA15-1 GKA: Systemic 2010 Urea 303.18 3.87 Hoffmann-La Roche Inc. (USA) C13H16Cl2N2O2 Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 12044462 356
GKA15-16 GKA15-16 GKA: Systemic 2010 Urea 355.26 4.55 Hoffmann-La Roche Inc. (USA) C17H20Cl2N2O2 Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 46223342 389
GKA15-17 GKA15-17 GKA: Systemic 2010 328.24 4.83 Hoffmann-La Roche Inc. (USA) C15H19Cl2N3O Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 46223343 390
GKA15-18 GKA15-18 GKA: Systemic 2010 Urea 357.27 5.32 Hoffmann-La Roche Inc. (USA) C17H22Cl2N2O2 Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 46223344 391
GKA15-19 GKA15-19 GKA: Systemic 2010 Urea 331.24 3.91 Hoffmann-La Roche Inc. (USA) C15H20Cl2N2O2 Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 46223568 392
GKA15-20 GKA15-20 GKA: Systemic 2010 359.31 5.74 Hoffmann-La Roche Inc. (USA) C16H20Cl2N2OS Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 46223569 393
GKA15-5a GKA15-5a GKA: Systemic 2010 Urea 301.17 3.66 Hoffmann-La Roche Inc. (USA) C13H14Cl2N2O2 Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 18626628 357
GKA15-5b GKA15-5b GKA: Systemic 2010 Urea 315.2 4.2 Hoffmann-La Roche Inc. (USA) C14H16Cl2N2O2 Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 18626630 358
GKA15-5c GKA15-5c GKA: Systemic 2010 Urea 329.22 4.74 Hoffmann-La Roche Inc. (USA) C15H18Cl2N2O2 Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 18626611 359
GKA15-5d GKA15-5d GKA: Systemic 2010 Urea 343.25 5.28 Hoffmann-La Roche Inc. (USA) C16H20Cl2N2O2 Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 12044450 360
GKA15-5e GKA15-5e GKA: Systemic 2010 Urea 357.27 5.82 Hoffmann-La Roche Inc. (USA) C17H22Cl2N2O2 Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 18626629 361
GKA15-5f GKA15-5f GKA: Systemic 2010 Urea 317.21 4.27 Hoffmann-La Roche Inc. (USA) C14H18Cl2N2O2 Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 18626608 362
GKA15-5g GKA15-5g GKA: Systemic 2010 Urea 357.27 5.68 Hoffmann-La Roche Inc. (USA) C17H22Cl2N2O2 Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 18626634 363
GKA15-5h GKA15-5h GKA: Systemic 2010 Urea 343.25 5.14 Hoffmann-La Roche Inc. (USA) C16H20Cl2N2O2 Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 12044460 364
GKA15-5i GKA15-5i GKA: Systemic 2010 Urea 357.27 5.68 Hoffmann-La Roche Inc. (USA) C17H22Cl2N2O2 Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 46224057 365
GKA15-5j GKA15-5j GKA: Systemic 2010 Urea 357.27 5.51 Hoffmann-La Roche Inc. (USA) C17H22Cl2N2O2 Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 12044461 366
GKA15-5k GKA15-5k GKA: Systemic 2010 Urea 371.3 6.04 Hoffmann-La Roche Inc. (USA) C18H24Cl2N2O2 Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 18626606 367
GKA15-5l GKA15-5l GKA: Systemic 2010 Urea 369.29 5.78 Hoffmann-La Roche Inc. (USA) C18H22Cl2N2O2 Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 12044467 368
GKA15-5m GKA15-5m GKA: Systemic 2010 Urea 385.33 6.47 Hoffmann-La Roche Inc. (USA) C19H26Cl2N2O2 Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 46224058 369
GKA15-5n GKA15-5n GKA: Systemic 2010 Urea 385.33 6.39 Hoffmann-La Roche Inc. (USA) C19H26Cl2N2O2 Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 46220715 370
GKA15-5o GKA15-5o GKA: Systemic 2010 Urea 415.31 5.43 Hoffmann-La Roche Inc. (USA) C19H24Cl2N2O4 Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 12044466 371
GKA15-5p GKA15-5p GKA: Systemic 2010 Urea 387.26 4.74 Hoffmann-La Roche Inc. (USA) C17H20Cl2N2O4 Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 22975836 372
GKA15-5q GKA15-5q GKA: Systemic 2010 Urea 401.28 5.06 Hoffmann-La Roche Inc. (USA) C18H22Cl2N2O4 Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 12044464 373
GKA15-5r GKA15-5r GKA: Systemic 2010 Urea 429.34 5.33 Hoffmann-La Roche Inc. (USA) C20H26Cl2N2O4 Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 46220716 374
GKA15-5s GKA15-5s GKA: Systemic 2010 Urea 401.28 4.64 Hoffmann-La Roche Inc. (USA) C18H22Cl2N2O4 Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 18626620 375
GKA15-5t GKA15-5t GKA: Systemic 2010 Urea 415.31 4.97 Hoffmann-La Roche Inc. (USA) C19H24Cl2N2O4 Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 12044465 376
GKA15-5u GKA15-5u GKA: Systemic 2010 Urea 373.27 4.46 Hoffmann-La Roche Inc. (USA) C17H22Cl2N2O3 Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 18626615 377
GKA15-5v GKA15-5v GKA: Systemic 2010 Urea 308.8 4.51 Hoffmann-La Roche Inc. (USA) C16H21ClN2O2 Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 12044451 378
GKA15-5w GKA15-5w GKA: Systemic 2010 Urea 308.8 4.51 Hoffmann-La Roche Inc. (USA) C16H21ClN2O2 Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 12044453 379
GKA15-5x GKA15-5x GKA: Systemic 2010 Urea 274.36 3.89 Hoffmann-La Roche Inc. (USA) C16H22N2O2 Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 12044455 380
GKA15-5y GKA15-5y GKA: Systemic 2010 Urea 310.34 4.09 Hoffmann-La Roche Inc. (USA) C16H20F2N2O2 Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 12044452 381
GKA15-5z GKA15-5z GKA: Systemic 2010 Urea 353.25 4.58 Hoffmann-La Roche Inc. (USA) C16H21BrN2O2 Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 12044456 382
GKA15-5za GKA15-5za GKA: Systemic 2010 Urea 319.36 3.71 Hoffmann-La Roche Inc. (USA) C16H21N3O4 Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 12044454 383
GKA15-5zb GKA15-5zb GKA: Systemic 2010 Urea 320.45 4.4 Hoffmann-La Roche Inc. (USA) C17H24N2O2S Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 12044459 384
GKA15-5zc GKA15-5zc GKA: Systemic 2010 Urea 374.42 5.61 Hoffmann-La Roche Inc. (USA) C17H21F3N2O2S Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 12044457 385
GKA15-5zd GKA15-5zd GKA: Systemic 2010 Urea,Sulfoxide/Sulfone derivatives 352.45 3.12 Hoffmann-La Roche Inc. (USA) C17H24N2O4S Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 18626646 386
GKA15-5ze GKA15-5ze GKA: Systemic 2010 Urea,Sulfoxide/Sulfone derivatives 406.42 4.33 Hoffmann-La Roche Inc. (USA) C17H21F3N2O4S Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 12044458 387
GKA15-5zf GKA15-5zf GKA: Systemic 2010 Urea,Sulfoxide/Sulfone derivatives 406.42 4.33 Hoffmann-La Roche Inc. (USA) C17H21F3N2O4S Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 18626605 388
GKA15-8a GKA15-8a GKA: Systemic 2010 Thiazole/Thiadiazole 369.31 5.9 Hoffmann-La Roche Inc. (USA) C17H18Cl2N2OS Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 54293052 396
GKA15-8b GKA15-8b GKA: Systemic 2010 Thiazole/Thiadiazole 377.29 5.3 Hoffmann-La Roche Inc. (USA) C18H14Cl2N2OS Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 46221387 397
GKA15-8c GKA15-8c GKA: Systemic 2010 Thiazole/Thiadiazole 383.34 6.3 Hoffmann-La Roche Inc. (USA) C18H20Cl2N2OS Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 22315184 398
GKA15-8d GKA15-8d GKA: Systemic 2010 Thiazole/Thiadiazole 383.34 6.3 Hoffmann-La Roche Inc. (USA) C18H20Cl2N2OS Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 22315145 399
GKA15-8e GKA15-8e GKA: Systemic 2010 Thiazole/Thiadiazole 397.36 6.7 Hoffmann-La Roche Inc. (USA) C19H22Cl2N2OS Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 46221595 400
GKA15-8f GKA15-8f GKA: Systemic 2010 Thiazole/Thiadiazole 441.37 6.46 Hoffmann-La Roche Inc. (USA) C20H22Cl2N2O3S Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 46221596 401
GKA15-8g GKA15-8g GKA: Systemic 2010 Thiazole/Thiadiazole 427.34 6.09 Hoffmann-La Roche Inc. (USA) C19H20Cl2N2O3S Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 53844435 402
GKA15-8h GKA15-8h GKA: Systemic 2010 Thiazole/Thiadiazole 399.33 5.05 Hoffmann-La Roche Inc. (USA) C18H20Cl2N2O2S Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 22315087 403
GKA15-8i GKA15-8i GKA: Systemic 2010 Thiazole/Thiadiazole 413.32 5.76 Hoffmann-La Roche Inc. (USA) C18H18Cl2N2O3S Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 12088922 404
GKA15-8j GKA15-8j GKA: Systemic 2010 Thiazole/Thiadiazole 441.37 6.46 Hoffmann-La Roche Inc. (USA) C20H22Cl2N2O3S Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 46221597 405
GKA15-8k GKA15-8k GKA: Systemic 2010 Thiazole/Thiadiazole 413.32 5.76 Hoffmann-La Roche Inc. (USA) C18H18Cl2N2O3S Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 22315271 406
GKA15-8l GKA15-8l GKA: Systemic 2010 Thiazole/Thiadiazole 427.34 6.09 Hoffmann-La Roche Inc. (USA) C19H20Cl2N2O3S Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 46221803 407
GKA15-8m GKA15-8m GKA: Systemic 2010 Thiazole/Thiadiazole 399.33 5.05 Hoffmann-La Roche Inc. (USA) C18H20Cl2N2O2S Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 12088921 408
GKA15-8n GKA15-8n GKA: Systemic 2010 Thiazole/Thiadiazole 455.4 6.09 Hoffmann-La Roche Inc. (USA) C21H24Cl2N2O3S Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 46221804 409
GKA15-8o GKA15-8o GKA: Systemic 2010 Thiazole/Thiadiazole 427.34 5.4 Hoffmann-La Roche Inc. (USA) C19H20Cl2N2O3S Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 9954241 410
GKA15-8p GKA15-8p GKA: Systemic 2010 Thiazole/Thiadiazole 441.37 5.73 Hoffmann-La Roche Inc. (USA) C20H22Cl2N2O3S Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 9932967 411
GKA15-8q GKA15-8q GKA: Systemic 2010 Thiazole/Thiadiazole 413.36 5.51 Hoffmann-La Roche Inc. (USA) C19H22Cl2N2O2S Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 9801831 412
GKA15-8r GKA15-8r GKA: Systemic 2010 Thiazole/Thiadiazole 334.86 5.27 Hoffmann-La Roche Inc. (USA) C17H19ClN2OS Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 9884133 413
GKA15-8s GKA15-8s GKA: Systemic 2010 Thiazole/Thiadiazole 334.86 5.27 Hoffmann-La Roche Inc. (USA) C17H19ClN2OS Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 9905747 414
GKA15-8t GKA15-8t GKA: Systemic 2010 Thiazole/Thiadiazole 345.42 4.48 Hoffmann-La Roche Inc. (USA) C17H19N3O3S Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 22315106 415
GKA15-8u GKA15-8u GKA: Systemic 2010 Thiazole/Thiadiazole 346.51 5.16 Hoffmann-La Roche Inc. (USA) C18H22N2OS2 Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 12088916 416
GKA15-8v GKA15-8v GKA: Systemic 2010 Thiazole/Thiadiazole 362.51 3.77 Hoffmann-La Roche Inc. (USA) C18H22N2O2S2 Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 22315147 417
GKA15-8w GKA15-8w GKA: Systemic 2010 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 378.51 3.88 Hoffmann-La Roche Inc. (USA) C18H22N2O3S2 Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 9886086 418
GKA15-8x GKA15-8x GKA: Systemic 2010 Thiazole/Thiadiazole 400.48 6.37 Hoffmann-La Roche Inc. (USA) C18H19F3N2OS2 Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 12088917 419
GKA15-8y GKA15-8y GKA: Systemic 2010 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 432.48 5.09 Hoffmann-La Roche Inc. (USA) C18H19F3N2O3S2 Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 12088918 420
GKA15-8z GKA15-8z GKA: Systemic 2010 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 432.48 5.09 Hoffmann-La Roche Inc. (USA) C18H19F3N2O3S2 Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 22315142 421
GKA15-9a GKA15-9a GKA: Systemic 2010 Urea 343.25 5.14 Hoffmann-La Roche Inc. (USA) C16H20Cl2N2O2 Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 12044460 394
GKA15-9b GKA15-9b GKA: Systemic 2010 Urea 343.25 5.14 Hoffmann-La Roche Inc. (USA) C16H20Cl2N2O2 Haynes, N. E. et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2 R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N- thiazol-2-yl-propionamide (RO0281675). J. Med. Chem. (2010) 46222021 395
GKA1-6 GKA1-6 GKA: Systemic 2005 Urea,Benzo/Pyrido-thiazole,Sulfoxide/Sulfone derivatives 507.65 3.76 OSI Pharmaceuticals (USA); Prosidion Limited (UK) C22H25N3O5S3 Castelhano, A. L. et al. Glucokinase-activating ureas. Bioorganic Med. Chem. Lett. (2005) 44389884 19
GKA16-9a GKA16-9a GKA: Systemic 2010 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 394.51 2.28 Chinese Academy of Sciences (Shanghai, CHINA) C18H22N2O4S2 Li, F. et al. Design, synthesis, and pharmacological evaluation of N-(4-mono and 4,5-disubstituted thiazol-2-yl)-2-aryl-3-(tetrahydro-2H-pyran-4-yl)propanamides as glucokinase activators. Bioorganic Med. Chem. (2010) 10250045 422
GKA16-9b GKA16-9b GKA: Systemic 2010 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 422.56 3.12 Chinese Academy of Sciences (Shanghai, CHINA) C20H26N2O4S2 Li, F. et al. Design, synthesis, and pharmacological evaluation of N-(4-mono and 4,5-disubstituted thiazol-2-yl)-2-aryl-3-(tetrahydro-2H-pyran-4-yl)propanamides as glucokinase activators. Bioorganic Med. Chem. (2010) 46194838 423
GKA16-9c GKA16-9c GKA: Systemic 2010 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 436.59 3.45 Chinese Academy of Sciences (Shanghai, CHINA) C21H28N2O4S2 Li, F. et al. Design, synthesis, and pharmacological evaluation of N-(4-mono and 4,5-disubstituted thiazol-2-yl)-2-aryl-3-(tetrahydro-2H-pyran-4-yl)propanamides as glucokinase activators. Bioorganic Med. Chem. (2010) 46907147 424
GKA16-9c__-R_ GKA16-9c (-R) GKA: Systemic 2010 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 436.59 3.45 Chinese Academy of Sciences (Shanghai, CHINA) C21H28N2O4S2 Li, F. et al. Design, synthesis, and pharmacological evaluation of N-(4-mono and 4,5-disubstituted thiazol-2-yl)-2-aryl-3-(tetrahydro-2H-pyran-4-yl)propanamides as glucokinase activators. Bioorganic Med. Chem. (2010) 46907147 425
GKA16-9d GKA16-9d GKA: Systemic 2010 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 450.61 3.91 Chinese Academy of Sciences (Shanghai, CHINA) C22H30N2O4S2 Li, F. et al. Design, synthesis, and pharmacological evaluation of N-(4-mono and 4,5-disubstituted thiazol-2-yl)-2-aryl-3-(tetrahydro-2H-pyran-4-yl)propanamides as glucokinase activators. Bioorganic Med. Chem. (2010) 46194839 426
GKA16-9e GKA16-9e GKA: Systemic 2010 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 450.61 3.99 Chinese Academy of Sciences (Shanghai, CHINA) C22H30N2O4S2 Li, F. et al. Design, synthesis, and pharmacological evaluation of N-(4-mono and 4,5-disubstituted thiazol-2-yl)-2-aryl-3-(tetrahydro-2H-pyran-4-yl)propanamides as glucokinase activators. Bioorganic Med. Chem. (2010) 46194694 427
GKA16-9f GKA16-9f GKA: Systemic 2010 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 434.57 2.86 Chinese Academy of Sciences (Shanghai, CHINA) C21H26N2O4S2 Li, F. et al. Design, synthesis, and pharmacological evaluation of N-(4-mono and 4,5-disubstituted thiazol-2-yl)-2-aryl-3-(tetrahydro-2H-pyran-4-yl)propanamides as glucokinase activators. Bioorganic Med. Chem. (2010) 46194695 428
GKA16-9g GKA16-9g GKA: Systemic 2010 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 470.6 3.95 Chinese Academy of Sciences (Shanghai, CHINA) C24H26N2O4S2 Li, F. et al. Design, synthesis, and pharmacological evaluation of N-(4-mono and 4,5-disubstituted thiazol-2-yl)-2-aryl-3-(tetrahydro-2H-pyran-4-yl)propanamides as glucokinase activators. Bioorganic Med. Chem. (2010) 46194840 429
GKA16-9h GKA16-9h GKA: Systemic 2010 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 500.63 3.92 Chinese Academy of Sciences (Shanghai, CHINA) C25H28N2O5S2 Li, F. et al. Design, synthesis, and pharmacological evaluation of N-(4-mono and 4,5-disubstituted thiazol-2-yl)-2-aryl-3-(tetrahydro-2H-pyran-4-yl)propanamides as glucokinase activators. Bioorganic Med. Chem. (2010) 46194836 430
GKA16-9i GKA16-9i GKA: Systemic 2010 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 488.59 4.05 Chinese Academy of Sciences (Shanghai, CHINA) C24H25FN2O4S2 Li, F. et al. Design, synthesis, and pharmacological evaluation of N-(4-mono and 4,5-disubstituted thiazol-2-yl)-2-aryl-3-(tetrahydro-2H-pyran-4-yl)propanamides as glucokinase activators. Bioorganic Med. Chem. (2010) 46194841 431
GKA16-9j GKA16-9j GKA: Systemic 2010 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 460.61 4.27 Chinese Academy of Sciences (Shanghai, CHINA) C23H28N2O4S2 Li, F. et al. Design, synthesis, and pharmacological evaluation of N-(4-mono and 4,5-disubstituted thiazol-2-yl)-2-aryl-3-(tetrahydro-2H-pyran-4-yl)propanamides as glucokinase activators. Bioorganic Med. Chem. (2010) 46844903 432
GKA16-9k GKA16-9k GKA: Systemic 2010 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 462.63 4 Chinese Academy of Sciences (Shanghai, CHINA) C23H30N2O4S2 Li, F. et al. Design, synthesis, and pharmacological evaluation of N-(4-mono and 4,5-disubstituted thiazol-2-yl)-2-aryl-3-(tetrahydro-2H-pyran-4-yl)propanamides as glucokinase activators. Bioorganic Med. Chem. (2010) 46195120 433
GKA16-9k__-R_ GKA16-9k (-R) GKA: Systemic 2010 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 462.63 4 Chinese Academy of Sciences (Shanghai, CHINA) C23H30N2O4S2 Li, F. et al. Design, synthesis, and pharmacological evaluation of N-(4-mono and 4,5-disubstituted thiazol-2-yl)-2-aryl-3-(tetrahydro-2H-pyran-4-yl)propanamides as glucokinase activators. Bioorganic Med. Chem. (2010) 46907148 434
GKA16-9l GKA16-9l GKA: Systemic 2010 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 422.56 3.09 Chinese Academy of Sciences (Shanghai, CHINA) C20H26N2O4S2 Li, F. et al. Design, synthesis, and pharmacological evaluation of N-(4-mono and 4,5-disubstituted thiazol-2-yl)-2-aryl-3-(tetrahydro-2H-pyran-4-yl)propanamides as glucokinase activators. Bioorganic Med. Chem. (2010) 46194692 435
GKA16-9m GKA16-9m GKA: Systemic 2010 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 450.61 3.85 Chinese Academy of Sciences (Shanghai, CHINA) C22H30N2O4S2 Li, F. et al. Design, synthesis, and pharmacological evaluation of N-(4-mono and 4,5-disubstituted thiazol-2-yl)-2-aryl-3-(tetrahydro-2H-pyran-4-yl)propanamides as glucokinase activators. Bioorganic Med. Chem. (2010) 46194693 436
GKA16-9n GKA16-9n GKA: Systemic 2010 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 541.52 5.03 Chinese Academy of Sciences (Shanghai, CHINA) C23H29BrN2O4S2 Li, F. et al. Design, synthesis, and pharmacological evaluation of N-(4-mono and 4,5-disubstituted thiazol-2-yl)-2-aryl-3-(tetrahydro-2H-pyran-4-yl)propanamides as glucokinase activators. Bioorganic Med. Chem. (2010) 46907180 437
GKA16-9o GKA16-9o GKA: Systemic 2010 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 588.52 4.69 Chinese Academy of Sciences (Shanghai, CHINA) C23H29IN2O4S2 Li, F. et al. Design, synthesis, and pharmacological evaluation of N-(4-mono and 4,5-disubstituted thiazol-2-yl)-2-aryl-3-(tetrahydro-2H-pyran-4-yl)propanamides as glucokinase activators. Bioorganic Med. Chem. (2010) 46907181 438
GKA16-9p GKA16-9p GKA: Systemic 2010 Thiazole/Thiadiazole,Benzo/Pyrido-thiazole,Sulfoxide/Sulfone derivatives 462.56 3.81 Chinese Academy of Sciences (Shanghai, CHINA) C22H23FN2O4S2 Li, F. et al. Design, synthesis, and pharmacological evaluation of N-(4-mono and 4,5-disubstituted thiazol-2-yl)-2-aryl-3-(tetrahydro-2H-pyran-4-yl)propanamides as glucokinase activators. Bioorganic Med. Chem. (2010) 46907182 439
GKA16-9q GKA16-9q GKA: Systemic 2010 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 474.64 3.92 Chinese Academy of Sciences (Shanghai, CHINA) C24H30N2O4S2 Li, F. et al. Design, synthesis, and pharmacological evaluation of N-(4-mono and 4,5-disubstituted thiazol-2-yl)-2-aryl-3-(tetrahydro-2H-pyran-4-yl)propanamides as glucokinase activators. Bioorganic Med. Chem. (2010) 46907262 440
GKA16-9q__-R_ GKA16-9q (-R) GKA: Systemic 2010 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 474.64 3.92 Chinese Academy of Sciences (Shanghai, CHINA) C24H30N2O4S2 Li, F. et al. Design, synthesis, and pharmacological evaluation of N-(4-mono and 4,5-disubstituted thiazol-2-yl)-2-aryl-3-(tetrahydro-2H-pyran-4-yl)propanamides as glucokinase activators. Bioorganic Med. Chem. (2010) 46907262 441
GKA16-9r GKA16-9r GKA: Systemic 2010 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 460.61 3.56 Chinese Academy of Sciences (Shanghai, CHINA) C23H28N2O4S2 Li, F. et al. Design, synthesis, and pharmacological evaluation of N-(4-mono and 4,5-disubstituted thiazol-2-yl)-2-aryl-3-(tetrahydro-2H-pyran-4-yl)propanamides as glucokinase activators. Bioorganic Med. Chem. (2010) 46907263 442
GKA16-9s GKA16-9s GKA: Systemic 2010 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 489.65 2.78 Chinese Academy of Sciences (Shanghai, CHINA) C24H31N3O4S2 Li, F. et al. Design, synthesis, and pharmacological evaluation of N-(4-mono and 4,5-disubstituted thiazol-2-yl)-2-aryl-3-(tetrahydro-2H-pyran-4-yl)propanamides as glucokinase activators. Bioorganic Med. Chem. (2010) 46907264 443
GKA16-9t GKA16-9t GKA: Systemic 2010 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 436.54 2.3 Chinese Academy of Sciences (Shanghai, CHINA) C20H24N2O5S2 Li, F. et al. Design, synthesis, and pharmacological evaluation of N-(4-mono and 4,5-disubstituted thiazol-2-yl)-2-aryl-3-(tetrahydro-2H-pyran-4-yl)propanamides as glucokinase activators. Bioorganic Med. Chem. (2010) 136016445 444
GKA16-9u GKA16-9u GKA: Systemic 2010 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 524.65 4.43 Chinese Academy of Sciences (Shanghai, CHINA) C27H28N2O5S2 Li, F. et al. Design, synthesis, and pharmacological evaluation of N-(4-mono and 4,5-disubstituted thiazol-2-yl)-2-aryl-3-(tetrahydro-2H-pyran-4-yl)propanamides as glucokinase activators. Bioorganic Med. Chem. (2010) 75250223 445
GKA16-9v GKA16-9v GKA: Systemic 2010 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 490.64 3.93 Chinese Academy of Sciences (Shanghai, CHINA) C24H30N2O5S2 Li, F. et al. Design, synthesis, and pharmacological evaluation of N-(4-mono and 4,5-disubstituted thiazol-2-yl)-2-aryl-3-(tetrahydro-2H-pyran-4-yl)propanamides as glucokinase activators. Bioorganic Med. Chem. (2010) 75250224 446
GKA1-7 GKA1-7 GKA: Systemic 2005 Thiazole/Thiadiazole,Urea 337.39 4.06 OSI Pharmaceuticals (USA); Prosidion Limited (UK) C16H17F2N3OS Castelhano, A. L. et al. Glucokinase-activating ureas. Bioorganic Med. Chem. Lett. (2005) 44389895 20
GKA17-10 GKA17-10 GKA: Systemic 2010 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 376.49 3.79 Hoffmann-La Roche Inc. (USA) C18H20N2O3S2 Sidduri, A. et al. 2,3-Disubstituted acrylamides as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2010) 46946861 449
GKA17-11 GKA17-11 GKA: Systemic 2010 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 390.52 4.33 Hoffmann-La Roche Inc. (USA) C19H22N2O3S2 Sidduri, A. et al. 2,3-Disubstituted acrylamides as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2010) 10293790 450
GKA17-12 GKA17-12 GKA: Systemic 2010 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 404.55 4.87 Hoffmann-La Roche Inc. (USA) C20H24N2O3S2 Sidduri, A. et al. 2,3-Disubstituted acrylamides as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2010) 10111868 451
GKA17-13 GKA17-13 GKA: Systemic 2010 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 418.57 5.41 Hoffmann-La Roche Inc. (USA) C21H26N2O3S2 Sidduri, A. et al. 2,3-Disubstituted acrylamides as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2010) 10159013 452
GKA17-14 GKA17-14 GKA: Systemic 2010 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 390.52 4.25 Hoffmann-La Roche Inc. (USA) C19H22N2O3S2 Sidduri, A. et al. 2,3-Disubstituted acrylamides as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2010) 10271714 453
GKA17-15 GKA17-15 GKA: Systemic 2010 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 376.49 3.79 Hoffmann-La Roche Inc. (USA) C18H20N2O3S2 Sidduri, A. et al. 2,3-Disubstituted acrylamides as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2010) 18316957 454
GKA17-16 GKA17-16 GKA: Systemic 2010 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 390.52 4.41 Hoffmann-La Roche Inc. (USA) C19H22N2O3S2 Sidduri, A. et al. 2,3-Disubstituted acrylamides as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2010) 52947581 455
GKA17-17 GKA17-17 GKA: Systemic 2010 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 410.94 4.75 Hoffmann-La Roche Inc. (USA) C18H19ClN2O3S2 Sidduri, A. et al. 2,3-Disubstituted acrylamides as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2010) 52941297 456
GKA17-18 GKA17-18 GKA: Systemic 2010 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 455.39 4.81 Hoffmann-La Roche Inc. (USA) C18H19BrN2O3S2 Sidduri, A. et al. 2,3-Disubstituted acrylamides as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2010) 10115151 457
GKA17-19 GKA17-19 GKA: Systemic 2010 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 390.52 4.19 Hoffmann-La Roche Inc. (USA) C19H22N2O3S2 Sidduri, A. et al. 2,3-Disubstituted acrylamides as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2010) 52944939 458
GKA17-20 GKA17-20 GKA: Systemic 2010 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 401.5 3.84 Hoffmann-La Roche Inc. (USA) C19H19N3O3S2 Sidduri, A. et al. 2,3-Disubstituted acrylamides as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2010) 52949438 459
GKA17-21 GKA17-21 GKA: Systemic 2010 Pyridine,Sulfoxide/Sulfone derivatives 404.91 4.31 Hoffmann-La Roche Inc. (USA) C20H21ClN2O3S Sidduri, A. et al. 2,3-Disubstituted acrylamides as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2010) 10111883 460
GKA17-22 GKA17-22 GKA: Systemic 2010 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 410.94 4.42 Hoffmann-La Roche Inc. (USA) C18H19ClN2O3S2 Sidduri, A. et al. 2,3-Disubstituted acrylamides as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2010) 10136295 461
GKA17-23 GKA17-23 GKA: Systemic 2010 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 455.39 4.48 Hoffmann-La Roche Inc. (USA) C18H19BrN2O3S2 Sidduri, A. et al. 2,3-Disubstituted acrylamides as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2010) 10115152 462
GKA17-24 GKA17-24 GKA: Systemic 2010 Thiazole/Thiadiazole 367.29 5.81 Hoffmann-La Roche Inc. (USA) C17H16Cl2N2OS Sidduri, A. et al. 2,3-Disubstituted acrylamides as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2010) 10270299 463
GKA17-25 GKA17-25 GKA: Systemic 2010 Thiazole/Thiadiazole 398.46 4.35 Hoffmann-La Roche Inc. (USA) C19H19FN6OS Sidduri, A. et al. 2,3-Disubstituted acrylamides as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2010) 10200886 464
GKA17-26 GKA17-26 GKA: Systemic 2010 Urea 372.4 3.59 Hoffmann-La Roche Inc. (USA) C18H21FN6O2 Sidduri, A. et al. 2,3-Disubstituted acrylamides as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2010) 10133857 465
GKA17-27 GKA17-27 GKA: Systemic 2010 Thiazole/Thiadiazole 414.91 4.88 Hoffmann-La Roche Inc. (USA) C19H19ClN6OS Sidduri, A. et al. 2,3-Disubstituted acrylamides as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2010) 10273261 466
GKA17-28 GKA17-28 GKA: Systemic 2010 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 458.52 5.14 Hoffmann-La Roche Inc. (USA) C20H21F3N2O3S2 Sidduri, A. et al. 2,3-Disubstituted acrylamides as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2010) 52946400 467
GKA17-29 GKA17-29 GKA: Systemic 2010 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 458.52 5.21 Hoffmann-La Roche Inc. (USA) C20H21F3N2O3S2 Sidduri, A. et al. 2,3-Disubstituted acrylamides as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2010) 10298126 468
GKA17-30 GKA17-30 GKA: Systemic 2010 Pyridine,Sulfoxide/Sulfone derivatives 531.39 5.8 Hoffmann-La Roche Inc. (USA) C22H22BrF3N2O3S Sidduri, A. et al. 2,3-Disubstituted acrylamides as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2010) 10230239 469
GKA17-31 GKA17-31 GKA: Systemic 2010 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 537.41 6.24 Hoffmann-La Roche Inc. (USA) C20H20BrF3N2O3S2 Sidduri, A. et al. 2,3-Disubstituted acrylamides as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2010) 10208969 470
GKA17-32 GKA17-32 GKA: Systemic 2010 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 435.52 4.16 Hoffmann-La Roche Inc. (USA) C19H21N3O5S2 Sidduri, A. et al. 2,3-Disubstituted acrylamides as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2010) 10160132 471
GKA17-33 GKA17-33 GKA: Systemic 2010 Thiazole/Thiadiazole 428.94 5.42 Hoffmann-La Roche Inc. (USA) C20H21ClN6OS Sidduri, A. et al. 2,3-Disubstituted acrylamides as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2010) 85326095 472
GKA17-34 GKA17-34 GKA: Systemic 2010 Thiazole/Thiadiazole 482.91 5.94 Hoffmann-La Roche Inc. (USA) C20H18ClF3N6OS Sidduri, A. et al. 2,3-Disubstituted acrylamides as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2010) 10206213 473
GKA17-35 GKA17-35 GKA: Systemic 2010 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 483.44 5.9 Hoffmann-La Roche Inc. (USA) C20H23BrN2O3S2 Sidduri, A. et al. 2,3-Disubstituted acrylamides as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2010) 10299638 474
GKA17-36 GKA17-36 GKA: Systemic 2010 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 551.44 6.78 Hoffmann-La Roche Inc. (USA) C21H22BrF3N2O3S2 Sidduri, A. et al. 2,3-Disubstituted acrylamides as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2010) 10209466 475
GKA17-37 GKA17-37 GKA: Systemic 2010 Thiazole/Thiadiazole 521.86 6.99 Hoffmann-La Roche Inc. (USA) C21H22BrClN6OS Sidduri, A. et al. 2,3-Disubstituted acrylamides as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2010) 10142817 476
GKA17-8 GKA17-8 GKA: Systemic 2010 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 336.43 2.59 Hoffmann-La Roche Inc. (USA) C15H16N2O3S2 Sidduri, A. et al. 2,3-Disubstituted acrylamides as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2010) 9884201 447
GKA17-9 GKA17-9 GKA: Systemic 2010 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 350.46 2.92 Hoffmann-La Roche Inc. (USA) C16H18N2O3S2 Sidduri, A. et al. 2,3-Disubstituted acrylamides as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2010) 52943981 448
GKA1-8 GKA1-8 GKA: Systemic 2005 Thiazole/Thiadiazole,Urea 371.83 5.02 OSI Pharmaceuticals (USA); Prosidion Limited (UK) C16H16ClF2N3OS Castelhano, A. L. et al. Glucokinase-activating ureas. Bioorganic Med. Chem. Lett. (2005) 44389902 21
GKA18-10 GKA18-10 GKA: Systemic 2011 Thiazole/Thiadiazole 278.37 3.65 4SC AG (Planneg-Martinsried, GERMANY) C14H18N2O2S Lang, M. et al. Discovery and hit-to-lead optimization of novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2011) 56665236 481
GKA18-11 GKA18-11 GKA: Systemic 2011 Thiazole/Thiadiazole 262.33 2.71 4SC AG (Planneg-Martinsried, GERMANY) C13H14N2O2S Lang, M. et al. Discovery and hit-to-lead optimization of novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2011) 33039817 482
GKA18-12 GKA18-12 GKA: Systemic 2011 Thiazole/Thiadiazole 288.36 2.78 4SC AG (Planneg-Martinsried, GERMANY) C15H16N2O2S Lang, M. et al. Discovery and hit-to-lead optimization of novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2011) 56678883 483
GKA18-13 GKA18-13 GKA: Systemic 2011 Thiazole/Thiadiazole 292.42 3.68 4SC AG (Planneg-Martinsried, GERMANY) C14H16N2OS2 Lang, M. et al. Discovery and hit-to-lead optimization of novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2011) 37911481 484
GKA18-14 GKA18-14 GKA: Systemic 2011 Thiazole/Thiadiazole 278.39 3.33 4SC AG (Planneg-Martinsried, GERMANY) C13H14N2OS2 Lang, M. et al. Discovery and hit-to-lead optimization of novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2011) 33040188 485
GKA18-15 GKA18-15 GKA: Systemic 2011 Thiazole/Thiadiazole 278.33 1.46 4SC AG (Planneg-Martinsried, GERMANY) C13H14N2O3S Lang, M. et al. Discovery and hit-to-lead optimization of novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2011) 56668691 486
GKA18-16 GKA18-16 GKA: Systemic 2011 Thiazole/Thiadiazole 292.35 2 4SC AG (Planneg-Martinsried, GERMANY) C14H16N2O3S Lang, M. et al. Discovery and hit-to-lead optimization of novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2011) 56675547 487
GKA18-17 GKA18-17 GKA: Systemic 2011 Thiazole/Thiadiazole 320.41 2.82 4SC AG (Planneg-Martinsried, GERMANY) C16H20N2O3S Lang, M. et al. Discovery and hit-to-lead optimization of novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2011) 56661791 488
GKA18-18 GKA18-18 GKA: Systemic 2011 Thiazole/Thiadiazole 318.39 2.26 4SC AG (Planneg-Martinsried, GERMANY) C16H18N2O3S Lang, M. et al. Discovery and hit-to-lead optimization of novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2011) 56668692 489
GKA18-19 GKA18-19 GKA: Systemic 2011 Thiazole/Thiadiazole 334.39 2.43 4SC AG (Planneg-Martinsried, GERMANY) C16H18N2O4S Lang, M. et al. Discovery and hit-to-lead optimization of novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2011) 56665237 490
GKA18-20 GKA18-20 GKA: Systemic 2011 Thiazole/Thiadiazole 333.41 1.85 4SC AG (Planneg-Martinsried, GERMANY) C16H19N3O3S Lang, M. et al. Discovery and hit-to-lead optimization of novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2011) 56672162 491
GKA18-21 GKA18-21 GKA: Systemic 2011 Thiazole/Thiadiazole 347.43 2.04 4SC AG (Planneg-Martinsried, GERMANY) C17H21N3O3S Lang, M. et al. Discovery and hit-to-lead optimization of novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2011) 56672163 492
GKA18-22 GKA18-22 GKA: Systemic 2011 Thiazole/Thiadiazole 319.38 1.46 4SC AG (Planneg-Martinsried, GERMANY) C15H17N3O3S Lang, M. et al. Discovery and hit-to-lead optimization of novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2011) 56678884 493
GKA18-23 GKA18-23 GKA: Systemic 2011 Thiazole/Thiadiazole 320.36 2.03 4SC AG (Planneg-Martinsried, GERMANY) C15H16N2O4S Lang, M. et al. Discovery and hit-to-lead optimization of novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2011) 56665238 494
GKA18-24 GKA18-24 GKA: Systemic 2011 Thiazole/Thiadiazole 366.43 3.66 4SC AG (Planneg-Martinsried, GERMANY) C20H18N2O3S Lang, M. et al. Discovery and hit-to-lead optimization of novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2011) 56658289 495
GKA18-25 GKA18-25 GKA: Systemic 2011 Thiazole/Thiadiazole 366.43 3.66 4SC AG (Planneg-Martinsried, GERMANY) C20H18N2O3S Lang, M. et al. Discovery and hit-to-lead optimization of novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2011) 56675548 496
GKA18-26 GKA18-26 GKA: Systemic 2011 Thiazole/Thiadiazole 338.42 4.33 4SC AG (Planneg-Martinsried, GERMANY) C19H18N2O2S Lang, M. et al. Discovery and hit-to-lead optimization of novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2011) 56661792 497
GKA18-27 GKA18-27 GKA: Systemic 2011 Thiazole/Thiadiazole 382.5 4.27 4SC AG (Planneg-Martinsried, GERMANY) C20H18N2O2S2 Lang, M. et al. Discovery and hit-to-lead optimization of novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2011) 56668693 498
GKA18-28 GKA18-28 GKA: Systemic 2011 Thiazole/Thiadiazole 368.47 3.87 4SC AG (Planneg-Martinsried, GERMANY) C19H16N2O2S2 Lang, M. et al. Discovery and hit-to-lead optimization of novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2011) 56658290 499
GKA18-29 GKA18-29 GKA: Systemic 2011 Thiazole/Thiadiazole 396.53 4.7 4SC AG (Planneg-Martinsried, GERMANY) C21H20N2O2S2 Lang, M. et al. Discovery and hit-to-lead optimization of novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2011) 56682200 500
GKA18-30 GKA18-30 GKA: Systemic 2011 Thiazole/Thiadiazole 396.53 4.63 4SC AG (Planneg-Martinsried, GERMANY) C21H20N2O2S2 Lang, M. et al. Discovery and hit-to-lead optimization of novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2011) 56661903 501
GKA18-31 GKA18-31 GKA: Systemic 2011 Thiazole/Thiadiazole 382.5 4.23 4SC AG (Planneg-Martinsried, GERMANY) C20H18N2O2S2 Lang, M. et al. Discovery and hit-to-lead optimization of novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2011) 56661793 502
GKA18-32 GKA18-32 GKA: Systemic 2011 Thiazole/Thiadiazole 410.55 5.06 4SC AG (Planneg-Martinsried, GERMANY) C22H22N2O2S2 Lang, M. et al. Discovery and hit-to-lead optimization of novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2011) 56675549 503
GKA18-33 GKA18-33 GKA: Systemic 2011 Thiazole/Thiadiazole 352.41 3.26 4SC AG (Planneg-Martinsried, GERMANY) C19H16N2O3S Lang, M. et al. Discovery and hit-to-lead optimization of novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2011) 56672164 504
GKA18-34 GKA18-34 GKA: Systemic 2011 Thiazole/Thiadiazole 380.46 4.09 4SC AG (Planneg-Martinsried, GERMANY) C21H20N2O3S Lang, M. et al. Discovery and hit-to-lead optimization of novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2011) 56658291 505
GKA18-35 GKA18-35 GKA: Systemic 2011 Thiazole/Thiadiazole 394.49 4.45 4SC AG (Planneg-Martinsried, GERMANY) C22H22N2O3S Lang, M. et al. Discovery and hit-to-lead optimization of novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2011) 56675550 506
GKA18-36 GKA18-36 GKA: Systemic 2011 Thiazole/Thiadiazole 382.43 3.72 4SC AG (Planneg-Martinsried, GERMANY) C20H18N2O4S Lang, M. et al. Discovery and hit-to-lead optimization of novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2011) 56672165 507
GKA18-37 GKA18-37 GKA: Systemic 2011 Thiazole/Thiadiazole 382.43 3.72 4SC AG (Planneg-Martinsried, GERMANY) C20H18N2O4S Lang, M. et al. Discovery and hit-to-lead optimization of novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2011) 56672166 508
GKA18-38 GKA18-38 GKA: Systemic 2011 Thiazole/Thiadiazole 382.43 3.82 4SC AG (Planneg-Martinsried, GERMANY) C20H18N2O4S Lang, M. et al. Discovery and hit-to-lead optimization of novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2011) 56665239 509
GKA18-39 GKA18-39 GKA: Systemic 2011 Thiazole/Thiadiazole 368.41 3.5 4SC AG (Planneg-Martinsried, GERMANY) C19H16N2O4S Lang, M. et al. Discovery and hit-to-lead optimization of novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2011) 56658292 510
GKA18-40 GKA18-40 GKA: Systemic 2011 Thiazole/Thiadiazole 349.41 3.69 4SC AG (Planneg-Martinsried, GERMANY) C19H15N3O2S Lang, M. et al. Discovery and hit-to-lead optimization of novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2011) 56672167 511
GKA18-41 GKA18-41 GKA: Systemic 2011 Thiazole/Thiadiazole 349.41 3.69 4SC AG (Planneg-Martinsried, GERMANY) C19H15N3O2S Lang, M. et al. Discovery and hit-to-lead optimization of novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2011) 56665240 512
GKA18-42 GKA18-42 GKA: Systemic 2011 Thiazole/Thiadiazole 369.39 3.8 4SC AG (Planneg-Martinsried, GERMANY) C18H15N3O4S Lang, M. et al. Discovery and hit-to-lead optimization of novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2011) 56661907 513
GKA18-43 GKA18-43 GKA: Systemic 2011 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 418.55 3.83 4SC AG (Planneg-Martinsried, GERMANY) C19H18N2O3S3 Lang, M. et al. Discovery and hit-to-lead optimization of novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2011) 56675683 514
GKA18-44 GKA18-44 GKA: Systemic 2011 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 432.58 4.26 4SC AG (Planneg-Martinsried, GERMANY) C20H20N2O3S3 Lang, M. et al. Discovery and hit-to-lead optimization of novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2011) 56672288 515
GKA18-45 GKA18-45 GKA: Systemic 2011 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 446.61 4.61 4SC AG (Planneg-Martinsried, GERMANY) C21H22N2O3S3 Lang, M. et al. Discovery and hit-to-lead optimization of novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2011) 56661908 516
GKA18-46 GKA18-46 GKA: Systemic 2011 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 402.49 3.21 4SC AG (Planneg-Martinsried, GERMANY) C19H18N2O4S2 Lang, M. et al. Discovery and hit-to-lead optimization of novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2011) 56668806 517
GKA18-47 GKA18-47 GKA: Systemic 2011 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 416.51 3.64 4SC AG (Planneg-Martinsried, GERMANY) C20H20N2O4S2 Lang, M. et al. Discovery and hit-to-lead optimization of novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2011) 56675684 518
GKA18-48 GKA18-48 GKA: Systemic 2011 Thiazole/Thiadiazole,Benzamide 383.49 3.46 4SC AG (Planneg-Martinsried, GERMANY) C19H17N3O2S2 Lang, M. et al. Discovery and hit-to-lead optimization of novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2011) 53387836 519
GKA18-49 GKA18-49 GKA: Systemic 2011 Thiazole/Thiadiazole,Benzamide 397.51 3.9 4SC AG (Planneg-Martinsried, GERMANY) C20H19N3O2S2 Lang, M. et al. Discovery and hit-to-lead optimization of novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2011) 53387835 520
GKA18-50 GKA18-50 GKA: Systemic 2011 Thiazole/Thiadiazole,Benzamide 367.42 2.85 4SC AG (Planneg-Martinsried, GERMANY) C19H17N3O3S Lang, M. et al. Discovery and hit-to-lead optimization of novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2011) 56665243 521
GKA18-51 GKA18-51 GKA: Systemic 2011 Thiazole/Thiadiazole,Benzamide 381.45 3.28 4SC AG (Planneg-Martinsried, GERMANY) C20H19N3O3S Lang, M. et al. Discovery and hit-to-lead optimization of novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2011) 56682206 522
GKA18-52 GKA18-52 GKA: Systemic 2011 Thiazole/Thiadiazole,Benzamide 395.47 3.43 4SC AG (Planneg-Martinsried, GERMANY) C21H21N3O3S Lang, M. et al. Discovery and hit-to-lead optimization of novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2011) 56661800 523
GKA18-6 GKA18-6 GKA: Systemic 2011 Thiazole/Thiadiazole,Benzamide 286.39 4.32 4SC AG (Planneg-Martinsried, GERMANY) C16H18N2OS Lang, M. et al. Discovery and hit-to-lead optimization of novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2011) 2471840 477
GKA18-7 GKA18-7 GKA: Systemic 2011 Benzamide,Benzo/Pyrido-thiazole 269.32 2.87 4SC AG (Planneg-Martinsried, GERMANY) C14H11N3OS Lang, M. et al. Discovery and hit-to-lead optimization of novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2011) 23132485 478
GKA18-8 GKA18-8 GKA: Systemic 2011 Thiazole/Thiadiazole 278.39 3.28 4SC AG (Planneg-Martinsried, GERMANY) C13H14N2OS2 Lang, M. et al. Discovery and hit-to-lead optimization of novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2011) 1245924 479
GKA18-9 GKA18-9 GKA: Systemic 2011 Thiazole/Thiadiazole 276.35 3.07 4SC AG (Planneg-Martinsried, GERMANY) C14H16N2O2S Lang, M. et al. Discovery and hit-to-lead optimization of novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2011) 4880864 480
GKA1-9 GKA1-9 GKA: Systemic 2005 Urea 331.36 3.96 OSI Pharmaceuticals (USA); Prosidion Limited (UK) C18H19F2N3O Castelhano, A. L. et al. Glucokinase-activating ureas. Bioorganic Med. Chem. Lett. (2005) 86041973 22
GKA19-12a GKA19-12a GKA: Systemic 2011 Benzamide,Pyridine 446.45 5.15 Chinese Academy of Medical Sciences (Beijing, CHINA) C26H20F2N2O3 Li, Y. Q. et al. Design, synthesis and biological evaluation of novel glucokinase activators. Chinese Chem. Lett. (2011) 141216494 528
GKA19-12b GKA19-12b GKA: Systemic 2011 Benzamide,Pyridine 428.45 5.05 Chinese Academy of Medical Sciences (Beijing, CHINA) C26H21FN2O3 Li, Y. Q. et al. Design, synthesis and biological evaluation of novel glucokinase activators. Chinese Chem. Lett. (2011) 141216496 529
GKA19-12c GKA19-12c GKA: Systemic 2011 Benzamide,Pyridine 462.9 5.68 Chinese Academy of Medical Sciences (Beijing, CHINA) C26H20ClFN2O3 Li, Y. Q. et al. Design, synthesis and biological evaluation of novel glucokinase activators. Chinese Chem. Lett. (2011) 141216506 530
GKA19-12d GKA19-12d GKA: Systemic 2011 Benzamide,Pyridine 410.44 3.78 Chinese Academy of Medical Sciences (Beijing, CHINA) C23H23FN2O4 Li, Y. Q. et al. Design, synthesis and biological evaluation of novel glucokinase activators. Chinese Chem. Lett. (2011) 141216459 531
GKA19-12e GKA19-12e GKA: Systemic 2011 Benzamide 414.43 3.69 Chinese Academy of Medical Sciences (Beijing, CHINA) C22H23FN2O5 Li, Y. Q. et al. Design, synthesis and biological evaluation of novel glucokinase activators. Chinese Chem. Lett. (2011) 141216474 532
GKA19-12f GKA19-12f GKA: Systemic 2011 Benzamide 432.44 4.97 Chinese Academy of Medical Sciences (Beijing, CHINA) C25H21FN2O4 Li, Y. Q. et al. Design, synthesis and biological evaluation of novel glucokinase activators. Chinese Chem. Lett. (2011) 141216442 533
GKA19-12g GKA19-12g GKA: Systemic 2011 Benzamide 466.89 5.6 Chinese Academy of Medical Sciences (Beijing, CHINA) C25H20ClFN2O4 Li, Y. Q. et al. Design, synthesis and biological evaluation of novel glucokinase activators. Chinese Chem. Lett. (2011) 141216445 534
GKA19-12h GKA19-12h GKA: Systemic 2011 Thiazole/Thiadiazole,Benzamide 468.93 5.78 Chinese Academy of Medical Sciences (Beijing, CHINA) C24H18ClFN2O3S Li, Y. Q. et al. Design, synthesis and biological evaluation of novel glucokinase activators. Chinese Chem. Lett. (2011) 141216522 535
GKA19-12i GKA19-12i GKA: Systemic 2011 Thiazole/Thiadiazole,Benzamide 434.48 5.15 Chinese Academy of Medical Sciences (Beijing, CHINA) C24H19FN2O3S Li, Y. Q. et al. Design, synthesis and biological evaluation of novel glucokinase activators. Chinese Chem. Lett. (2011) 141216443 536
GKA19-12j GKA19-12j GKA: Systemic 2011 Thiazole/Thiadiazole,Benzamide 386.44 4.46 Chinese Academy of Medical Sciences (Beijing, CHINA) C20H19FN2O3S Li, Y. Q. et al. Design, synthesis and biological evaluation of novel glucokinase activators. Chinese Chem. Lett. (2011) 141216475 537
GKA19-9a GKA19-9a GKA: Systemic 2011 Benzamide 342.32 3.7 Chinese Academy of Medical Sciences (Beijing, CHINA) C18H15FN2O4 Li, Y. Q. et al. Design, synthesis and biological evaluation of novel glucokinase activators. Chinese Chem. Lett. (2011) 141216513 524
GKA19-9b GKA19-9b GKA: Systemic 2011 Thiazole/Thiadiazole,Benzamide 358.39 4.28 Chinese Academy of Medical Sciences (Beijing, CHINA) C18H15FN2O3S Li, Y. Q. et al. Design, synthesis and biological evaluation of novel glucokinase activators. Chinese Chem. Lett. (2011) 141216458 525
GKA19-9c GKA19-9c GKA: Systemic 2011 Benzamide,Pyridine 352.36 4.15 Chinese Academy of Medical Sciences (Beijing, CHINA) C20H17FN2O3 Li, Y. Q. et al. Design, synthesis and biological evaluation of novel glucokinase activators. Chinese Chem. Lett. (2011) 141216516 526
GKA19-9d GKA19-9d GKA: Systemic 2011 Benzamide,Pyridine 338.33 3.78 Chinese Academy of Medical Sciences (Beijing, CHINA) C19H15FN2O3 Li, Y. Q. et al. Design, synthesis and biological evaluation of novel glucokinase activators. Chinese Chem. Lett. (2011) 141216514 527
GKA20-18 GKA20-18 GKA: Systemic 2011 Benzamide,Pyrazine 432.43 1.67 Pfizer Global Research & Development (USA) C22H20N6O4 Pfefferkorn, J. A. et al. Designing glucokinase activators with reduced hypoglycemia risk: Discovery of N,N-dimethyl-5-(2-methyl-6-((5-methylpyrazin-2-yl)-carbamoyl)benzofuran-4- yloxy)pyrimidine-2-carboxamide as a clinical candidate for the treatment of type 2 diabetes mellitus. Medchemcomm (2011) 46916741 538
GKA20-27 GKA20-27 GKA: Systemic 2011 Benzamide,Pyridine,Pyrazine 431.44 2.41 Pfizer Global Research & Development (USA) C23H21N5O4 Pfefferkorn, J. A. et al. Designing glucokinase activators with reduced hypoglycemia risk: Discovery of N,N-dimethyl-5-(2-methyl-6-((5-methylpyrazin-2-yl)-carbamoyl)benzofuran-4- yloxy)pyrimidine-2-carboxamide as a clinical candidate for the treatment of type 2 diabetes mellitus. Medchemcomm (2011) 90665740 539
GKA20-28 GKA20-28 GKA: Systemic 2011 Benzamide,Pyrimidine,Pyrazine 432.43 1.76 Pfizer Global Research & Development (USA) C22H20N6O4 Pfefferkorn, J. A. et al. Designing glucokinase activators with reduced hypoglycemia risk: Discovery of N,N-dimethyl-5-(2-methyl-6-((5-methylpyrazin-2-yl)-carbamoyl)benzofuran-4- yloxy)pyrimidine-2-carboxamide as a clinical candidate for the treatment of type 2 diabetes mellitus. Medchemcomm (2011) 46916694 540
GKA20-29 GKA20-29 GKA: Systemic 2011 Benzamide,Pyrazine 373.4 4.05 Pfizer Global Research & Development (USA) C22H19N3O3 Pfefferkorn, J. A. et al. Designing glucokinase activators with reduced hypoglycemia risk: Discovery of N,N-dimethyl-5-(2-methyl-6-((5-methylpyrazin-2-yl)-carbamoyl)benzofuran-4- yloxy)pyrimidine-2-carboxamide as a clinical candidate for the treatment of type 2 diabetes mellitus. Medchemcomm (2011) 90665736 541
GKA20-30 GKA20-30 GKA: Systemic 2011 Benzamide,Pyrazine,Sulfoxide/Sulfone derivatives 437.47 2.92 Pfizer Global Research & Development (USA) C22H19N3O5S Pfefferkorn, J. A. et al. Designing glucokinase activators with reduced hypoglycemia risk: Discovery of N,N-dimethyl-5-(2-methyl-6-((5-methylpyrazin-2-yl)-carbamoyl)benzofuran-4- yloxy)pyrimidine-2-carboxamide as a clinical candidate for the treatment of type 2 diabetes mellitus. Medchemcomm (2011) 90665737 542
GKA20-31 GKA20-31 GKA: Systemic 2011 Benzamide,Pyrazine 384.39 3.4 Pfizer Global Research & Development (USA) C22H16N4O3 Pfefferkorn, J. A. et al. Designing glucokinase activators with reduced hypoglycemia risk: Discovery of N,N-dimethyl-5-(2-methyl-6-((5-methylpyrazin-2-yl)-carbamoyl)benzofuran-4- yloxy)pyrimidine-2-carboxamide as a clinical candidate for the treatment of type 2 diabetes mellitus. Medchemcomm (2011) 90665738 543
GKA20-32 GKA20-32 GKA: Systemic 2011 Benzamide,Pyrazine 430.46 3.14 Pfizer Global Research & Development (USA) C24H22N4O4 Pfefferkorn, J. A. et al. Designing glucokinase activators with reduced hypoglycemia risk: Discovery of N,N-dimethyl-5-(2-methyl-6-((5-methylpyrazin-2-yl)-carbamoyl)benzofuran-4- yloxy)pyrimidine-2-carboxamide as a clinical candidate for the treatment of type 2 diabetes mellitus. Medchemcomm (2011) 90665739 544
GKA20-33 GKA20-33 GKA: Systemic 2011 Benzamide,Pyrimidine,Pyrazine 432.43 1.76 Pfizer Global Research & Development (USA) C22H20N6O4 Pfefferkorn, J. A. et al. Designing glucokinase activators with reduced hypoglycemia risk: Discovery of N,N-dimethyl-5-(2-methyl-6-((5-methylpyrazin-2-yl)-carbamoyl)benzofuran-4- yloxy)pyrimidine-2-carboxamide as a clinical candidate for the treatment of type 2 diabetes mellitus. Medchemcomm (2011) 90665741 545
GKA20-34 GKA20-34 GKA: Systemic 2011 Benzamide,Pyrazine 446.46 2.04 Pfizer Global Research & Development (USA) C23H22N6O4 Pfefferkorn, J. A. et al. Designing glucokinase activators with reduced hypoglycemia risk: Discovery of N,N-dimethyl-5-(2-methyl-6-((5-methylpyrazin-2-yl)-carbamoyl)benzofuran-4- yloxy)pyrimidine-2-carboxamide as a clinical candidate for the treatment of type 2 diabetes mellitus. Medchemcomm (2011) 59483313 546
GKA20-35 GKA20-35 GKA: Systemic 2011 Benzamide,Pyrazine 418.41 1.49 Pfizer Global Research & Development (USA) C21H18N6O4 Pfefferkorn, J. A. et al. Designing glucokinase activators with reduced hypoglycemia risk: Discovery of N,N-dimethyl-5-(2-methyl-6-((5-methylpyrazin-2-yl)-carbamoyl)benzofuran-4- yloxy)pyrimidine-2-carboxamide as a clinical candidate for the treatment of type 2 diabetes mellitus. Medchemcomm (2011) 90665742 547
GKA20-36 GKA20-36 GKA: Systemic 2011 Benzamide,Pyrazine 444.44 1.8 Pfizer Global Research & Development (USA) C23H20N6O4 Pfefferkorn, J. A. et al. Designing glucokinase activators with reduced hypoglycemia risk: Discovery of N,N-dimethyl-5-(2-methyl-6-((5-methylpyrazin-2-yl)-carbamoyl)benzofuran-4- yloxy)pyrimidine-2-carboxamide as a clinical candidate for the treatment of type 2 diabetes mellitus. Medchemcomm (2011) 90665743 548
GKA20-37 GKA20-37 GKA: Systemic 2011 Benzamide,Pyrazine 458.47 2.16 Pfizer Global Research & Development (USA) C24H22N6O4 Pfefferkorn, J. A. et al. Designing glucokinase activators with reduced hypoglycemia risk: Discovery of N,N-dimethyl-5-(2-methyl-6-((5-methylpyrazin-2-yl)-carbamoyl)benzofuran-4- yloxy)pyrimidine-2-carboxamide as a clinical candidate for the treatment of type 2 diabetes mellitus. Medchemcomm (2011) 90665744 549
GKA20-38 GKA20-38 GKA: Systemic 2011 Benzamide,Pyrazine 472.5 2.52 Pfizer Global Research & Development (USA) C25H24N6O4 Pfefferkorn, J. A. et al. Designing glucokinase activators with reduced hypoglycemia risk: Discovery of N,N-dimethyl-5-(2-methyl-6-((5-methylpyrazin-2-yl)-carbamoyl)benzofuran-4- yloxy)pyrimidine-2-carboxamide as a clinical candidate for the treatment of type 2 diabetes mellitus. Medchemcomm (2011) 90665745 550
GKA20-39 GKA20-39 GKA: Systemic 2011 Benzamide,Pyrazine 444.44 1.84 Pfizer Global Research & Development (USA) C23H20N6O4 Pfefferkorn, J. A. et al. Designing glucokinase activators with reduced hypoglycemia risk: Discovery of N,N-dimethyl-5-(2-methyl-6-((5-methylpyrazin-2-yl)-carbamoyl)benzofuran-4- yloxy)pyrimidine-2-carboxamide as a clinical candidate for the treatment of type 2 diabetes mellitus. Medchemcomm (2011) 90665746 551
GKA20-40 GKA20-40 GKA: Systemic 2011 Benzamide,Pyrazine 458.47 2.23 Pfizer Global Research & Development (USA) C24H22N6O4 Pfefferkorn, J. A. et al. Designing glucokinase activators with reduced hypoglycemia risk: Discovery of N,N-dimethyl-5-(2-methyl-6-((5-methylpyrazin-2-yl)-carbamoyl)benzofuran-4- yloxy)pyrimidine-2-carboxamide as a clinical candidate for the treatment of type 2 diabetes mellitus. Medchemcomm (2011) 90665747 552
GKA20-41 GKA20-41 GKA: Systemic 2011 Benzamide,Pyrazine 460.44 0.96 Pfizer Global Research & Development (USA) C23H20N6O5 Pfefferkorn, J. A. et al. Designing glucokinase activators with reduced hypoglycemia risk: Discovery of N,N-dimethyl-5-(2-methyl-6-((5-methylpyrazin-2-yl)-carbamoyl)benzofuran-4- yloxy)pyrimidine-2-carboxamide as a clinical candidate for the treatment of type 2 diabetes mellitus. Medchemcomm (2011) 90665748 553
GKA20-42 GKA20-42 GKA: Systemic 2011 Benzamide,Pyrazine 460.44 0.61 Pfizer Global Research & Development (USA) C23H20N6O5 Pfefferkorn, J. A. et al. Designing glucokinase activators with reduced hypoglycemia risk: Discovery of N,N-dimethyl-5-(2-methyl-6-((5-methylpyrazin-2-yl)-carbamoyl)benzofuran-4- yloxy)pyrimidine-2-carboxamide as a clinical candidate for the treatment of type 2 diabetes mellitus. Medchemcomm (2011) 90665749 554
GKA20-43 GKA20-43 GKA: Systemic 2011 Benzamide,Pyrazine 472.45 0.79 Pfizer Global Research & Development (USA) C24H20N6O5 Pfefferkorn, J. A. et al. Designing glucokinase activators with reduced hypoglycemia risk: Discovery of N,N-dimethyl-5-(2-methyl-6-((5-methylpyrazin-2-yl)-carbamoyl)benzofuran-4- yloxy)pyrimidine-2-carboxamide as a clinical candidate for the treatment of type 2 diabetes mellitus. Medchemcomm (2011) 90665750 555
GKA20-44 GKA20-44 GKA: Systemic 2011 Benzamide,Pyridine,Pyrazine 431.44 2.7 Pfizer Global Research & Development (USA) C23H21N5O4 Pfefferkorn, J. A. et al. Designing glucokinase activators with reduced hypoglycemia risk: Discovery of N,N-dimethyl-5-(2-methyl-6-((5-methylpyrazin-2-yl)-carbamoyl)benzofuran-4- yloxy)pyrimidine-2-carboxamide as a clinical candidate for the treatment of type 2 diabetes mellitus. Medchemcomm (2011) 90665751 556
GKA20-45 GKA20-45 GKA: Systemic 2011 Benzamide,Pyrazine 418.41 1.27 Pfizer Global Research & Development (USA) C21H18N6O4 Pfefferkorn, J. A. et al. Designing glucokinase activators with reduced hypoglycemia risk: Discovery of N,N-dimethyl-5-(2-methyl-6-((5-methylpyrazin-2-yl)-carbamoyl)benzofuran-4- yloxy)pyrimidine-2-carboxamide as a clinical candidate for the treatment of type 2 diabetes mellitus. Medchemcomm (2011) 90665752 557
GKA20-46 GKA20-46 GKA: Systemic 2011 Benzamide,Pyrazine 448.43 1.58 Pfizer Global Research & Development (USA) C22H20N6O5 Pfefferkorn, J. A. et al. Designing glucokinase activators with reduced hypoglycemia risk: Discovery of N,N-dimethyl-5-(2-methyl-6-((5-methylpyrazin-2-yl)-carbamoyl)benzofuran-4- yloxy)pyrimidine-2-carboxamide as a clinical candidate for the treatment of type 2 diabetes mellitus. Medchemcomm (2011) 90665753 558
GKA20-47 GKA20-47 GKA: Systemic 2011 Benzamide,Pyrazine 486.4 2.19 Pfizer Global Research & Development (USA) C22H17F3N6O4 Pfefferkorn, J. A. et al. Designing glucokinase activators with reduced hypoglycemia risk: Discovery of N,N-dimethyl-5-(2-methyl-6-((5-methylpyrazin-2-yl)-carbamoyl)benzofuran-4- yloxy)pyrimidine-2-carboxamide as a clinical candidate for the treatment of type 2 diabetes mellitus. Medchemcomm (2011) 90665754 559
GKA20-48 GKA20-48 GKA: Systemic 2011 Benzamide,Pyrazine 446.46 2.1 Pfizer Global Research & Development (USA) C23H22N6O4 Pfefferkorn, J. A. et al. Designing glucokinase activators with reduced hypoglycemia risk: Discovery of N,N-dimethyl-5-(2-methyl-6-((5-methylpyrazin-2-yl)-carbamoyl)benzofuran-4- yloxy)pyrimidine-2-carboxamide as a clinical candidate for the treatment of type 2 diabetes mellitus. Medchemcomm (2011) 90665755 560
GKA20-49 GKA20-49 GKA: Systemic 2011 Benzamide,Pyrazine 420.42 1.72 Pfizer Global Research & Development (USA) C21H20N6O4 Pfefferkorn, J. A. et al. Designing glucokinase activators with reduced hypoglycemia risk: Discovery of N,N-dimethyl-5-(2-methyl-6-((5-methylpyrazin-2-yl)-carbamoyl)benzofuran-4- yloxy)pyrimidine-2-carboxamide as a clinical candidate for the treatment of type 2 diabetes mellitus. Medchemcomm (2011) 90665756 561
GKA20-50 GKA20-50 GKA: Systemic 2011 Benzamide,Pyrimidine,Pyrazine 418.41 1.69 Pfizer Global Research & Development (USA) C21H18N6O4 Pfefferkorn, J. A. et al. Designing glucokinase activators with reduced hypoglycemia risk: Discovery of N,N-dimethyl-5-(2-methyl-6-((5-methylpyrazin-2-yl)-carbamoyl)benzofuran-4- yloxy)pyrimidine-2-carboxamide as a clinical candidate for the treatment of type 2 diabetes mellitus. Medchemcomm (2011) 90665757 562
GKA21-_GKA60_ GKA21-(GKA60) GKA: Systemic 2011 Benzamide,Pyridine,Sulfoxide/Sulfone derivatives 458.41 3.53 AstraZeneca (UK) C23H20F2N2O6 Pike, K. G. et al. Design of a potent, soluble glucokinase activator with increased pharmacokinetic half-life. Bioorganic Med. Chem. Lett. (2011) 11751490 584
GKA2-10 GKA2-10 GKA: Systemic 2005 Benzamide,Pyridine 348.35 3.01 AstraZeneca (UK) C20H16N2O4 McKerrecher, D. et al. Discovery, synthesis and biological evaluation of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2005) 44400984 54
GKA21-1 GKA21-1 GKA: Systemic 2011 Benzamide,Pyridine 482.5 4.26 AstraZeneca (UK) C26H27FN2O6 Pike, K. G. et al. Design of a potent, soluble glucokinase activator with increased pharmacokinetic half-life. Bioorganic Med. Chem. Lett. (2011) 11363673 563
GKA2-11 GKA2-11 GKA: Systemic 2005 Benzamide,Pyridine 382.8 3.64 AstraZeneca (UK) C20H15ClN2O4 McKerrecher, D. et al. Discovery, synthesis and biological evaluation of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2005) 44401001 55
GKA21-10 GKA21-10 GKA: Systemic 2011 Benzamide,Pyridine 486.46 3.91 AstraZeneca (UK) C25H24F2N2O6 Pike, K. G. et al. Design of a potent, soluble glucokinase activator with increased pharmacokinetic half-life. Bioorganic Med. Chem. Lett. (2011) 11752100 572
GKA21-11 GKA21-11 GKA: Systemic 2011 Benzamide,Pyridine 432.47 4.35 AstraZeneca (UK) C25H24N2O5 Pike, K. G. et al. Design of a potent, soluble glucokinase activator with increased pharmacokinetic half-life. Bioorganic Med. Chem. Lett. (2011) 54584650 573
GKA21-12 GKA21-12 GKA: Systemic 2011 Benzamide,Pyridine 420.46 4.18 AstraZeneca (UK) C24H24N2O5 Pike, K. G. et al. Design of a potent, soluble glucokinase activator with increased pharmacokinetic half-life. Bioorganic Med. Chem. Lett. (2011) 44410834 574
GKA21-13 GKA21-13 GKA: Systemic 2011 Benzamide,Pyridine 392.4 3.85 AstraZeneca (UK) C22H20N2O5 Pike, K. G. et al. Design of a potent, soluble glucokinase activator with increased pharmacokinetic half-life. Bioorganic Med. Chem. Lett. (2011) 11188508 575
GKA21-14 GKA21-14 GKA: Systemic 2011 Benzamide,Pyridine 422.43 3.33 AstraZeneca (UK) C23H22N2O6 Pike, K. G. et al. Design of a potent, soluble glucokinase activator with increased pharmacokinetic half-life. Bioorganic Med. Chem. Lett. (2011) 11235541 576
GKA21-15 GKA21-15 GKA: Systemic 2011 Benzamide,Pyridine 452.46 3.3 AstraZeneca (UK) C24H24N2O7 Pike, K. G. et al. Design of a potent, soluble glucokinase activator with increased pharmacokinetic half-life. Bioorganic Med. Chem. Lett. (2011) 54584651 577
GKA21-16 GKA21-16 GKA: Systemic 2011 Benzamide,Pyridine 452.46 3.3 AstraZeneca (UK) C24H24N2O7 Pike, K. G. et al. Design of a potent, soluble glucokinase activator with increased pharmacokinetic half-life. Bioorganic Med. Chem. Lett. (2011) 11476499 578
GKA21-17 GKA21-17 GKA: Systemic 2011 Benzamide,Pyridine 456.88 3.96 AstraZeneca (UK) C23H21ClN2O6 Pike, K. G. et al. Design of a potent, soluble glucokinase activator with increased pharmacokinetic half-life. Bioorganic Med. Chem. Lett. (2011) 54585589 579
GKA21-18 GKA21-18 GKA: Systemic 2011 Benzamide,Pyridine 456.88 3.96 AstraZeneca (UK) C23H21ClN2O6 Pike, K. G. et al. Design of a potent, soluble glucokinase activator with increased pharmacokinetic half-life. Bioorganic Med. Chem. Lett. (2011) 54587596 580
GKA21-19 GKA21-19 GKA: Systemic 2011 Benzamide,Pyridine 440.42 3.43 AstraZeneca (UK) C23H21FN2O6 Pike, K. G. et al. Design of a potent, soluble glucokinase activator with increased pharmacokinetic half-life. Bioorganic Med. Chem. Lett. (2011) 11270610 581
GKA21-2 GKA21-2 GKA: Systemic 2011 Benzamide,Pyridine 494.54 4.13 AstraZeneca (UK) C27H30N2O7 Pike, K. G. et al. Design of a potent, soluble glucokinase activator with increased pharmacokinetic half-life. Bioorganic Med. Chem. Lett. (2011) 11409307 564
GKA2-12 GKA2-12 GKA: Systemic 2005 Benzamide,Pyridine 523.36 5.73 AstraZeneca (UK) C27H20Cl2N2O5 McKerrecher, D. et al. Discovery, synthesis and biological evaluation of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2005) 44401406 56
GKA21-20 GKA21-20 GKA: Systemic 2011 Benzamide,Pyridine 465.5 3.46 AstraZeneca (UK) C25H27N3O6 Pike, K. G. et al. Design of a potent, soluble glucokinase activator with increased pharmacokinetic half-life. Bioorganic Med. Chem. Lett. (2011) 54585590 582
GKA21-21 GKA21-21 GKA: Systemic 2011 Benzamide,Pyridine 500.52 2.57 AstraZeneca (UK) C24H24N2O8S Pike, K. G. et al. Design of a potent, soluble glucokinase activator with increased pharmacokinetic half-life. Bioorganic Med. Chem. Lett. (2011) 54581717 583
GKA21-3 GKA21-3 GKA: Systemic 2011 Benzamide,Pyridine 500.49 4.36 AstraZeneca (UK) C26H26F2N2O6 Pike, K. G. et al. Design of a potent, soluble glucokinase activator with increased pharmacokinetic half-life. Bioorganic Med. Chem. Lett. (2011) 72976770 565
GKA2-13 GKA2-13 GKA: Systemic 2005 Benzamide,Pyridine 372.41 3.62 AstraZeneca (UK) C20H24N2O5 McKerrecher, D. et al. Discovery, synthesis and biological evaluation of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2005) 10044792 57
GKA21-4 GKA21-4 GKA: Systemic 2011 Benzamide,Pyridine 488.92 4.23 AstraZeneca (UK) C24H25ClN2O7 Pike, K. G. et al. Design of a potent, soluble glucokinase activator with increased pharmacokinetic half-life. Bioorganic Med. Chem. Lett. (2011) 11340776 566
GKA2-14 GKA2-14 GKA: Systemic 2005 Benzamide,Pyridine 454.47 4.48 AstraZeneca (UK) C27H22N2O5 McKerrecher, D. et al. Discovery, synthesis and biological evaluation of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2005) 10161315 58
GKA21-5 GKA21-5 GKA: Systemic 2011 Benzamide,Pyridine 456.53 4.76 AstraZeneca (UK) C25H32N2O6 Pike, K. G. et al. Design of a potent, soluble glucokinase activator with increased pharmacokinetic half-life. Bioorganic Med. Chem. Lett. (2011) 54583686 567
GKA2-15 GKA2-15 GKA: Systemic 2005 Benzamide,Pyridine 490.45 4.68 AstraZeneca (UK) C27H20F2N2O5 McKerrecher, D. et al. Discovery, synthesis and biological evaluation of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2005) 44401302 59
GKA21-6 GKA21-6 GKA: Systemic 2011 Benzamide,Pyridine 434.48 4.68 AstraZeneca (UK) C25H26N2O5 Pike, K. G. et al. Design of a potent, soluble glucokinase activator with increased pharmacokinetic half-life. Bioorganic Med. Chem. Lett. (2011) 44410908 568
GKA2-16 GKA2-16 GKA: Systemic 2005 Benzamide,Pyridine 428.48 3.24 AstraZeneca (UK) C23H28N2O6 McKerrecher, D. et al. Discovery, synthesis and biological evaluation of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2005) 44402618 60
GKA21-7 GKA21-7 GKA: Systemic 2011 Benzamide,Pyridine 478.54 4.35 AstraZeneca (UK) C27H30N2O6 Pike, K. G. et al. Design of a potent, soluble glucokinase activator with increased pharmacokinetic half-life. Bioorganic Med. Chem. Lett. (2011) 54587595 569
GKA2-17 GKA2-17 GKA: Systemic 2005 Benzamide,Pyridine 398.45 4.12 AstraZeneca (UK) C22H26N2O5 McKerrecher, D. et al. Discovery, synthesis and biological evaluation of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2005) 44400943 61
GKA21-8 GKA21-8 GKA: Systemic 2011 Benzamide,Pyridine 476.52 4.28 AstraZeneca (UK) C27H28N2O6 Pike, K. G. et al. Design of a potent, soluble glucokinase activator with increased pharmacokinetic half-life. Bioorganic Med. Chem. Lett. (2011) 54580718 570
GKA2-18 GKA2-18 GKA: Systemic 2005 Benzamide,Pyridine 412.48 4.84 AstraZeneca (UK) C23H28N2O5 McKerrecher, D. et al. Discovery, synthesis and biological evaluation of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2005) 44401535 62
GKA21-9 GKA21-9 GKA: Systemic 2011 Benzamide,Pyridine 464.51 4.06 AstraZeneca (UK) C26H28N2O6 Pike, K. G. et al. Design of a potent, soluble glucokinase activator with increased pharmacokinetic half-life. Bioorganic Med. Chem. Lett. (2011) 11294219 571
GKA2-19 GKA2-19 GKA: Systemic 2005 Benzamide,Pyridine 421.45 3.17 AstraZeneca (UK) C23H23N3O5 McKerrecher, D. et al. Discovery, synthesis and biological evaluation of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2005) 44401138 63
GKA2-20 GKA2-20 GKA: Systemic 2005 Benzamide,Pyridine 421.45 3.17 AstraZeneca (UK) C23H23N3O5 McKerrecher, D. et al. Discovery, synthesis and biological evaluation of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2005) 44401503 64
GKA2-21 GKA2-21 GKA: Systemic 2005 Benzamide,Pyridine 420.46 4.24 AstraZeneca (UK) C24H24N2O5 McKerrecher, D. et al. Discovery, synthesis and biological evaluation of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2005) 44401270 65
GKA2-23 GKA2-23 GKA: Systemic 2005 Benzamide,Pyridine 406.43 3.78 AstraZeneca (UK) C23H22N2O5 McKerrecher, D. et al. Discovery, synthesis and biological evaluation of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2005) 44401426 66
GKA2-24 GKA2-24 GKA: Systemic 2005 Benzamide,Pyridine 434.48 4.6 AstraZeneca (UK) C25H26N2O5 McKerrecher, D. et al. Discovery, synthesis and biological evaluation of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2005) 44401059 67
GKA2-25 GKA2-25 GKA: Systemic 2005 Benzamide,Pyridine 424.42 3.88 AstraZeneca (UK) C23H21FN2O5 McKerrecher, D. et al. Discovery, synthesis and biological evaluation of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2005) 44401073 68
GKA22-9a GKA22-9a GKA: Systemic 2011 Thiazole/Thiadiazole,Pyrimidine 399.47 4.38 Chinese Academy of Medical Sciences (Beijing, CHINA) C19H21N5O3S Song, H. et al. Novel N-(pyrimidin-4-yl)thiazol-2-amine derivatives as dual-action hypoglycemic agents that activate GK and PPARγ. Acta Pharm. Sin. B (2011) 71542608 585
GKA22-9b GKA22-9b GKA: Systemic 2011 Thiazole/Thiadiazole,Pyrimidine 371.41 3.68 Chinese Academy of Medical Sciences (Beijing, CHINA) C17H17N5O3S Song, H. et al. Novel N-(pyrimidin-4-yl)thiazol-2-amine derivatives as dual-action hypoglycemic agents that activate GK and PPARγ. Acta Pharm. Sin. B (2011) 71542609 586
GKA22-9c GKA22-9c GKA: Systemic 2011 Thiazole/Thiadiazole,Pyrimidine 399.47 4.38 Chinese Academy of Medical Sciences (Beijing, CHINA) C19H21N5O3S Song, H. et al. Novel N-(pyrimidin-4-yl)thiazol-2-amine derivatives as dual-action hypoglycemic agents that activate GK and PPARγ. Acta Pharm. Sin. B (2011) 71542689 587
GKA22-9d GKA22-9d GKA: Systemic 2011 Thiazole/Thiadiazole,Pyrimidine 371.41 3.68 Chinese Academy of Medical Sciences (Beijing, CHINA) C17H17N5O3S Song, H. et al. Novel N-(pyrimidin-4-yl)thiazol-2-amine derivatives as dual-action hypoglycemic agents that activate GK and PPARγ. Acta Pharm. Sin. B (2011) 71542690 588
GKA22-9e GKA22-9e GKA: Systemic 2011 Thiazole/Thiadiazole,Pyrimidine 385.44 3.87 Chinese Academy of Medical Sciences (Beijing, CHINA) C18H19N5O3S Song, H. et al. Novel N-(pyrimidin-4-yl)thiazol-2-amine derivatives as dual-action hypoglycemic agents that activate GK and PPARγ. Acta Pharm. Sin. B (2011) 71542611 589
GKA22-9f GKA22-9f GKA: Systemic 2011 Thiazole/Thiadiazole,Pyrimidine 485.56 5.12 Chinese Academy of Medical Sciences (Beijing, CHINA) C23H27N5O5S Song, H. et al. Novel N-(pyrimidin-4-yl)thiazol-2-amine derivatives as dual-action hypoglycemic agents that activate GK and PPARγ. Acta Pharm. Sin. B (2011) 71542613 590
GKA22-9g GKA22-9g GKA: Systemic 2011 Thiazole/Thiadiazole,Pyrimidine 435.5 3.04 Chinese Academy of Medical Sciences (Beijing, CHINA) C19H25N5O5S Song, H. et al. Novel N-(pyrimidin-4-yl)thiazol-2-amine derivatives as dual-action hypoglycemic agents that activate GK and PPARγ. Acta Pharm. Sin. B (2011) 71542775 591
GKA22-9h GKA22-9h GKA: Systemic 2011 Thiazole/Thiadiazole,Pyrimidine 392.48 1.98 Chinese Academy of Medical Sciences (Beijing, CHINA) C17H24N6O3S Song, H. et al. Novel N-(pyrimidin-4-yl)thiazol-2-amine derivatives as dual-action hypoglycemic agents that activate GK and PPARγ. Acta Pharm. Sin. B (2011) 49821971 592
GKA22-9i GKA22-9i GKA: Systemic 2011 Thiazole/Thiadiazole,Pyrimidine 391.49 3.27 Chinese Academy of Medical Sciences (Beijing, CHINA) C18H25N5O3S Song, H. et al. Novel N-(pyrimidin-4-yl)thiazol-2-amine derivatives as dual-action hypoglycemic agents that activate GK and PPARγ. Acta Pharm. Sin. B (2011) 71542694 593
GKA22-9j GKA22-9j GKA: Systemic 2011 Thiazole/Thiadiazole,Pyrimidine 334.44 1.83 Chinese Academy of Medical Sciences (Beijing, CHINA) C15H22N6OS Song, H. et al. Novel N-(pyrimidin-4-yl)thiazol-2-amine derivatives as dual-action hypoglycemic agents that activate GK and PPARγ. Acta Pharm. Sin. B (2011) 71542693 594
GKA2-3 GKA2-3 GKA: Systemic 2005 Pyridine 377.46 4.66 AstraZeneca (UK) C22H19NO3S McKerrecher, D. et al. Discovery, synthesis and biological evaluation of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2005) 9934507 47
GKA23-10 GKA23-10 GKA: Systemic 2012 Thiazole/Thiadiazole 474.99 4.23 AstraZeneca (UK) C20H19ClN6O2S2 Bonn, P. et al. The discovery of a novel series of glucokinase activators based on a pyrazolopyrimidine scaffold. Bioorganic Med. Chem. Lett. (2012) 57504293 602
GKA23-11 GKA23-11 GKA: Systemic 2012 Thiazole/Thiadiazole 519.04 4.08 AstraZeneca (UK) C22H23ClN6O3S2 Bonn, P. et al. The discovery of a novel series of glucokinase activators based on a pyrazolopyrimidine scaffold. Bioorganic Med. Chem. Lett. (2012) 57504292 603
GKA23-12 GKA23-12 GKA: Systemic 2012 Thiazole/Thiadiazole 493 5.68 AstraZeneca (UK) C23H17ClN6OS2 Bonn, P. et al. The discovery of a novel series of glucokinase activators based on a pyrazolopyrimidine scaffold. Bioorganic Med. Chem. Lett. (2012) 71450638 604
GKA23-13 GKA23-13 GKA: Systemic 2012 Thiazole/Thiadiazole 400.84 3.44 AstraZeneca (UK) C17H13ClN6O2S Bonn, P. et al. The discovery of a novel series of glucokinase activators based on a pyrazolopyrimidine scaffold. Bioorganic Med. Chem. Lett. (2012) 71463148 605
GKA23-14 GKA23-14 GKA: Systemic 2012 Thiazole/Thiadiazole 456.95 5.27 AstraZeneca (UK) C21H21ClN6O2S Bonn, P. et al. The discovery of a novel series of glucokinase activators based on a pyrazolopyrimidine scaffold. Bioorganic Med. Chem. Lett. (2012) 59279533 606
GKA23-15__-R_ GKA23-15 (-R) GKA: Systemic 2012 Pyridine 452.89 3.55 AstraZeneca (UK) C22H21ClN6O3 Bonn, P. et al. The discovery of a novel series of glucokinase activators based on a pyrazolopyrimidine scaffold. Bioorganic Med. Chem. Lett. (2012) 57504265 608
GKA23-15__racemic_ GKA23-15 (racemic) GKA: Systemic 2012 Pyridine 452.89 3.55 AstraZeneca (UK) C22H21ClN6O3 Bonn, P. et al. The discovery of a novel series of glucokinase activators based on a pyrazolopyrimidine scaffold. Bioorganic Med. Chem. Lett. (2012) 57504265 607
GKA23-15__-S_ GKA23-15 (-S) GKA: Systemic 2012 Pyridine 452.89 3.55 AstraZeneca (UK) C22H21ClN6O3 Bonn, P. et al. The discovery of a novel series of glucokinase activators based on a pyrazolopyrimidine scaffold. Bioorganic Med. Chem. Lett. (2012) 57504266 609
GKA23-16 GKA23-16 GKA: Systemic 2012 Pyridine 432.48 3.29 AstraZeneca (UK) C23H24N6O3 Bonn, P. et al. The discovery of a novel series of glucokinase activators based on a pyrazolopyrimidine scaffold. Bioorganic Med. Chem. Lett. (2012) 57504263 610
GKA23-17__-R_ GKA23-17 (-R) GKA: Systemic 2012 Pyridine 486.45 3.81 AstraZeneca (UK) C23H21F3N6O3 Bonn, P. et al. The discovery of a novel series of glucokinase activators based on a pyrazolopyrimidine scaffold. Bioorganic Med. Chem. Lett. (2012) 57504272 612
GKA23-17__racemic_ GKA23-17 (racemic) GKA: Systemic 2012 Pyridine 486.45 3.81 AstraZeneca (UK) C23H21F3N6O3 Bonn, P. et al. The discovery of a novel series of glucokinase activators based on a pyrazolopyrimidine scaffold. Bioorganic Med. Chem. Lett. (2012) 57504272 611
GKA23-17__-S_ GKA23-17 (-S) GKA: Systemic 2012 Pyridine 486.45 3.81 AstraZeneca (UK) C23H21F3N6O3 Bonn, P. et al. The discovery of a novel series of glucokinase activators based on a pyrazolopyrimidine scaffold. Bioorganic Med. Chem. Lett. (2012) 57504474 613
GKA23-18__-R_ GKA23-18 (-R) GKA: Systemic 2012 Pyridine 448.47 2.89 AstraZeneca (UK) C23H24N6O4 Bonn, P. et al. The discovery of a novel series of glucokinase activators based on a pyrazolopyrimidine scaffold. Bioorganic Med. Chem. Lett. (2012) 57504267 615
GKA23-18__racemic_ GKA23-18 (racemic) GKA: Systemic 2012 Pyridine 448.47 2.89 AstraZeneca (UK) C23H24N6O4 Bonn, P. et al. The discovery of a novel series of glucokinase activators based on a pyrazolopyrimidine scaffold. Bioorganic Med. Chem. Lett. (2012) 57504267 614
GKA23-18__-S_ GKA23-18 (-S) GKA: Systemic 2012 Pyridine 448.47 2.89 AstraZeneca (UK) C23H24N6O4 Bonn, P. et al. The discovery of a novel series of glucokinase activators based on a pyrazolopyrimidine scaffold. Bioorganic Med. Chem. Lett. (2012) 57504268 616
GKA23-3 GKA23-3 GKA: Systemic 2012 Thiazole/Thiadiazole 416.91 3.98 AstraZeneca (UK) C17H13ClN6OS2 Bonn, P. et al. The discovery of a novel series of glucokinase activators based on a pyrazolopyrimidine scaffold. Bioorganic Med. Chem. Lett. (2012) 647685 595
GKA23-4 GKA23-4 GKA: Systemic 2012 382.46 3.36 AstraZeneca (UK) C17H14N6OS2 Bonn, P. et al. The discovery of a novel series of glucokinase activators based on a pyrazolopyrimidine scaffold. Bioorganic Med. Chem. Lett. (2012) 1172823 596
GKA23-5 GKA23-5 GKA: Systemic 2012 395.87 4.22 AstraZeneca (UK) C19H14ClN5OS Bonn, P. et al. The discovery of a novel series of glucokinase activators based on a pyrazolopyrimidine scaffold. Bioorganic Med. Chem. Lett. (2012) 1445399 597
GKA23-6 GKA23-6 GKA: Systemic 2012 Pyridine 410.88 3.85 AstraZeneca (UK) C19H15ClN6OS Bonn, P. et al. The discovery of a novel series of glucokinase activators based on a pyrazolopyrimidine scaffold. Bioorganic Med. Chem. Lett. (2012) 71455985 598
GKA23-7 GKA23-7 GKA: Systemic 2012 Pyrimidine 397.84 2.83 AstraZeneca (UK) C17H12ClN7OS Bonn, P. et al. The discovery of a novel series of glucokinase activators based on a pyrazolopyrimidine scaffold. Bioorganic Med. Chem. Lett. (2012) 71454226 599
GKA23-8 GKA23-8 GKA: Systemic 2012 399.86 2.86 AstraZeneca (UK) C17H14ClN7OS Bonn, P. et al. The discovery of a novel series of glucokinase activators based on a pyrazolopyrimidine scaffold. Bioorganic Med. Chem. Lett. (2012) 71454227 600
GKA23-9 GKA23-9 GKA: Systemic 2012 Thiazole/Thiadiazole 473.01 5.81 AstraZeneca (UK) C21H21ClN6OS2 Bonn, P. et al. The discovery of a novel series of glucokinase activators based on a pyrazolopyrimidine scaffold. Bioorganic Med. Chem. Lett. (2012) 57504305 601
GKA2-4 GKA2-4 GKA: Systemic 2005 Pyridine 439.5 5.56 AstraZeneca (UK) C28H25NO4 McKerrecher, D. et al. Discovery, synthesis and biological evaluation of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2005) 44400835 48
GKA24-10 GKA24-10 GKA: Systemic 2012 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 502.58 5.35 Chinese Academy of Sciences (Shanghai, CHINA) C24H23FN2O5S2 Mao, W. et al. Design, synthesis, and pharmacological evaluation of benzamide derivatives as glucokinase activators. Bioorganic Med. Chem. (2012) 70685578 618
GKA24-13a GKA24-13a GKA: Systemic 2012 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 529.63 3.9 Chinese Academy of Sciences (Shanghai, CHINA) C25H27N3O6S2 Mao, W. et al. Design, synthesis, and pharmacological evaluation of benzamide derivatives as glucokinase activators. Bioorganic Med. Chem. (2012) 70683468 619
GKA24-13b GKA24-13b GKA: Systemic 2012 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 547.62 4.33 Chinese Academy of Sciences (Shanghai, CHINA) C25H26FN3O6S2 Mao, W. et al. Design, synthesis, and pharmacological evaluation of benzamide derivatives as glucokinase activators. Bioorganic Med. Chem. (2012) 70687724 620
GKA24-14a GKA24-14a GKA: Systemic 2012 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 557.68 4.76 Chinese Academy of Sciences (Shanghai, CHINA) C27H31N3O6S2 Mao, W. et al. Design, synthesis, and pharmacological evaluation of benzamide derivatives as glucokinase activators. Bioorganic Med. Chem. (2012) 70681373 621
GKA24-14b GKA24-14b GKA: Systemic 2012 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 575.67 5.2 Chinese Academy of Sciences (Shanghai, CHINA) C27H30FN3O6S2 Mao, W. et al. Design, synthesis, and pharmacological evaluation of benzamide derivatives as glucokinase activators. Bioorganic Med. Chem. (2012) 70685590 622
GKA24-15a GKA24-15a GKA: Systemic 2012 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 555.67 4.52 Chinese Academy of Sciences (Shanghai, CHINA) C27H29N3O6S2 Mao, W. et al. Design, synthesis, and pharmacological evaluation of benzamide derivatives as glucokinase activators. Bioorganic Med. Chem. (2012) 70696106 623
GKA24-15b GKA24-15b GKA: Systemic 2012 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 573.66 4.95 Chinese Academy of Sciences (Shanghai, CHINA) C27H28FN3O6S2 Mao, W. et al. Design, synthesis, and pharmacological evaluation of benzamide derivatives as glucokinase activators. Bioorganic Med. Chem. (2012) 70681393 624
GKA24-16a GKA24-16a GKA: Systemic 2012 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 531.62 4.81 Chinese Academy of Sciences (Shanghai, CHINA) C25H26FN3O5S2 Mao, W. et al. Design, synthesis, and pharmacological evaluation of benzamide derivatives as glucokinase activators. Bioorganic Med. Chem. (2012) 70685591 625
GKA24-16b GKA24-16b GKA: Systemic 2012 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 549.61 5.25 Chinese Academy of Sciences (Shanghai, CHINA) C25H25F2N3O5S2 Mao, W. et al. Design, synthesis, and pharmacological evaluation of benzamide derivatives as glucokinase activators. Bioorganic Med. Chem. (2012) 60150713 626
GKA24-17a GKA24-17a GKA: Systemic 2012 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 557.68 4.68 Chinese Academy of Sciences (Shanghai, CHINA) C27H31N3O6S2 Mao, W. et al. Design, synthesis, and pharmacological evaluation of benzamide derivatives as glucokinase activators. Bioorganic Med. Chem. (2012) 70689789 627
GKA24-17b GKA24-17b GKA: Systemic 2012 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 575.67 5.11 Chinese Academy of Sciences (Shanghai, CHINA) C27H30FN3O6S2 Mao, W. et al. Design, synthesis, and pharmacological evaluation of benzamide derivatives as glucokinase activators. Bioorganic Med. Chem. (2012) 70696107 628
GKA24-18 GKA24-18 GKA: Systemic 2012 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 578.67 6.68 Chinese Academy of Sciences (Shanghai, CHINA) C30H27FN2O5S2 Mao, W. et al. Design, synthesis, and pharmacological evaluation of benzamide derivatives as glucokinase activators. Bioorganic Med. Chem. (2012) 70687742 629
GKA24-19 GKA24-19 GKA: Systemic 2012 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 540.69 6.62 Chinese Academy of Sciences (Shanghai, CHINA) C28H32N2O5S2 Mao, W. et al. Design, synthesis, and pharmacological evaluation of benzamide derivatives as glucokinase activators. Bioorganic Med. Chem. (2012) 70691929 630
GKA24-20 GKA24-20 GKA: Systemic 2012 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 500.59 4.38 Chinese Academy of Sciences (Shanghai, CHINA) C24H24N2O6S2 Mao, W. et al. Design, synthesis, and pharmacological evaluation of benzamide derivatives as glucokinase activators. Bioorganic Med. Chem. (2012) 136264103 631
GKA24-21 GKA24-21 GKA: Systemic 2012 Benzamide,Sulfoxide/Sulfone derivatives 495.59 4.59 Chinese Academy of Sciences (Shanghai, CHINA) C26H29N3O5S Mao, W. et al. Design, synthesis, and pharmacological evaluation of benzamide derivatives as glucokinase activators. Bioorganic Med. Chem. (2012) 70681394 632
GKA24-22 GKA24-22 GKA: Systemic 2012 Benzamide,Pyrazine,Sulfoxide/Sulfone derivatives 493.57 4.14 Chinese Academy of Sciences (Shanghai, CHINA) C26H27N3O5S Mao, W. et al. Design, synthesis, and pharmacological evaluation of benzamide derivatives as glucokinase activators. Bioorganic Med. Chem. (2012) 70683488 633
GKA24-23 GKA24-23 GKA: Systemic 2012 Benzamide,Sulfoxide/Sulfone derivatives 518.58 4.65 Chinese Academy of Sciences (Shanghai, CHINA) C27H26N4O5S Mao, W. et al. Design, synthesis, and pharmacological evaluation of benzamide derivatives as glucokinase activators. Bioorganic Med. Chem. (2012) 70683489 634
GKA24-24a GKA24-24a GKA: Systemic 2012 Benzamide,Sulfoxide/Sulfone derivatives 540.63 3.58 Chinese Academy of Sciences (Shanghai, CHINA) C27H32N4O6S Mao, W. et al. Design, synthesis, and pharmacological evaluation of benzamide derivatives as glucokinase activators. Bioorganic Med. Chem. (2012) 70693981 635
GKA24-24b GKA24-24b GKA: Systemic 2012 Benzamide,Sulfoxide/Sulfone derivatives 526.6 3.18 Chinese Academy of Sciences (Shanghai, CHINA) C26H30N4O6S Mao, W. et al. Design, synthesis, and pharmacological evaluation of benzamide derivatives as glucokinase activators. Bioorganic Med. Chem. (2012) 70689790 636
GKA24-25a GKA24-25a GKA: Systemic 2012 Benzamide,Sulfoxide/Sulfone derivatives 568.68 4.44 Chinese Academy of Sciences (Shanghai, CHINA) C29H36N4O6S Mao, W. et al. Design, synthesis, and pharmacological evaluation of benzamide derivatives as glucokinase activators. Bioorganic Med. Chem. (2012) 70694001 637
GKA24-25b GKA24-25b GKA: Systemic 2012 Benzamide,Sulfoxide/Sulfone derivatives 554.66 4.04 Chinese Academy of Sciences (Shanghai, CHINA) C28H34N4O6S Mao, W. et al. Design, synthesis, and pharmacological evaluation of benzamide derivatives as glucokinase activators. Bioorganic Med. Chem. (2012) 70691949 638
GKA24-26a GKA24-26a GKA: Systemic 2012 Benzamide,Sulfoxide/Sulfone derivatives 566.67 4.2 Chinese Academy of Sciences (Shanghai, CHINA) C29H34N4O6S Mao, W. et al. Design, synthesis, and pharmacological evaluation of benzamide derivatives as glucokinase activators. Bioorganic Med. Chem. (2012) 70685618 639
GKA24-26b GKA24-26b GKA: Systemic 2012 Benzamide,Sulfoxide/Sulfone derivatives 552.64 3.8 Chinese Academy of Sciences (Shanghai, CHINA) C28H32N4O6S Mao, W. et al. Design, synthesis, and pharmacological evaluation of benzamide derivatives as glucokinase activators. Bioorganic Med. Chem. (2012) 70689814 640
GKA24-27a GKA24-27a GKA: Systemic 2012 Benzamide,Sulfoxide/Sulfone derivatives 542.62 4.49 Chinese Academy of Sciences (Shanghai, CHINA) C27H31FN4O5S Mao, W. et al. Design, synthesis, and pharmacological evaluation of benzamide derivatives as glucokinase activators. Bioorganic Med. Chem. (2012) 70685619 641
GKA24-27b GKA24-27b GKA: Systemic 2012 Benzamide,Sulfoxide/Sulfone derivatives 528.6 4.09 Chinese Academy of Sciences (Shanghai, CHINA) C26H29FN4O5S Mao, W. et al. Design, synthesis, and pharmacological evaluation of benzamide derivatives as glucokinase activators. Bioorganic Med. Chem. (2012) 70691950 642
GKA24-28a GKA24-28a GKA: Systemic 2012 Benzamide,Sulfoxide/Sulfone derivatives 568.68 4.36 Chinese Academy of Sciences (Shanghai, CHINA) C29H36N4O6S Mao, W. et al. Design, synthesis, and pharmacological evaluation of benzamide derivatives as glucokinase activators. Bioorganic Med. Chem. (2012) 70685620 643
GKA24-28b GKA24-28b GKA: Systemic 2012 Benzamide,Sulfoxide/Sulfone derivatives 554.66 3.96 Chinese Academy of Sciences (Shanghai, CHINA) C28H34N4O6S Mao, W. et al. Design, synthesis, and pharmacological evaluation of benzamide derivatives as glucokinase activators. Bioorganic Med. Chem. (2012) 70681408 644
GKA24-5 GKA24-5 GKA: Systemic 2012 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 484.59 4.91 Chinese Academy of Sciences (Shanghai, CHINA) C24H24N2O5S2 Mao, W. et al. Design, synthesis, and pharmacological evaluation of benzamide derivatives as glucokinase activators. Bioorganic Med. Chem. (2012) 60150714 617
GKA2-5 GKA2-5 GKA: Systemic 2005 Pyridine 289.28 1.82 AstraZeneca (UK) C15H15NO5 McKerrecher, D. et al. Discovery, synthesis and biological evaluation of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2005) 44400862 49
GKA25-17 GKA25-17 GKA: Systemic 2012 Pyridine 366.38 4.15 Pfizer Global Research & Development (USA) C18H21F3N4O Pfefferkorn, J. A. et al. Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl) propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. J. Med. Chem. (2012) 46181353 645
GKA25-20 GKA25-20 GKA: Systemic 2012 Pyridine 396.36 3.65 Pfizer Global Research & Development (USA) C18H19F3N4O3 Pfefferkorn, J. A. et al. Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl) propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. J. Med. Chem. (2012) 56955210 646
GKA25-21 GKA25-21 GKA: Systemic 2012 Pyridine 396.36 3.32 Pfizer Global Research & Development (USA) C18H19F3N4O3 Pfefferkorn, J. A. et al. Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl) propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. J. Med. Chem. (2012) 56955211 647
GKA25-22 GKA25-22 GKA: Hepatoselective 2012 Pyridine 410.39 3.25 Pfizer Global Research & Development (USA) C19H21F3N4O3 Pfefferkorn, J. A. et al. Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl) propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. J. Med. Chem. (2012) 46181666 648
GKA25-23 GKA25-23 GKA: Hepatoselective 2012 Pyridine,Sulfoxide/Sulfone derivatives 432.42 2.54 Pfizer Global Research & Development (USA) C17H19F3N4O4S Pfefferkorn, J. A. et al. Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl) propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. J. Med. Chem. (2012) 46181585 649
GKA25-24 GKA25-24 GKA: Systemic 2012 Pyridine 432.33 1.83 Pfizer Global Research & Development (USA) C17H20F3N4O4P Pfefferkorn, J. A. et al. Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl) propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. J. Med. Chem. (2012) 46181586 650
GKA25-25 GKA25-25 GKA: Hepatoselective 2012 Pyridine 420.39 3.08 Pfizer Global Research & Development (USA) C18H19F3N8O Pfefferkorn, J. A. et al. Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl) propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. J. Med. Chem. (2012) 56955212 651
GKA25-26 GKA25-26 GKA: Hepatoselective 2012 Pyridine 439.39 2.93 Pfizer Global Research & Development (USA) C19H20F3N5O4 Pfefferkorn, J. A. et al. Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl) propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. J. Med. Chem. (2012) 46181668 652
GKA25-27 GKA25-27 GKA: Systemic 2012 399.37 2.87 Pfizer Global Research & Development (USA) C17H20F3N5O3 Pfefferkorn, J. A. et al. Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl) propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. J. Med. Chem. (2012) 46181581 653
GKA25-28 GKA25-28 GKA: Systemic 2012 Pyrazine 397.35 2.58 Pfizer Global Research & Development (USA) C17H18F3N5O3 Pfefferkorn, J. A. et al. Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl) propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. J. Med. Chem. (2012) 46181505 654
GKA2-6 GKA2-6 GKA: Systemic 2005 Pyridine 441.48 5.11 AstraZeneca (UK) C27H23NO5 McKerrecher, D. et al. Discovery, synthesis and biological evaluation of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2005) 44400874 50
GKA26-16 GKA26-16 GKA: Systemic 2012 Benzamide,Pyrazine 432.44 0.52 Pfizer Global Research & Development (USA) C21H20N8O3 Pfefferkorn, J. A. et al. The design and synthesis of indazole and pyrazolopyridine based glucokinase activators for the treatment of Type 2 diabetes mellitus. Bioorganic Med. Chem. Lett. (2012) 46909841 655
GKA26-26 GKA26-26 GKA: Systemic 2012 Benzamide,Pyrazine 432.44 0.41 Pfizer Global Research & Development (USA) C21H20N8O3 Pfefferkorn, J. A. et al. The design and synthesis of indazole and pyrazolopyridine based glucokinase activators for the treatment of Type 2 diabetes mellitus. Bioorganic Med. Chem. Lett. (2012) 71454074 656
GKA26-27 GKA26-27 GKA: Systemic 2012 Benzamide,Pyrazine 430.46 1.99 Pfizer Global Research & Development (USA) C23H22N6O3 Pfefferkorn, J. A. et al. The design and synthesis of indazole and pyrazolopyridine based glucokinase activators for the treatment of Type 2 diabetes mellitus. Bioorganic Med. Chem. Lett. (2012) 71454075 657
GKA26-28 GKA26-28 GKA: Systemic 2012 Benzamide,Pyrazine,Sulfoxide/Sulfone derivatives 437.47 1.77 Pfizer Global Research & Development (USA) C21H19N5O4S Pfefferkorn, J. A. et al. The design and synthesis of indazole and pyrazolopyridine based glucokinase activators for the treatment of Type 2 diabetes mellitus. Bioorganic Med. Chem. Lett. (2012) 46910963 658
GKA26-29 GKA26-29 GKA: Systemic 2012 Benzamide,Pyrazine,Sulfoxide/Sulfone derivatives 451.5 2.13 Pfizer Global Research & Development (USA) C22H21N5O4S Pfefferkorn, J. A. et al. The design and synthesis of indazole and pyrazolopyridine based glucokinase activators for the treatment of Type 2 diabetes mellitus. Bioorganic Med. Chem. Lett. (2012) 46911020 659
GKA26-30 GKA26-30 GKA: Systemic 2012 Benzamide,Pyrazine,Sulfoxide/Sulfone derivatives 463.51 2.32 Pfizer Global Research & Development (USA) C23H21N5O4S Pfefferkorn, J. A. et al. The design and synthesis of indazole and pyrazolopyridine based glucokinase activators for the treatment of Type 2 diabetes mellitus. Bioorganic Med. Chem. Lett. (2012) 46911021 660
GKA26-31 GKA26-31 GKA: Systemic 2012 Benzamide,Pyrazine,Sulfoxide/Sulfone derivatives 466.51 1.68 Pfizer Global Research & Development (USA) C22H22N6O4S Pfefferkorn, J. A. et al. The design and synthesis of indazole and pyrazolopyridine based glucokinase activators for the treatment of Type 2 diabetes mellitus. Bioorganic Med. Chem. Lett. (2012) 71457592 661
GKA26-32 GKA26-32 GKA: Systemic 2012 Benzamide,Pyrazine,Sulfoxide/Sulfone derivatives 452.49 1.49 Pfizer Global Research & Development (USA) C21H20N6O4S Pfefferkorn, J. A. et al. The design and synthesis of indazole and pyrazolopyridine based glucokinase activators for the treatment of Type 2 diabetes mellitus. Bioorganic Med. Chem. Lett. (2012) 71457593 662
GKA26-33 GKA26-33 GKA: Systemic 2012 Benzamide,Pyrazine,Sulfoxide/Sulfone derivatives 438.46 1.09 Pfizer Global Research & Development (USA) C20H18N6O4S Pfefferkorn, J. A. et al. The design and synthesis of indazole and pyrazolopyridine based glucokinase activators for the treatment of Type 2 diabetes mellitus. Bioorganic Med. Chem. Lett. (2012) 71450444 663
GKA26-34 GKA26-34 GKA: Systemic 2012 Benzamide,Pyridine,Pyrazine 449.44 1.35 Pfizer Global Research & Development (USA) C22H20FN7O3 Pfefferkorn, J. A. et al. The design and synthesis of indazole and pyrazolopyridine based glucokinase activators for the treatment of Type 2 diabetes mellitus. Bioorganic Med. Chem. Lett. (2012) 46911180 664
GKA26-35 GKA26-35 GKA: Systemic 2012 Benzamide,Pyridine,Pyrazine 461.45 1.48 Pfizer Global Research & Development (USA) C23H20FN7O3 Pfefferkorn, J. A. et al. The design and synthesis of indazole and pyrazolopyridine based glucokinase activators for the treatment of Type 2 diabetes mellitus. Bioorganic Med. Chem. Lett. (2012) 71461227 665
GKA26-36 GKA26-36 GKA: Systemic 2012 Benzamide,Pyrimidine,Pyrazine 432.44 0.6 Pfizer Global Research & Development (USA) C21H20N8O3 Pfefferkorn, J. A. et al. The design and synthesis of indazole and pyrazolopyridine based glucokinase activators for the treatment of Type 2 diabetes mellitus. Bioorganic Med. Chem. Lett. (2012) 46911072 666
GKA26-37 GKA26-37 GKA: Systemic 2012 Benzamide,Pyrazine 451.5 2.07 Pfizer Global Research & Development (USA) C22H21N5O4S Pfefferkorn, J. A. et al. The design and synthesis of indazole and pyrazolopyridine based glucokinase activators for the treatment of Type 2 diabetes mellitus. Bioorganic Med. Chem. Lett. (2012) 46911181 667
GKA26-38 GKA26-38 GKA: Systemic 2012 Benzamide,Pyrazine 465.52 2.59 Pfizer Global Research & Development (USA) C23H23N5O4S Pfefferkorn, J. A. et al. The design and synthesis of indazole and pyrazolopyridine based glucokinase activators for the treatment of Type 2 diabetes mellitus. Bioorganic Med. Chem. Lett. (2012) 71459489 668
GKA26-39 GKA26-39 GKA: Systemic 2012 Benzamide,Pyrazine 467.5 1.02 Pfizer Global Research & Development (USA) C22H21N5O5S Pfefferkorn, J. A. et al. The design and synthesis of indazole and pyrazolopyridine based glucokinase activators for the treatment of Type 2 diabetes mellitus. Bioorganic Med. Chem. Lett. (2012) 71450445 669
GKA26-40 GKA26-40 GKA: Systemic 2012 Benzamide,Pyrazine 463.51 2.22 Pfizer Global Research & Development (USA) C23H21N5O4S Pfefferkorn, J. A. et al. The design and synthesis of indazole and pyrazolopyridine based glucokinase activators for the treatment of Type 2 diabetes mellitus. Bioorganic Med. Chem. Lett. (2012) 71461228 670
GKA26-41 GKA26-41 GKA: Systemic 2012 Benzamide,Pyridine,Pyrazine 463.46 1.65 Pfizer Global Research & Development (USA) C23H22FN7O3 Pfefferkorn, J. A. et al. The design and synthesis of indazole and pyrazolopyridine based glucokinase activators for the treatment of Type 2 diabetes mellitus. Bioorganic Med. Chem. Lett. (2012) 46911123 671
GKA26-42 GKA26-42 GKA: Systemic 2012 Benzamide,Pyridine,Pyrazine 475.47 1.78 Pfizer Global Research & Development (USA) C24H22FN7O3 Pfefferkorn, J. A. et al. The design and synthesis of indazole and pyrazolopyridine based glucokinase activators for the treatment of Type 2 diabetes mellitus. Bioorganic Med. Chem. Lett. (2012) 46911124 672
GKA2-7 GKA2-7 GKA: Systemic 2005 Pyridine 454.47 4.48 AstraZeneca (UK) C27H22N2O5 McKerrecher, D. et al. Discovery, synthesis and biological evaluation of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2005) 44401560 51
GKA27-1 GKA27-1 GKA: Systemic 2012 Benzamide 450.49 2.24 AstraZeneca (UK) C24H26N4O5 Waring, M. J. et al. Property based optimisation of glucokinase activators - Discovery of the phase IIb clinical candidate AZD1656. Medchemcomm (2012) 73004962 673
GKA27-15 GKA27-15 GKA: Systemic 2012 Benzamide 464.51 2.78 AstraZeneca (UK) C25H28N4O5 Waring, M. J. et al. Property based optimisation of glucokinase activators - Discovery of the phase IIb clinical candidate AZD1656. Medchemcomm (2012) 11634069 680
GKA27-16 GKA27-16 GKA: Systemic 2012 Benzamide 434.49 3.29 AstraZeneca (UK) C24H26N4O4 Waring, M. J. et al. Property based optimisation of glucokinase activators - Discovery of the phase IIb clinical candidate AZD1656. Medchemcomm (2012) 11178027 681
GKA27-17 GKA27-17 GKA: Systemic 2012 Benzamide 462.5 2.54 AstraZeneca (UK) C25H26N4O5 Waring, M. J. et al. Property based optimisation of glucokinase activators - Discovery of the phase IIb clinical candidate AZD1656. Medchemcomm (2012) 15942650 682
GKA27-18 GKA27-18 GKA: Systemic 2012 Benzamide 476.52 2.9 AstraZeneca (UK) C26H28N4O5 Waring, M. J. et al. Property based optimisation of glucokinase activators - Discovery of the phase IIb clinical candidate AZD1656. Medchemcomm (2012) 16071499 683
GKA27-19 GKA27-19 GKA: Systemic 2012 Benzamide 470.47 3.25 AstraZeneca (UK) C24H24F2N4O4 Waring, M. J. et al. Property based optimisation of glucokinase activators - Discovery of the phase IIb clinical candidate AZD1656. Medchemcomm (2012) 16071731 684
GKA27-2 GKA27-2 GKA: Systemic 2012 Benzamide 464.51 2.54 AstraZeneca (UK) C25H28N4O5 Waring, M. J. et al. Property based optimisation of glucokinase activators - Discovery of the phase IIb clinical candidate AZD1656. Medchemcomm (2012) 11626833 674
GKA27-20 GKA27-20 GKA: Systemic 2012 Benzamide,Pyrazine 476.52 2.73 AstraZeneca (UK) C26H28N4O5 Waring, M. J. et al. Property based optimisation of glucokinase activators - Discovery of the phase IIb clinical candidate AZD1656. Medchemcomm (2012) 90666148 685
GKA27-21 GKA27-21 GKA: Systemic 2012 Benzamide,Pyridine,Pyrazine 477.51 1.99 AstraZeneca (UK) C25H27N5O5 Waring, M. J. et al. Property based optimisation of glucokinase activators - Discovery of the phase IIb clinical candidate AZD1656. Medchemcomm (2012) 16039834 686
GKA27-22 GKA27-22 GKA: Systemic 2012 Benzamide,Pyridine,Pyrazine 477.51 1.99 AstraZeneca (UK) C25H27N5O5 Waring, M. J. et al. Property based optimisation of glucokinase activators - Discovery of the phase IIb clinical candidate AZD1656. Medchemcomm (2012) 73224029 687
GKA27-23 GKA27-23 GKA: Systemic 2012 Benzamide,Pyridine,Pyrazine 511.96 2.62 AstraZeneca (UK) C25H26ClN5O5 Waring, M. J. et al. Property based optimisation of glucokinase activators - Discovery of the phase IIb clinical candidate AZD1656. Medchemcomm (2012) 16039796 688
GKA27-24 GKA27-24 GKA: Systemic 2012 Benzamide,Pyrazine 478.5 1.25 AstraZeneca (UK) C24H26N6O5 Waring, M. J. et al. Property based optimisation of glucokinase activators - Discovery of the phase IIb clinical candidate AZD1656. Medchemcomm (2012) 16039797 689
GKA27-3 GKA27-3 GKA: Systemic 2012 Benzamide 478.54 2.94 AstraZeneca (UK) C26H30N4O5 Waring, M. J. et al. Property based optimisation of glucokinase activators - Discovery of the phase IIb clinical candidate AZD1656. Medchemcomm (2012) 11634336 675
GKA27-4 GKA27-4 GKA: Systemic 2012 Benzamide 436.46 2.22 AstraZeneca (UK) C23H24N4O5 Waring, M. J. et al. Property based optimisation of glucokinase activators - Discovery of the phase IIb clinical candidate AZD1656. Medchemcomm (2012) 11662060 676
GKA27-5 GKA27-5 GKA: Systemic 2012 Thiazole/Thiadiazole,Benzamide 453.51 2.96 AstraZeneca (UK) C23H23N3O5S Waring, M. J. et al. Property based optimisation of glucokinase activators - Discovery of the phase IIb clinical candidate AZD1656. Medchemcomm (2012) 11576079 677
GKA27-6 GKA27-6 GKA: Systemic 2012 Thiazole/Thiadiazole,Benzamide 468.53 3.16 AstraZeneca (UK) C23H24N4O5S Waring, M. J. et al. Property based optimisation of glucokinase activators - Discovery of the phase IIb clinical candidate AZD1656. Medchemcomm (2012) 11641315 678
GKA27-7 GKA27-7 GKA: Systemic 2012 Benzamide,Pyrazine 462.5 2.19 AstraZeneca (UK) C25H26N4O5 Waring, M. J. et al. Property based optimisation of glucokinase activators - Discovery of the phase IIb clinical candidate AZD1656. Medchemcomm (2012) 11539903 679
GKA2-8 GKA2-8 GKA: Systemic 2005 Pyridine 394.44 3.52 AstraZeneca (UK) C21H18N2O4S McKerrecher, D. et al. Discovery, synthesis and biological evaluation of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2005) 44401351 52
GKA28-11a GKA28-11a GKA: Systemic 2012 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 476.57 2.65 Chinese Academy of Sciences (Shanghai, CHINA) C22H24N2O6S2 Ye, N. et al. Investigation on the oxidation of aryl oxiranylmethanols and the synthesis of 2-aryl-N-thiazolyl-oxirane-2-carboxamides as glucokinase activators. Tetrahedron Lett. (2012) 70677270 693
GKA28-4a GKA28-4a GKA: Systemic 2012 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 476.61 3.26 Chinese Academy of Sciences (Shanghai, CHINA) C23H28N2O5S2 Ye, N. et al. Investigation on the oxidation of aryl oxiranylmethanols and the synthesis of 2-aryl-N-thiazolyl-oxirane-2-carboxamides as glucokinase activators. Tetrahedron Lett. (2012) 70677111 690
GKA28-4b GKA28-4b GKA: Systemic 2012 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 452.52 2.53 Chinese Academy of Sciences (Shanghai, CHINA) C20H21FN2O5S2 Ye, N. et al. Investigation on the oxidation of aryl oxiranylmethanols and the synthesis of 2-aryl-N-thiazolyl-oxirane-2-carboxamides as glucokinase activators. Tetrahedron Lett. (2012) 70677112 691
GKA28-4c GKA28-4c GKA: Systemic 2012 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 579.73 3.53 Chinese Academy of Sciences (Shanghai, CHINA) C30H33N3O5S2 Ye, N. et al. Investigation on the oxidation of aryl oxiranylmethanols and the synthesis of 2-aryl-N-thiazolyl-oxirane-2-carboxamides as glucokinase activators. Tetrahedron Lett. (2012) 70677269 692
GKA2-9 GKA2-9 GKA: Systemic 2005 Benzamide,Pyridine 394.44 3.52 AstraZeneca (UK) C21H18N2O4S McKerrecher, D. et al. Discovery, synthesis and biological evaluation of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2005) 44401271 53
GKA29-1a GKA29-1a GKA: Systemic 2012 Thiazole/Thiadiazole,Indole/Benzimidazole/Indazole 424.9 4.55 Chinese Academy of Sciences (Shanghai, CHINA) C21H17ClN4O2S Zhang, L. et al. Discover+L692:M699y of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 71533483 694
GKA29-1b GKA29-1b GKA: Systemic 2012 Thiazole/Thiadiazole,Indole/Benzimidazole/Indazole 482.94 4.73 Chinese Academy of Sciences (Shanghai, CHINA) C23H19ClN4O4S Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 71541684 695
GKA29-1c GKA29-1c GKA: Systemic 2012 Thiazole/Thiadiazole,Indole/Benzimidazole/Indazole 559.04 6.23 Chinese Academy of Sciences (Shanghai, CHINA) C29H23ClN4O4S Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 71541685 696
GKA29-1d GKA29-1d GKA: Systemic 2012 Thiazole/Thiadiazole,Indole/Benzimidazole/Indazole 496.97 5.1 Chinese Academy of Sciences (Shanghai, CHINA) C24H21ClN4O4S Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 71541686 697
GKA29-1e GKA29-1e GKA: Systemic 2012 Thiazole/Thiadiazole,Indole/Benzimidazole/Indazole 559.04 6.23 Chinese Academy of Sciences (Shanghai, CHINA) C29H23ClN4O4S Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 71540033 698
GKA29-1f GKA29-1f GKA: Systemic 2012 Thiazole/Thiadiazole,Indole/Benzimidazole/Indazole 478.52 4.08 Chinese Academy of Sciences (Shanghai, CHINA) C24H22N4O5S Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 71540034 699
GKA29-1g GKA29-1g GKA: Systemic 2012 Thiazole/Thiadiazole,Indole/Benzimidazole/Indazole 425.89 3.98 Chinese Academy of Sciences (Shanghai, CHINA) C20H16ClN5O2S Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 71540035 700
GKA29-1h GKA29-1h GKA: Systemic 2012 Pyridine,Indole/Benzimidazole/Indazole 418.88 4.44 Chinese Academy of Sciences (Shanghai, CHINA) C23H19ClN4O2 Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 71540036 701
GKA29-1i GKA29-1i GKA: Systemic 2012 Pyridine,Indole/Benzimidazole/Indazole 476.91 4.3 Chinese Academy of Sciences (Shanghai, CHINA) C25H21ClN4O4 Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 71533536 702
GKA29-1j GKA29-1j GKA: Systemic 2012 Pyridine,Indole/Benzimidazole/Indazole 478.93 2.91 Chinese Academy of Sciences (Shanghai, CHINA) C25H23ClN4O4 Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 78101726 703
GKA29-1k GKA29-1k GKA: Systemic 2012 Pyridine,Indole/Benzimidazole/Indazole 444.91 5.22 Chinese Academy of Sciences (Shanghai, CHINA) C25H21ClN4O2 Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 71540037 704
GKA29-1l GKA29-1l GKA: Systemic 2012 Pyridine,Indole/Benzimidazole/Indazole 477.9 3.74 Chinese Academy of Sciences (Shanghai, CHINA) C24H20ClN5O4 Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 71540138 705
GKA29-2a GKA29-2a GKA: Systemic 2012 Pyridine,Indole/Benzimidazole/Indazole 271.7 3.11 Chinese Academy of Sciences (Shanghai, CHINA) C14H10ClN3O Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 46557807 706
GKA29-2b GKA29-2b GKA: Systemic 2012 Pyridine,Indole/Benzimidazole/Indazole 329.74 2.96 Chinese Academy of Sciences (Shanghai, CHINA) C16H12ClN3O3 Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 71540139 707
GKA29-2c GKA29-2c GKA: Systemic 2012 Pyridine,Indole/Benzimidazole/Indazole 405.83 4.46 Chinese Academy of Sciences (Shanghai, CHINA) C22H16ClN3O3 Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 71540140 708
GKA29-2d GKA29-2d GKA: Systemic 2012 Pyridine,Indole/Benzimidazole/Indazole 315.71 2.64 Chinese Academy of Sciences (Shanghai, CHINA) C15H10ClN3O3 Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 71540141 709
GKA29-2e GKA29-2e GKA: Systemic 2012 Pyridine,Indole/Benzimidazole/Indazole 297.74 3.88 Chinese Academy of Sciences (Shanghai, CHINA) C16H12ClN3O Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 85881420 710
GKA29-2f GKA29-2f GKA: Systemic 2012 Pyridine,Indole/Benzimidazole/Indazole 350.6 3.8 Chinese Academy of Sciences (Shanghai, CHINA) C14H9BrClN3O Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 85881380 711
GKA29-2g GKA29-2g GKA: Systemic 2012 Thiazole/Thiadiazole,Indole/Benzimidazole/Indazole 349.79 3.76 Chinese Academy of Sciences (Shanghai, CHINA) C15H12ClN3O3S Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 71540142 712
GKA29-2h GKA29-2h GKA: Systemic 2012 Thiazole/Thiadiazole,Indole/Benzimidazole/Indazole 335.77 3.4 Chinese Academy of Sciences (Shanghai, CHINA) C14H10ClN3O3S Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 71540143 713
GKA29-2i GKA29-2i GKA: Systemic 2012 Pyridine 388.8 0.92 Chinese Academy of Sciences (Shanghai, CHINA) C18H17ClN4O4 Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 71540144 714
GKA29-3a GKA29-3a GKA: Systemic 2012 Thiazole/Thiadiazole 438.37 5.61 Chinese Academy of Sciences (Shanghai, CHINA) C20H21Cl2N3O2S Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 10138013 715
GKA29-3b GKA29-3b GKA: Systemic 2012 Thiazole/Thiadiazole 452.4 6.01 Chinese Academy of Sciences (Shanghai, CHINA) C21H23Cl2N3O2S Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 71540261 716
GKA29-3c GKA29-3c GKA: Systemic 2012 Thiazole/Thiadiazole 496.41 5.79 Chinese Academy of Sciences (Shanghai, CHINA) C22H23Cl2N3O4S Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 71540262 717
GKA29-3d GKA29-3d GKA: Systemic 2012 Thiazole/Thiadiazole 510.43 6.16 Chinese Academy of Sciences (Shanghai, CHINA) C23H25Cl2N3O4S Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 71540263 718
GKA29-3e GKA29-3e GKA: Systemic 2012 Thiazole/Thiadiazole 468.4 4.76 Chinese Academy of Sciences (Shanghai, CHINA) C21H23Cl2N3O3S Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 71540264 719
GKA29-3f GKA29-3f GKA: Systemic 2012 Thiazole/Thiadiazole 482.38 5.47 Chinese Academy of Sciences (Shanghai, CHINA) C21H21Cl2N3O4S Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 71540265 720
GKA29-3g GKA29-3g GKA: Systemic 2012 Thiazole/Thiadiazole 452.4 6.01 Chinese Academy of Sciences (Shanghai, CHINA) C21H23Cl2N3O2S Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 71540266 721
GKA29-3h GKA29-3h GKA: Systemic 2012 Thiazole/Thiadiazole 496.41 5.79 Chinese Academy of Sciences (Shanghai, CHINA) C22H23Cl2N3O4S Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 71540376 722
GKA29-3i GKA29-3i GKA: Systemic 2012 Thiazole/Thiadiazole 510.43 6.16 Chinese Academy of Sciences (Shanghai, CHINA) C23H25Cl2N3O4S Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 71540377 723
GKA29-3j GKA29-3j GKA: Systemic 2012 Thiazole/Thiadiazole 482.38 5.47 Chinese Academy of Sciences (Shanghai, CHINA) C21H21Cl2N3O4S Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 71540378 724
GKA29-3k GKA29-3k GKA: Systemic 2012 Thiazole/Thiadiazole 524.46 5.8 Chinese Academy of Sciences (Shanghai, CHINA) C24H27Cl2N3O4S Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 71540379 725
GKA29-3l GKA29-3l GKA: Systemic 2012 Thiazole/Thiadiazole 510.43 5.43 Chinese Academy of Sciences (Shanghai, CHINA) C23H25Cl2N3O4S Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 71540380 726
GKA29-3m GKA29-3m GKA: Systemic 2012 Thiazole/Thiadiazole 496.41 5.11 Chinese Academy of Sciences (Shanghai, CHINA) C22H23Cl2N3O4S Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 71540381 727
GKA29-3n GKA29-3n GKA: Systemic 2012 Thiazole/Thiadiazole 482.42 5.22 Chinese Academy of Sciences (Shanghai, CHINA) C22H25Cl2N3O3S Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 71540484 728
GKA29-3o GKA29-3o GKA: Systemic 2012 Benzo/Pyrido-thiazole 488.43 7.03 Chinese Academy of Sciences (Shanghai, CHINA) C24H23Cl2N3O2S Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 71540485 729
GKA29-3p GKA29-3p GKA: Systemic 2012 Benzo/Pyrido-thiazole 522.87 7.66 Chinese Academy of Sciences (Shanghai, CHINA) C24H22Cl3N3O2S Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 71540486 730
GKA29-3q GKA29-3q GKA: Systemic 2012 Pyridine 490.38 5.36 Chinese Academy of Sciences (Shanghai, CHINA) C24H25Cl2N3O4 Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 71540487 731
GKA29-3r GKA29-3r GKA: Systemic 2012 Pyridine 490.38 5.36 Chinese Academy of Sciences (Shanghai, CHINA) C24H25Cl2N3O4 Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 71540488 732
GKA29-3s GKA29-3s GKA: Systemic 2012 Thiazole/Thiadiazole 508.35 4.76 Chinese Academy of Sciences (Shanghai, CHINA) C22H16Cl2FN3O4S Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 71540489 733
GKA29-3t GKA29-3t GKA: Systemic 2012 Thiazole/Thiadiazole 522.38 4.39 Chinese Academy of Sciences (Shanghai, CHINA) C23H18Cl2FN3O4S Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 71540592 734
GKA29-4a GKA29-4a GKA: Systemic 2012 Thiazole/Thiadiazole 452.35 5.55 Chinese Academy of Sciences (Shanghai, CHINA) C20H19Cl2N3O3S Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 71540593 735
GKA29-4b GKA29-4b GKA: Systemic 2012 Thiazole/Thiadiazole 466.38 5.95 Chinese Academy of Sciences (Shanghai, CHINA) C21H21Cl2N3O3S Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 71540594 736
GKA29-4c GKA29-4c GKA: Systemic 2012 Thiazole/Thiadiazole 524.42 6.11 Chinese Academy of Sciences (Shanghai, CHINA) C23H23Cl2N3O5S Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 71540595 737
GKA29-4d GKA29-4d GKA: Systemic 2012 Thiazole/Thiadiazole 510.39 5.74 Chinese Academy of Sciences (Shanghai, CHINA) C22H21Cl2N3O5S Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 71540596 738
GKA29-4e GKA29-4e GKA: Systemic 2012 Thiazole/Thiadiazole 510.39 5.74 Chinese Academy of Sciences (Shanghai, CHINA) C22H21Cl2N3O5S Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 71540597 739
GKA29-4f GKA29-4f GKA: Systemic 2012 Thiazole/Thiadiazole 524.42 6.11 Chinese Academy of Sciences (Shanghai, CHINA) C23H23Cl2N3O5S Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 71540709 740
GKA29-4g GKA29-4g GKA: Systemic 2012 Benzo/Pyrido-thiazole 502.41 6.98 Chinese Academy of Sciences (Shanghai, CHINA) C24H21Cl2N3O3S Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 71540710 741
GKA29-4h GKA29-4h GKA: Systemic 2012 Thiazole/Thiadiazole 522.33 4.7 Chinese Academy of Sciences (Shanghai, CHINA) C22H14Cl2FN3O5S Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 71540711 742
GKA29-5a GKA29-5a GKA: Systemic 2012 Thiazole/Thiadiazole,Urea 481.4 5.68 Chinese Academy of Sciences (Shanghai, CHINA) C21H22Cl2N4O3S Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 71540712 743
GKA29-5b GKA29-5b GKA: Systemic 2012 Thiazole/Thiadiazole,Urea 525.4 5.47 Chinese Academy of Sciences (Shanghai, CHINA) C22H22Cl2N4O5S Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 71540713 744
GKA29-5c GKA29-5c GKA: Systemic 2012 Thiazole/Thiadiazole,Urea 539.43 5.83 Chinese Academy of Sciences (Shanghai, CHINA) C23H24Cl2N4O5S Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 71540825 745
GKA29-5d GKA29-5d GKA: Systemic 2012 Thiazole/Thiadiazole,Urea 511.38 5.14 Chinese Academy of Sciences (Shanghai, CHINA) C21H20Cl2N4O5S Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 71540826 746
GKA29-5e GKA29-5e GKA: Systemic 2012 Thiazole/Thiadiazole,Urea 537.35 4.43 Chinese Academy of Sciences (Shanghai, CHINA) C22H15Cl2FN4O5S Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 71540827 747
GKA29-6a GKA29-6a GKA: Systemic 2012 Thiazole/Thiadiazole,Benzamide 455.4 6.12 Chinese Academy of Sciences (Shanghai, CHINA) C20H24Cl2N4O2S Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 71540828 748
GKA29-6b GKA29-6b GKA: Systemic 2012 Thiazole/Thiadiazole,Benzamide 499.41 5.91 Chinese Academy of Sciences (Shanghai, CHINA) C21H24Cl2N4O4S Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 71540829 749
GKA29-6c GKA29-6c GKA: Systemic 2012 Thiazole/Thiadiazole,Benzamide 513.44 6.28 Chinese Academy of Sciences (Shanghai, CHINA) C22H26Cl2N4O4S Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 71540940 750
GKA29-6d GKA29-6d GKA: Systemic 2012 Thiazole/Thiadiazole,Benzamide 511.35 4.87 Chinese Academy of Sciences (Shanghai, CHINA) C21H17Cl2FN4O4S Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 71540941 751
GKA29-6e GKA29-6e GKA: Systemic 2012 Benzamide,Pyridine 478.37 5.61 Chinese Academy of Sciences (Shanghai, CHINA) C23H25Cl2N3O4 Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 71540942 752
GKA29-6f GKA29-6f GKA: Systemic 2012 Benzamide,Pyridine 490.31 4.57 Chinese Academy of Sciences (Shanghai, CHINA) C23H18Cl2FN3O4 Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 71540943 753
GKA29-6g GKA29-6g GKA: Systemic 2012 Benzamide,Pyridine,Sulfoxide/Sulfone derivatives 487.57 3.59 Chinese Academy of Sciences (Shanghai, CHINA) C24H29N3O6S Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 78101727 754
GKA29-6h GKA29-6h GKA: Systemic 2012 Benzamide,Pyridine,Sulfoxide/Sulfone derivatives 473.54 3.26 Chinese Academy of Sciences (Shanghai, CHINA) C23H27N3O6S Zhang, L. et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. Eur. J. Med. Chem. (2012) 71540944 755
GKA30-10 GKA30-10 GKA: Systemic 2012 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 435.56 3.5 Hoffmann-La Roche Inc. (USA) C20H25N3O4S2 Sarabu, R. et al. Discovery of piragliatin-first glucokinase activator studied in type 2 diabetic patients. J. Med. Chem. (2012) 66560559 761
GKA30-11 GKA30-11 GKA: Systemic 2012 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 423.51 4.05 Hoffmann-La Roche Inc. (USA) C18H21N3O5S2 Sarabu, R. et al. Discovery of piragliatin-first glucokinase activator studied in type 2 diabetic patients. J. Med. Chem. (2012) 66560560 762
GKA30-12 GKA30-12 GKA: Systemic 2012 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 412.95 4.51 Hoffmann-La Roche Inc. (USA) C18H21ClN2O3S2 Sarabu, R. et al. Discovery of piragliatin-first glucokinase activator studied in type 2 diabetic patients. J. Med. Chem. (2012) 59086457 763
GKA30-13 GKA30-13 GKA: Systemic 2012 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 457.4 4.58 Hoffmann-La Roche Inc. (USA) C18H21BrN2O3S2 Sarabu, R. et al. Discovery of piragliatin-first glucokinase activator studied in type 2 diabetic patients. J. Med. Chem. (2012) 22315245 764
GKA30-14 GKA30-14 GKA: Systemic 2012 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 396.5 3.99 Hoffmann-La Roche Inc. (USA) C18H21FN2O3S2 Sarabu, R. et al. Discovery of piragliatin-first glucokinase activator studied in type 2 diabetic patients. J. Med. Chem. (2012) 22315157 765
GKA30-15 GKA30-15 GKA: Systemic 2012 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 446.51 4.77 Hoffmann-La Roche Inc. (USA) C19H21F3N2O3S2 Sarabu, R. et al. Discovery of piragliatin-first glucokinase activator studied in type 2 diabetic patients. J. Med. Chem. (2012) 87416902 766
GKA30-16 GKA30-16 GKA: Systemic 2012 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 423.51 3.71 Hoffmann-La Roche Inc. (USA) C18H21N3O5S2 Sarabu, R. et al. Discovery of piragliatin-first glucokinase activator studied in type 2 diabetic patients. J. Med. Chem. (2012) 12088920 767
GKA30-17 GKA30-17 GKA: Systemic 2012 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 403.52 3.6 Hoffmann-La Roche Inc. (USA) C19H21N3O3S2 Sarabu, R. et al. Discovery of piragliatin-first glucokinase activator studied in type 2 diabetic patients. J. Med. Chem. (2012) 22315136 768
GKA30-18 GKA30-18 GKA: Systemic 2012 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 393.52 3.76 Hoffmann-La Roche Inc. (USA) C18H23N3O3S2 Sarabu, R. et al. Discovery of piragliatin-first glucokinase activator studied in type 2 diabetic patients. J. Med. Chem. (2012) 22315133 769
GKA30-19 GKA30-19 GKA: Systemic 2012 Pyridine,Sulfoxide/Sulfone derivatives 372.48 3.78 Hoffmann-La Roche Inc. (USA) C20H24N2O3S Sarabu, R. et al. Discovery of piragliatin-first glucokinase activator studied in type 2 diabetic patients. J. Med. Chem. (2012) 22315084 770
GKA30-20 GKA30-20 GKA: Systemic 2012 Pyridine,Sulfoxide/Sulfone derivatives 406.93 4.41 Hoffmann-La Roche Inc. (USA) C20H23ClN2O3S Sarabu, R. et al. Discovery of piragliatin-first glucokinase activator studied in type 2 diabetic patients. J. Med. Chem. (2012) 59086458 771
GKA30-21 GKA30-21 GKA: Systemic 2012 Pyrazine,Sulfoxide/Sulfone derivatives 373.47 2.71 Hoffmann-La Roche Inc. (USA) C19H23N3O3S Sarabu, R. et al. Discovery of piragliatin-first glucokinase activator studied in type 2 diabetic patients. J. Med. Chem. (2012) 23394571 772
GKA30-22 GKA30-22 GKA: Systemic 2012 Pyrazine,Sulfoxide/Sulfone derivatives 407.91 3.34 Hoffmann-La Roche Inc. (USA) C19H22ClN3O3S Sarabu, R. et al. Discovery of piragliatin-first glucokinase activator studied in type 2 diabetic patients. J. Med. Chem. (2012) 59086459 773
GKA30-23 GKA30-23 GKA: Systemic 2012 Sulfoxide/Sulfone derivatives,Quinoline/Quinazoline 422.54 5.12 Hoffmann-La Roche Inc. (USA) C24H26N2O3S Sarabu, R. et al. Discovery of piragliatin-first glucokinase activator studied in type 2 diabetic patients. J. Med. Chem. (2012) 10224075 774
GKA30-24 GKA30-24 GKA: Systemic 2012 Sulfoxide/Sulfone derivatives,Quinoline/Quinazoline 456.98 5.75 Hoffmann-La Roche Inc. (USA) C24H25ClN2O3S Sarabu, R. et al. Discovery of piragliatin-first glucokinase activator studied in type 2 diabetic patients. J. Med. Chem. (2012) 12067661 775
GKA30-25 GKA30-25 GKA: Systemic 2012 Pyrimidine,Sulfoxide/Sulfone derivatives 373.47 3.13 Hoffmann-La Roche Inc. (USA) C19H23N3O3S Sarabu, R. et al. Discovery of piragliatin-first glucokinase activator studied in type 2 diabetic patients. J. Med. Chem. (2012) 58957184 776
GKA30-26 GKA30-26 GKA: Systemic 2012 Pyrimidine,Sulfoxide/Sulfone derivatives 407.91 3.76 Hoffmann-La Roche Inc. (USA) C19H22ClN3O3S Sarabu, R. et al. Discovery of piragliatin-first glucokinase activator studied in type 2 diabetic patients. J. Med. Chem. (2012) 22315196 777
GKA30-27 GKA30-27 GKA: Systemic 2012 Pyrazine,Sulfoxide/Sulfone derivatives 423.91 1.63 Hoffmann-La Roche Inc. (USA) C19H22ClN3O4S Sarabu, R. et al. Discovery of piragliatin-first glucokinase activator studied in type 2 diabetic patients. J. Med. Chem. (2012) 21051869 778
GKA30-28 GKA30-28 GKA: Systemic 2012 Pyrazine,Sulfoxide/Sulfone derivatives 423.91 1.63 Hoffmann-La Roche Inc. (USA) C19H22ClN3O4S Sarabu, R. et al. Discovery of piragliatin-first glucokinase activator studied in type 2 diabetic patients. J. Med. Chem. (2012) 21051870 779
GKA30-29 GKA30-29 GKA: Systemic 2012 Pyrazine,Sulfoxide/Sulfone derivatives 421.9 1.35 Hoffmann-La Roche Inc. (USA) C19H20ClN3O4S Sarabu, R. et al. Discovery of piragliatin-first glucokinase activator studied in type 2 diabetic patients. J. Med. Chem. (2012) 21959027 780
GKA30-5 GKA30-5 GKA: Systemic 2012 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 422.56 3.5 Hoffmann-La Roche Inc. (USA) C20H26N2O4S2 Sarabu, R. et al. Discovery of piragliatin-first glucokinase activator studied in type 2 diabetic patients. J. Med. Chem. (2012) 22315246 756
GKA30-6 GKA30-6 GKA: Systemic 2012 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 408.53 3.03 Hoffmann-La Roche Inc. (USA) C19H24N2O4S2 Sarabu, R. et al. Discovery of piragliatin-first glucokinase activator studied in type 2 diabetic patients. J. Med. Chem. (2012) 22315308 757
GKA30-7 GKA30-7 GKA: Systemic 2012 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 412.95 4.85 Hoffmann-La Roche Inc. (USA) C18H21ClN2O3S2 Sarabu, R. et al. Discovery of piragliatin-first glucokinase activator studied in type 2 diabetic patients. J. Med. Chem. (2012) 59086461 758
GKA30-8 GKA30-8 GKA: Systemic 2012 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 457.4 4.91 Hoffmann-La Roche Inc. (USA) C18H21BrN2O3S2 Sarabu, R. et al. Discovery of piragliatin-first glucokinase activator studied in type 2 diabetic patients. J. Med. Chem. (2012) 59086456 759
GKA30-9 GKA30-9 GKA: Systemic 2012 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 421.53 3.09 Hoffmann-La Roche Inc. (USA) C19H23N3O4S2 Sarabu, R. et al. Discovery of piragliatin-first glucokinase activator studied in type 2 diabetic patients. J. Med. Chem. (2012) 23394566 760
GKA3-10 GKA3-10 GKA: Systemic 2006 Benzamide,Pyridine 388.41 2.57 AstraZeneca (UK) C20H24N2O6 McKerrecher, D. et al. Design of a potent, soluble glucokinase activator with excellent in vivo efficacy. Bioorganic Med. Chem. Lett. (2006) 44410893 71
GKA3-11 GKA3-11 GKA: Systemic 2006 Benzamide,Pyridine 388.41 2.57 AstraZeneca (UK) C20H24N2O6 McKerrecher, D. et al. Design of a potent, soluble glucokinase activator with excellent in vivo efficacy. Bioorganic Med. Chem. Lett. (2006) 44410896 72
GKA31-10 GKA31-10 GKA: Systemic 2013 Pyrazine,Sulfoxide/Sulfone derivatives 470.01 2.8 Hoffmann-La Roche Inc. (USA) C20H24ClN3O4S2 Qian, Y. et al. Identification of RO4597014, a glucokinase activator studied in the clinic for the treatment of type 2 diabetes. ACS Med. Chem. Lett. (2013) 67482709 786
GKA31-11 GKA31-11 GKA: Systemic 2013 Pyrazine,Sulfoxide/Sulfone derivatives 497.99 2.34 Hoffmann-La Roche Inc. (USA) C22H28ClN3O6S Qian, Y. et al. Identification of RO4597014, a glucokinase activator studied in the clinic for the treatment of type 2 diabetes. ACS Med. Chem. Lett. (2013) 10323620 787
GKA31-12 GKA31-12 GKA: Systemic 2013 Pyrazine,Sulfoxide/Sulfone derivatives 497.99 2.34 Hoffmann-La Roche Inc. (USA) C22H28ClN3O6S Qian, Y. et al. Identification of RO4597014, a glucokinase activator studied in the clinic for the treatment of type 2 diabetes. ACS Med. Chem. Lett. (2013) 10074618 788
GKA31-13 GKA31-13 GKA: Systemic 2013 Pyrazine,Sulfoxide/Sulfone derivatives 465.95 2.81 Hoffmann-La Roche Inc. (USA) C20H24ClN5O4S Qian, Y. et al. Identification of RO4597014, a glucokinase activator studied in the clinic for the treatment of type 2 diabetes. ACS Med. Chem. Lett. (2013) 135550502 789
GKA31-14 GKA31-14 GKA: Systemic 2013 Pyrazine,Sulfoxide/Sulfone derivatives 464.97 3.62 Hoffmann-La Roche Inc. (USA) C21H25ClN4O4S Qian, Y. et al. Identification of RO4597014, a glucokinase activator studied in the clinic for the treatment of type 2 diabetes. ACS Med. Chem. Lett. (2013) 135589979 790
GKA31-15 GKA31-15 GKA: Systemic 2013 Pyrazine,Sulfoxide/Sulfone derivatives 500.03 2.55 Hoffmann-La Roche Inc. (USA) C21H26ClN3O5S2 Qian, Y. et al. Identification of RO4597014, a glucokinase activator studied in the clinic for the treatment of type 2 diabetes. ACS Med. Chem. Lett. (2013) 10051679 791
GKA31-16 GKA31-16 GKA: Systemic 2013 Pyrazine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 461.96 2.89 Hoffmann-La Roche Inc. (USA) C22H24ClN3O4S Qian, Y. et al. Identification of RO4597014, a glucokinase activator studied in the clinic for the treatment of type 2 diabetes. ACS Med. Chem. Lett. (2013) 10411992 792
GKA31-17 GKA31-17 GKA: Systemic 2013 Pyrazine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 490.01 3.48 Hoffmann-La Roche Inc. (USA) C24H28ClN3O4S Qian, Y. et al. Identification of RO4597014, a glucokinase activator studied in the clinic for the treatment of type 2 diabetes. ACS Med. Chem. Lett. (2013) 9983024 793
GKA31-18 GKA31-18 GKA: Systemic 2013 Pyrazine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 489.03 3.61 Hoffmann-La Roche Inc. (USA) C24H29ClN4O3S Qian, Y. et al. Identification of RO4597014, a glucokinase activator studied in the clinic for the treatment of type 2 diabetes. ACS Med. Chem. Lett. (2013) 10074262 794
GKA31-19 GKA31-19 GKA: Systemic 2013 Pyrazine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 475.99 3.42 Hoffmann-La Roche Inc. (USA) C23H26ClN3O4S Qian, Y. et al. Identification of RO4597014, a glucokinase activator studied in the clinic for the treatment of type 2 diabetes. ACS Med. Chem. Lett. (2013) 9982406 795
GKA3-12 GKA3-12 GKA: Systemic 2006 Benzamide,Pyridine 434.48 4.68 AstraZeneca (UK) C25H26N2O5 McKerrecher, D. et al. Design of a potent, soluble glucokinase activator with excellent in vivo efficacy. Bioorganic Med. Chem. Lett. (2006) 44410908 73
GKA31-20 GKA31-20 GKA: Systemic 2013 Pyrazine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 532.05 3.08 Hoffmann-La Roche Inc. (USA) C26H30ClN3O5S Qian, Y. et al. Identification of RO4597014, a glucokinase activator studied in the clinic for the treatment of type 2 diabetes. ACS Med. Chem. Lett. (2013) 10007234 796
GKA31-21 GKA31-21 GKA: Systemic 2013 Pyrazine,Sulfoxide/Sulfone derivatives 536.08 3.54 Hoffmann-La Roche Inc. (USA) C26H34ClN3O5S Qian, Y. et al. Identification of RO4597014, a glucokinase activator studied in the clinic for the treatment of type 2 diabetes. ACS Med. Chem. Lett. (2013) 10482286 797
GKA31-22 GKA31-22 GKA: Systemic 2013 Pyrazine,Sulfoxide/Sulfone derivatives 496.02 2.46 Hoffmann-La Roche Inc. (USA) C23H30ClN3O5S Qian, Y. et al. Identification of RO4597014, a glucokinase activator studied in the clinic for the treatment of type 2 diabetes. ACS Med. Chem. Lett. (2013) 10413475 798
GKA31-23 GKA31-23 GKA: Systemic 2013 Pyrazine,Sulfoxide/Sulfone derivatives 466.94 2.46 Hoffmann-La Roche Inc. (USA) C20H23ClN4O5S Qian, Y. et al. Identification of RO4597014, a glucokinase activator studied in the clinic for the treatment of type 2 diabetes. ACS Med. Chem. Lett. (2013) 135507290 799
GKA31-24 GKA31-24 GKA: Systemic 2013 Pyrazine,Sulfoxide/Sulfone derivatives 467.97 1.84 Hoffmann-La Roche Inc. (USA) C21H26ClN3O5S Qian, Y. et al. Identification of RO4597014, a glucokinase activator studied in the clinic for the treatment of type 2 diabetes. ACS Med. Chem. Lett. (2013) 11754355 800
GKA3-13 GKA3-13 GKA: Systemic 2006 Benzamide,Pyridine 434.48 4.68 AstraZeneca (UK) C25H26N2O5 McKerrecher, D. et al. Design of a potent, soluble glucokinase activator with excellent in vivo efficacy. Bioorganic Med. Chem. Lett. (2006) 44410910 74
GKA31-4 GKA31-4 GKA: Systemic 2013 Pyrazine,Sulfoxide/Sulfone derivatives 467.97 1.84 Hoffmann-La Roche Inc. (USA) C21H26ClN3O5S Qian, Y. et al. Identification of RO4597014, a glucokinase activator studied in the clinic for the treatment of type 2 diabetes. ACS Med. Chem. Lett. (2013) 10073306 781
GKA31-6 GKA31-6 GKA: Systemic 2013 Pyrazine,Sulfoxide/Sulfone derivatives 403.5 2.69 Hoffmann-La Roche Inc. (USA) C20H25N3O4S Qian, Y. et al. Identification of RO4597014, a glucokinase activator studied in the clinic for the treatment of type 2 diabetes. ACS Med. Chem. Lett. (2013) 71625733 782
GKA31-7 GKA31-7 GKA: Systemic 2013 Pyrazine,Sulfoxide/Sulfone derivatives 423.91 1.74 Hoffmann-La Roche Inc. (USA) C19H22ClN3O4S Qian, Y. et al. Identification of RO4597014, a glucokinase activator studied in the clinic for the treatment of type 2 diabetes. ACS Med. Chem. Lett. (2013) 21958981 783
GKA31-8 GKA31-8 GKA: Systemic 2013 Pyrazine,Sulfoxide/Sulfone derivatives 409.89 1.38 Hoffmann-La Roche Inc. (USA) C18H20ClN3O4S Qian, Y. et al. Identification of RO4597014, a glucokinase activator studied in the clinic for the treatment of type 2 diabetes. ACS Med. Chem. Lett. (2013) 21959013 784
GKA31-9 GKA31-9 GKA: Systemic 2013 Pyrazine,Sulfoxide/Sulfone derivatives 454.01 4.19 Hoffmann-La Roche Inc. (USA) C20H24ClN3O3S2 Qian, Y. et al. Identification of RO4597014, a glucokinase activator studied in the clinic for the treatment of type 2 diabetes. ACS Med. Chem. Lett. (2013) 10366670 785
GKA32-10 GKA32-10 GKA: Systemic 2013 Thiazole/Thiadiazole,Urea,Quinoline/Quinazoline 392.43 2.89 Takeda California Inc. (USA) C20H16N4O3S Cheruvallath, Z. S. et al. Design, synthesis and SAR of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2013) 71579465 803
GKA32-11 GKA32-11 GKA: Systemic 2013 Thiazole/Thiadiazole,Urea,Quinoline/Quinazoline 358.41 2.62 Takeda California Inc. (USA) C17H18N4O3S Cheruvallath, Z. S. et al. Design, synthesis and SAR of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2013) 24745013 804
GKA32-12 GKA32-12 GKA: Systemic 2013 Thiazole/Thiadiazole,Urea,Sulfoxide/Sulfone derivatives,Quinoline/Quinazoline 476.57 3.26 Takeda California Inc. (USA) C21H24N4O5S2 Cheruvallath, Z. S. et al. Design, synthesis and SAR of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2013) 71579556 805
GKA32-13 GKA32-13 GKA: Systemic 2013 Thiazole/Thiadiazole,Urea,Quinoline/Quinazoline 432.92 4.65 Takeda California Inc. (USA) C20H21ClN4O3S Cheruvallath, Z. S. et al. Design, synthesis and SAR of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2013) 71579557 806
GKA32-14 GKA32-14 GKA: Systemic 2013 Thiazole/Thiadiazole,Urea,Quinoline/Quinazoline 428.5 4 Takeda California Inc. (USA) C21H24N4O4S Cheruvallath, Z. S. et al. Design, synthesis and SAR of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2013) 71579558 807
GKA32-15 GKA32-15 GKA: Systemic 2013 Thiazole/Thiadiazole,Urea,Quinoline/Quinazoline 416.47 4.13 Takeda California Inc. (USA) C20H21FN4O3S Cheruvallath, Z. S. et al. Design, synthesis and SAR of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2013) 71295772 808
GKA32-16 GKA32-16 GKA: Systemic 2013 Thiazole/Thiadiazole,Urea,Sulfoxide/Sulfone derivatives,Quinoline/Quinazoline 511.01 4.23 Takeda California Inc. (USA) C21H23ClN4O5S2 Cheruvallath, Z. S. et al. Design, synthesis and SAR of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2013) 57461474 809
GKA32-17 GKA32-17 GKA: Systemic 2013 Thiazole/Thiadiazole,Pyridone/Pyrimidone/Pyrazinone,Quinoline/Quinazoline 382.48 4.29 Takeda California Inc. (USA) C20H22N4O2S Cheruvallath, Z. S. et al. Design, synthesis and SAR of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2013) 24745328 810
GKA32-18 GKA32-18 GKA: Systemic 2013 Thiazole/Thiadiazole,Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives,Quinoline/Quinazoline 460.57 3.53 Takeda California Inc. (USA) C21H24N4O4S2 Cheruvallath, Z. S. et al. Design, synthesis and SAR of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2013) 71579559 811
GKA32-19 GKA32-19 GKA: Systemic 2013 Thiazole/Thiadiazole,Pyridone/Pyrimidone/Pyrazinone,Quinoline/Quinazoline 500.01 5.08 Takeda California Inc. (USA) C24H26ClN5O3S Cheruvallath, Z. S. et al. Design, synthesis and SAR of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2013) 57461532 812
GKA32-20 GKA32-20 GKA: Systemic 2013 Thiazole/Thiadiazole,Pyridone/Pyrimidone/Pyrazinone,Quinoline/Quinazoline 501.99 2.94 Takeda California Inc. (USA) C23H24ClN5O4S Cheruvallath, Z. S. et al. Design, synthesis and SAR of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2013) 57461541 813
GKA32-21 GKA32-21 GKA: Systemic 2013 Thiazole/Thiadiazole,Pyridone/Pyrimidone/Pyrazinone,Quinoline/Quinazoline 416.92 4.92 Takeda California Inc. (USA) C20H21ClN4O2S Cheruvallath, Z. S. et al. Design, synthesis and SAR of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2013) 24745820 814
GKA32-22 GKA32-22 GKA: Systemic 2013 Thiazole/Thiadiazole,Pyridone/Pyrimidone/Pyrazinone,Quinoline/Quinazoline 400.47 4.39 Takeda California Inc. (USA) C20H21FN4O2S Cheruvallath, Z. S. et al. Design, synthesis and SAR of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2013) 71295771 815
GKA32-23 GKA32-23 GKA: Systemic 2013 Thiazole/Thiadiazole,Pyridone/Pyrimidone/Pyrazinone,Quinoline/Quinazoline 396.51 4.65 Takeda California Inc. (USA) C21H24N4O2S Cheruvallath, Z. S. et al. Design, synthesis and SAR of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2013) 71579644 816
GKA32-24 GKA32-24 GKA: Systemic 2013 Thiazole/Thiadiazole,Pyridone/Pyrimidone/Pyrazinone,Quinoline/Quinazoline 473.98 4.53 Takeda California Inc. (USA) C22H24ClN5O3S Cheruvallath, Z. S. et al. Design, synthesis and SAR of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2013) 71579645 817
GKA32-25 GKA32-25 GKA: Systemic 2013 Thiazole/Thiadiazole,Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives,Quinoline/Quinazoline 532.65 5.23 Takeda California Inc. (USA) C25H29FN4O4S2 Cheruvallath, Z. S. et al. Design, synthesis and SAR of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2013) 71579646 818
GKA32-26 GKA32-26 GKA: Systemic 2013 Thiazole/Thiadiazole,Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives,Quinoline/Quinazoline 549.11 5.75 Takeda California Inc. (USA) C25H29ClN4O4S2 Cheruvallath, Z. S. et al. Design, synthesis and SAR of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2013) 71579738 819
GKA32-27 GKA32-27 GKA: Systemic 2013 Thiazole/Thiadiazole,Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives,Quinoline/Quinazoline 492.59 4.33 Takeda California Inc. (USA) C22H25FN4O4S2 Cheruvallath, Z. S. et al. Design, synthesis and SAR of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2013) 71579739 820
GKA32-28 GKA32-28 GKA: Systemic 2013 Thiazole/Thiadiazole,Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives,Quinoline/Quinazoline 494.56 2.18 Takeda California Inc. (USA) C21H23FN4O5S2 Cheruvallath, Z. S. et al. Design, synthesis and SAR of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2013) 821
GKA32-29 GKA32-29 GKA: Systemic 2013 Thiazole/Thiadiazole,Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives,Quinoline/Quinazoline 472.58 3.54 Takeda California Inc. (USA) C22H24N4O4S2 Cheruvallath, Z. S. et al. Design, synthesis and SAR of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2013) 71579741 822
GKA32-30 GKA32-30 GKA: Systemic 2013 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 414.54 2.21 Takeda California Inc. (USA) C17H26N4O4S2 Cheruvallath, Z. S. et al. Design, synthesis and SAR of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2013) 71295773 823
GKA32-31 GKA32-31 GKA: Systemic 2013 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 440.58 2.77 Takeda California Inc. (USA) C19H28N4O4S2 Cheruvallath, Z. S. et al. Design, synthesis and SAR of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2013) 57657369 824
GKA32-32 GKA32-32 GKA: Systemic 2013 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 468.63 3.48 Takeda California Inc. (USA) C21H32N4O4S2 Cheruvallath, Z. S. et al. Design, synthesis and SAR of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2013) 57657324 825
GKA32-33 GKA32-33 GKA: Systemic 2013 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 477 1.59 Takeda California Inc. (USA) C18H25ClN4O5S2 Cheruvallath, Z. S. et al. Design, synthesis and SAR of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2013) 25073991 826
GKA32-34 GKA32-34 GKA: Systemic 2013 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 450.96 1.03 Takeda California Inc. (USA) C16H23ClN4O5S2 Cheruvallath, Z. S. et al. Design, synthesis and SAR of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2013) 827
GKA32-35 GKA32-35 GKA: Systemic 2013 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 511.06 4.4 Takeda California Inc. (USA) C22H27ClN4O4S2 Cheruvallath, Z. S. et al. Design, synthesis and SAR of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2013) 25071203 828
GKA32-36 GKA32-36 GKA: Systemic 2013 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 512.59 3.97 Takeda California Inc. (USA) C22H26F2N4O4S2 Cheruvallath, Z. S. et al. Design, synthesis and SAR of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2013) 57657277 829
GKA32-37 GKA32-37 GKA: Systemic 2013 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 490.64 4.14 Takeda California Inc. (USA) C23H30N4O4S2 Cheruvallath, Z. S. et al. Design, synthesis and SAR of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2013) 25073999 830
GKA32-38 GKA32-38 GKA: Systemic 2013 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 508.63 4.24 Takeda California Inc. (USA) C23H29FN4O4S2 Cheruvallath, Z. S. et al. Design, synthesis and SAR of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2013) 25072138 831
GKA32-39 GKA32-39 GKA: Systemic 2013 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 466.57 3.17 Takeda California Inc. (USA) C20H26N4O5S2 Cheruvallath, Z. S. et al. Design, synthesis and SAR of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2013) 71579836 832
GKA32-40 GKA32-40 GKA: Systemic 2013 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 480.6 2.42 Takeda California Inc. (USA) C20H28N6O4S2 Cheruvallath, Z. S. et al. Design, synthesis and SAR of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2013) 57657364 833
GKA32-41 GKA32-41 GKA: Systemic 2013 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 490.64 3.71 Takeda California Inc. (USA) C23H30N4O4S2 Cheruvallath, Z. S. et al. Design, synthesis and SAR of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2013) 25069589 834
GKA32-42 GKA32-42 GKA: Systemic 2013 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 442.6 3.01 Takeda California Inc. (USA) C19H30N4O4S2 Cheruvallath, Z. S. et al. Design, synthesis and SAR of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2013) 25070876 835
GKA32-43 GKA32-43 GKA: Systemic 2013 Thiazole/Thiadiazole,Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 423.55 3.12 Takeda California Inc. (USA) C19H25N3O4S2 Cheruvallath, Z. S. et al. Design, synthesis and SAR of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2013) 57665301 836
GKA32-44 GKA32-44 GKA: Systemic 2013 Thiazole/Thiadiazole,Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 437.58 3.48 Takeda California Inc. (USA) C20H27N3O4S2 Cheruvallath, Z. S. et al. Design, synthesis and SAR of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2013) 71579931 837
GKA32-45 GKA32-45 GKA: Systemic 2013 Thiazole/Thiadiazole,Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 477.64 4.39 Takeda California Inc. (USA) C23H31N3O4S2 Cheruvallath, Z. S. et al. Design, synthesis and SAR of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2013) 71579932 838
GKA32-46 GKA32-46 GKA: Systemic 2013 Thiazole/Thiadiazole,Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 437.58 2.98 Takeda California Inc. (USA) C20H27N3O4S2 Cheruvallath, Z. S. et al. Design, synthesis and SAR of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2013) 57665307 839
GKA32-47 GKA32-47 GKA: Systemic 2013 Thiazole/Thiadiazole,Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 435.56 2.76 Takeda California Inc. (USA) C20H25N3O4S2 Cheruvallath, Z. S. et al. Design, synthesis and SAR of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2013) 24962524 840
GKA32-48 GKA32-48 GKA: Systemic 2013 Thiazole/Thiadiazole,Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 463.61 3.84 Takeda California Inc. (USA) C22H29N3O4S2 Cheruvallath, Z. S. et al. Design, synthesis and SAR of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2013) 24962881 841
GKA32-49 GKA32-49 GKA: Systemic 2013 Thiazole/Thiadiazole,Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 479.61 2.25 Takeda California Inc. (USA) C22H29N3O5S2 Cheruvallath, Z. S. et al. Design, synthesis and SAR of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2013) 87647241 842
GKA32-50 GKA32-50 GKA: Systemic 2013 Thiazole/Thiadiazole,Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 437.58 3.08 Takeda California Inc. (USA) C20H27N3O4S2 Cheruvallath, Z. S. et al. Design, synthesis and SAR of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2013) 24962885 843
GKA32-51 GKA32-51 GKA: Systemic 2013 Thiazole/Thiadiazole,Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 514.06 3.21 Takeda California Inc. (USA) C22H28ClN3O5S2 Cheruvallath, Z. S. et al. Design, synthesis and SAR of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2013) 24957755 844
GKA32-52 GKA32-52 GKA: Systemic 2013 Thiazole/Thiadiazole,Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 497.6 2.68 Takeda California Inc. (USA) C22H28FN3O5S2 Cheruvallath, Z. S. et al. Design, synthesis and SAR of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2013) 24957382 845
GKA32-53 GKA32-53 GKA: Systemic 2013 Thiazole/Thiadiazole,Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 453.55 3.56 Takeda California Inc. (USA) C20H24FN3O4S2 Cheruvallath, Z. S. et al. Design, synthesis and SAR of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2013) 57665404 846
GKA32-54 GKA32-54 GKA: Systemic 2013 Thiazole/Thiadiazole,Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 486 2.49 Takeda California Inc. (USA) C20H24ClN3O5S2 Cheruvallath, Z. S. et al. Design, synthesis and SAR of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2013) 57665304 847
GKA32-55 GKA32-55 GKA: Systemic 2013 Thiazole/Thiadiazole,Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 470.01 4.09 Takeda California Inc. (USA) C20H24ClN3O4S2 Cheruvallath, Z. S. et al. Design, synthesis and SAR of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2013) 57665343 848
GKA32-8 GKA32-8 (racemic) GKA: Systemic 2013 Thiazole/Thiadiazole,Urea,Quinoline/Quinazoline 358.41 2.62 Takeda California Inc. (USA) C17H18N4O3S Cheruvallath, Z. S. et al. Design, synthesis and SAR of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2013) 24745013 801
GKA32-9 GKA32-9 GKA: Systemic 2013 Thiazole/Thiadiazole,Urea,Quinoline/Quinazoline 398.48 4.03 Takeda California Inc. (USA) C20H22N4O3S Cheruvallath, Z. S. et al. Design, synthesis and SAR of novel glucokinase activators. Bioorganic Med. Chem. Lett. (2013) 71579464 802
GKA33-17 GKA33-17 GKA: Systemic 2013 Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 400.45 2.46 Pfizer Global Research & Development (USA) C20H20N2O5S Filipski, K. J. et al. Pyrimidone-based series of glucokinase activators with alternative donor-acceptor motif. Bioorganic Med. Chem. Lett. (2013) 71813504 852
GKA33-2 GKA33-2 GKA: Systemic 2013 Pyridone/Pyrimidone/Pyrazinone 283.35 2.34 Pfizer Global Research & Development (USA) C15H13N3OS Filipski, K. J. et al. Pyrimidone-based series of glucokinase activators with alternative donor-acceptor motif. Bioorganic Med. Chem. Lett. (2013) 71627422 849
GKA33-21 GKA33-21 GKA: Systemic 2013 Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 400.45 2.46 Pfizer Global Research & Development (USA) C20H20N2O5S Filipski, K. J. et al. Pyrimidone-based series of glucokinase activators with alternative donor-acceptor motif. Bioorganic Med. Chem. Lett. (2013) 71813669 853
GKA33-25 GKA33-25 GKA: Systemic 2013 Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 400.45 2.47 Pfizer Global Research & Development (USA) C20H20N2O5S Filipski, K. J. et al. Pyrimidone-based series of glucokinase activators with alternative donor-acceptor motif. Bioorganic Med. Chem. Lett. (2013) 54767117 854
GKA33-26 GKA33-26 GKA: Systemic 2013 Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 414.47 2.84 Pfizer Global Research & Development (USA) C21H22N2O5S Filipski, K. J. et al. Pyrimidone-based series of glucokinase activators with alternative donor-acceptor motif. Bioorganic Med. Chem. Lett. (2013) 54767116 855
GKA33-27 GKA33-27 GKA: Systemic 2013 Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 414.47 2.84 Pfizer Global Research & Development (USA) C21H22N2O5S Filipski, K. J. et al. Pyrimidone-based series of glucokinase activators with alternative donor-acceptor motif. Bioorganic Med. Chem. Lett. (2013) 136239454 856
GKA33-3 GKA33-3 GKA: Systemic 2013 Benzamide,Pyridine,Sulfoxide/Sulfone derivatives 440.51 3.92 Pfizer Global Research & Development (USA) C23H24N2O5S Filipski, K. J. et al. Pyrimidone-based series of glucokinase activators with alternative donor-acceptor motif. Bioorganic Med. Chem. Lett. (2013) 73350645 850
GKA33-30 GKA33-30 GKA: Systemic 2013 Pyrimidine,Pyridone/Pyrimidone/Pyrazinone 395.41 1.31 Pfizer Global Research & Development (USA) C20H21N5O4 Filipski, K. J. et al. Pyrimidone-based series of glucokinase activators with alternative donor-acceptor motif. Bioorganic Med. Chem. Lett. (2013) 54767610 857
GKA33-36 GKA33-36 GKA: Systemic 2013 Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 430.47 1.79 Pfizer Global Research & Development (USA) C21H22N2O6S Filipski, K. J. et al. Pyrimidone-based series of glucokinase activators with alternative donor-acceptor motif. Bioorganic Med. Chem. Lett. (2013) 54767447 858
GKA33-37 GKA33-37 GKA: Systemic 2013 Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 428.5 3.28 Pfizer Global Research & Development (USA) C22H24N2O5S Filipski, K. J. et al. Pyrimidone-based series of glucokinase activators with alternative donor-acceptor motif. Bioorganic Med. Chem. Lett. (2013) 54767118 859
GKA33-38 GKA33-38 GKA: Systemic 2013 Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 442.53 3.61 Pfizer Global Research & Development (USA) C23H26N2O5S Filipski, K. J. et al. Pyrimidone-based series of glucokinase activators with alternative donor-acceptor motif. Bioorganic Med. Chem. Lett. (2013) 54766044 860
GKA33-39 GKA33-39 GKA: Systemic 2013 Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 430.47 2.65 Pfizer Global Research & Development (USA) C21H22N2O6S Filipski, K. J. et al. Pyrimidone-based series of glucokinase activators with alternative donor-acceptor motif. Bioorganic Med. Chem. Lett. (2013) 54767120 861
GKA33-4 GKA33-4 GKA: Systemic 2013 Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 399.46 3.38 Pfizer Global Research & Development (USA) C21H21NO5S Filipski, K. J. et al. Pyrimidone-based series of glucokinase activators with alternative donor-acceptor motif. Bioorganic Med. Chem. Lett. (2013) 71813336 851
GKA33-40 GKA33-40 GKA: Systemic 2013 Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 434.89 3.31 Pfizer Global Research & Development (USA) C20H19ClN2O5S Filipski, K. J. et al. Pyrimidone-based series of glucokinase activators with alternative donor-acceptor motif. Bioorganic Med. Chem. Lett. (2013) 54767119 862
GKA33-41 GKA33-41 GKA: Systemic 2013 Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 425.46 2.4 Pfizer Global Research & Development (USA) C21H19N3O5S Filipski, K. J. et al. Pyrimidone-based series of glucokinase activators with alternative donor-acceptor motif. Bioorganic Med. Chem. Lett. (2013) 67996937 863
GKA33-42 GKA33-42 GKA: Systemic 2013 Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 415.46 2.2 Pfizer Global Research & Development (USA) C20H21N3O5S Filipski, K. J. et al. Pyrimidone-based series of glucokinase activators with alternative donor-acceptor motif. Bioorganic Med. Chem. Lett. (2013) 54767784 864
GKA33-43 GKA33-43 GKA: Systemic 2013 Pyridine,Pyridone/Pyrimidone/Pyrazinone 412.41 2.06 Pfizer Global Research & Development (USA) C21H21FN4O4 Filipski, K. J. et al. Pyrimidone-based series of glucokinase activators with alternative donor-acceptor motif. Bioorganic Med. Chem. Lett. (2013) 54767786 865
GKA33-44 GKA33-44 GKA: Systemic 2013 Pyrazine,Pyridone/Pyrimidone/Pyrazinone 395.41 1.22 Pfizer Global Research & Development (USA) C20H21N5O4 Filipski, K. J. et al. Pyrimidone-based series of glucokinase activators with alternative donor-acceptor motif. Bioorganic Med. Chem. Lett. (2013) 54767782 866
GKA33-45 GKA33-45 GKA: Systemic 2013 Pyrimidine,Pyridone/Pyrimidone/Pyrazinone 423.47 2.36 Pfizer Global Research & Development (USA) C22H25N5O4 Filipski, K. J. et al. Pyrimidone-based series of glucokinase activators with alternative donor-acceptor motif. Bioorganic Med. Chem. Lett. (2013) 54766500 867
GKA33-46 GKA33-46 GKA: Systemic 2013 Pyrimidine,Pyridone/Pyrimidone/Pyrazinone 421.45 1.78 Pfizer Global Research & Development (USA) C22H23N5O4 Filipski, K. J. et al. Pyrimidone-based series of glucokinase activators with alternative donor-acceptor motif. Bioorganic Med. Chem. Lett. (2013) 54766199 868
GKA33-47 GKA33-47 GKA: Systemic 2013 Pyrimidine,Pyridone/Pyrimidone/Pyrazinone 411.41 0.26 Pfizer Global Research & Development (USA) C20H21N5O5 Filipski, K. J. et al. Pyrimidone-based series of glucokinase activators with alternative donor-acceptor motif. Bioorganic Med. Chem. Lett. (2013) 54765880 869
GKA33-48 GKA33-48 GKA: Systemic 2013 Pyrimidine,Pyridone/Pyrimidone/Pyrazinone 425.44 0.79 Pfizer Global Research & Development (USA) C21H23N5O5 Filipski, K. J. et al. Pyrimidone-based series of glucokinase activators with alternative donor-acceptor motif. Bioorganic Med. Chem. Lett. (2013) 54766497 870
GKA33-49 GKA33-49 GKA: Systemic 2013 Pyrimidine,Pyridone/Pyrimidone/Pyrazinone 423.42 0.56 Pfizer Global Research & Development (USA) C21H21N5O5 Filipski, K. J. et al. Pyrimidone-based series of glucokinase activators with alternative donor-acceptor motif. Bioorganic Med. Chem. Lett. (2013) 67996575 871
GKA33-50 GKA33-50 GKA: Systemic 2013 Pyrimidine,Pyridone/Pyrimidone/Pyrazinone 450.45 0.2 Pfizer Global Research & Development (USA) C22H22N6O5 Filipski, K. J. et al. Pyrimidone-based series of glucokinase activators with alternative donor-acceptor motif. Bioorganic Med. Chem. Lett. (2013) 71814304 872
GKA33-51 GKA33-51 GKA: Systemic 2013 Pyrimidine,Pyridone/Pyrimidone/Pyrazinone 409.44 1.68 Pfizer Global Research & Development (USA) C21H23N5O4 Filipski, K. J. et al. Pyrimidone-based series of glucokinase activators with alternative donor-acceptor motif. Bioorganic Med. Chem. Lett. (2013) 54767787 873
GKA33-52 GKA33-52 GKA: Systemic 2013 Pyrazine,Pyridone/Pyrimidone/Pyrazinone 425.44 0.71 Pfizer Global Research & Development (USA) C21H23N5O5 Filipski, K. J. et al. Pyrimidone-based series of glucokinase activators with alternative donor-acceptor motif. Bioorganic Med. Chem. Lett. (2013) 54766195 874
GKA33-53 GKA33-53 GKA: Systemic 2013 Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 459.52 1.7 Pfizer Global Research & Development (USA) C22H25N3O6S Filipski, K. J. et al. Pyrimidone-based series of glucokinase activators with alternative donor-acceptor motif. Bioorganic Med. Chem. Lett. (2013) 54765712 875
GKA33-54 GKA33-54 GKA: Systemic 2013 Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 445.49 1.52 Pfizer Global Research & Development (USA) C21H23N3O6S Filipski, K. J. et al. Pyrimidone-based series of glucokinase activators with alternative donor-acceptor motif. Bioorganic Med. Chem. Lett. (2013) 54765716 876
GKA34-1 GKA34-1 GKA: Systemic 2013 Thiazole/Thiadiazole,Pyridine 297.37 3.96 Array BioPharma (USA) C16H15N3OS Hinklin, R. J. et al. Identification of a new class of glucokinase activators through structure-based design. J. Med. Chem. (2013) 16660015 877
GKA34-10 GKA34-10 GKA: Systemic 2013 Thiazole/Thiadiazole,Pyridine,Quinoline/Quinazoline 348.42 4.23 Array BioPharma (USA) C19H16N4OS Hinklin, R. J. et al. Identification of a new class of glucokinase activators through structure-based design. J. Med. Chem. (2013) 16660167 882
GKA34-13 GKA34-13 GKA: Systemic 2013 Thiazole/Thiadiazole,Pyridine 376.27 4.65 Array BioPharma (USA) C16H14BrN3OS Hinklin, R. J. et al. Identification of a new class of glucokinase activators through structure-based design. J. Med. Chem. (2013) 16061466 883
GKA34-14 GKA34-14 GKA: Systemic 2013 Thiazole/Thiadiazole,Pyridine 390.3 5.08 Array BioPharma (USA) C17H16BrN3OS Hinklin, R. J. et al. Identification of a new class of glucokinase activators through structure-based design. J. Med. Chem. (2013) 72705641 884
GKA34-15 GKA34-15 GKA: Systemic 2013 Thiazole/Thiadiazole,Pyridine 404.32 5.41 Array BioPharma (USA) C18H18BrN3OS Hinklin, R. J. et al. Identification of a new class of glucokinase activators through structure-based design. J. Med. Chem. (2013) 16660845 885
GKA34-16 GKA34-16 GKA: Systemic 2013 Thiazole/Thiadiazole,Pyridine 418.35 5.87 Array BioPharma (USA) C19H20BrN3OS Hinklin, R. J. et al. Identification of a new class of glucokinase activators through structure-based design. J. Med. Chem. (2013) 16660844 886
GKA34-17 GKA34-17 GKA: Systemic 2013 Thiazole/Thiadiazole,Pyridine 311.4 4.32 Array BioPharma (USA) C17H17N3OS Hinklin, R. J. et al. Identification of a new class of glucokinase activators through structure-based design. J. Med. Chem. (2013) 59225669 887
GKA34-18 GKA34-18 GKA: Systemic 2013 Thiazole/Thiadiazole,Pyridine 331.82 4.59 Array BioPharma (USA) C16H14ClN3OS Hinklin, R. J. et al. Identification of a new class of glucokinase activators through structure-based design. J. Med. Chem. (2013) 16660170 888
GKA34-19 GKA34-19 GKA: Systemic 2013 Thiazole/Thiadiazole,Pyridine 405.54 6.03 Array BioPharma (USA) C22H19N3OS2 Hinklin, R. J. et al. Identification of a new class of glucokinase activators through structure-based design. J. Med. Chem. (2013) 59225645 889
GKA34-20 GKA34-20 GKA: Systemic 2013 Thiazole/Thiadiazole,Pyridine 406.52 5.29 Array BioPharma (USA) C21H18N4OS2 Hinklin, R. J. et al. Identification of a new class of glucokinase activators through structure-based design. J. Med. Chem. (2013) 16660671 890
GKA34-21 GKA34-21 GKA: Systemic 2013 Thiazole/Thiadiazole,Pyridine 419.56 5.96 Array BioPharma (USA) C23H21N3OS2 Hinklin, R. J. et al. Identification of a new class of glucokinase activators through structure-based design. J. Med. Chem. (2013) 16660174 891
GKA34-24 GKA34-24 GKA: Systemic 2013 Thiazole/Thiadiazole,Pyridine 420.55 4.93 Array BioPharma (USA) C22H20N4OS2 Hinklin, R. J. et al. Identification of a new class of glucokinase activators through structure-based design. J. Med. Chem. (2013) 16660507 892
GKA34-25 GKA34-25 GKA: Systemic 2013 Thiazole/Thiadiazole,Pyridine 423.55 4.19 Array BioPharma (USA) C21H21N5OS2 Hinklin, R. J. et al. Identification of a new class of glucokinase activators through structure-based design. J. Med. Chem. (2013) 59225642 893
GKA34-26 GKA34-26 GKA: Systemic 2013 Thiazole/Thiadiazole,Pyridine 451.61 4.95 Array BioPharma (USA) C23H25N5OS2 Hinklin, R. J. et al. Identification of a new class of glucokinase activators through structure-based design. J. Med. Chem. (2013) 72703061 894
GKA34-6 GKA34-6 GKA: Systemic 2013 Thiazole/Thiadiazole,Pyridine 327.4 3.93 Array BioPharma (USA) C17H17N3O2S Hinklin, R. J. et al. Identification of a new class of glucokinase activators through structure-based design. J. Med. Chem. (2013) 16660168 878
GKA34-7 GKA34-7 GKA: Systemic 2013 Thiazole/Thiadiazole,Pyridine 298.36 2.92 Array BioPharma (USA) C15H14N4OS Hinklin, R. J. et al. Identification of a new class of glucokinase activators through structure-based design. J. Med. Chem. (2013) 16660016 879
GKA34-8 GKA34-8 GKA: Systemic 2013 Thiazole/Thiadiazole,Pyridine 298.36 2.89 Array BioPharma (USA) C15H14N4OS Hinklin, R. J. et al. Identification of a new class of glucokinase activators through structure-based design. J. Med. Chem. (2013) 16660017 880
GKA34-9 GKA34-9 GKA: Systemic 2013 Thiazole/Thiadiazole,Pyridine 313.37 3.6 Array BioPharma (USA) C16H15N3O2S Hinklin, R. J. et al. Identification of a new class of glucokinase activators through structure-based design. J. Med. Chem. (2013) 16660331 881
GKA35-16a GKA35-16a GKA: Systemic 2013 Benzamide 462.49 4.04 Yuhan Research Institute (SOUTH KOREA) C26H26N2O6 Park, K. et al. Discovery of a novel phenylethyl benzamide glucokinase activator for the treatment of type 2 diabetes mellitus. Bioorganic Med. Chem. Lett. (2013) 71540966 895
GKA35-16b GKA35-16b GKA: Systemic 2013 Benzamide 486.44 4.37 Yuhan Research Institute (SOUTH KOREA) C25H21F3N2O5 Park, K. et al. Discovery of a novel phenylethyl benzamide glucokinase activator for the treatment of type 2 diabetes mellitus. Bioorganic Med. Chem. Lett. (2013) 71540965 896
GKA35-16c GKA35-16c GKA: Systemic 2013 Benzamide 468.45 4.27 Yuhan Research Institute (SOUTH KOREA) C25H22F2N2O5 Park, K. et al. Discovery of a novel phenylethyl benzamide glucokinase activator for the treatment of type 2 diabetes mellitus. Bioorganic Med. Chem. Lett. (2013) 71540964 897
GKA35-16d GKA35-16d GKA: Systemic 2013 Benzamide 468.45 4.27 Yuhan Research Institute (SOUTH KOREA) C25H22F2N2O5 Park, K. et al. Discovery of a novel phenylethyl benzamide glucokinase activator for the treatment of type 2 diabetes mellitus. Bioorganic Med. Chem. Lett. (2013) 71540963 898
GKA35-16e GKA35-16e GKA: Systemic 2013 Benzamide 468.45 4.27 Yuhan Research Institute (SOUTH KOREA) C25H22F2N2O5 Park, K. et al. Discovery of a novel phenylethyl benzamide glucokinase activator for the treatment of type 2 diabetes mellitus. Bioorganic Med. Chem. Lett. (2013) 71540962 899
GKA35-16f GKA35-16f GKA: Systemic 2013 Benzamide 450.46 4.17 Yuhan Research Institute (SOUTH KOREA) C25H23FN2O5 Park, K. et al. Discovery of a novel phenylethyl benzamide glucokinase activator for the treatment of type 2 diabetes mellitus. Bioorganic Med. Chem. Lett. (2013) 78104324 900
GKA35-16g GKA35-16g GKA: Systemic 2013 Benzamide 450.46 4.17 Yuhan Research Institute (SOUTH KOREA) C25H23FN2O5 Park, K. et al. Discovery of a novel phenylethyl benzamide glucokinase activator for the treatment of type 2 diabetes mellitus. Bioorganic Med. Chem. Lett. (2013) 71540844 901
GKA35-16h GKA35-16h GKA: Systemic 2013 Benzamide 477.47 3.9 Yuhan Research Institute (SOUTH KOREA) C25H23N3O7 Park, K. et al. Discovery of a novel phenylethyl benzamide glucokinase activator for the treatment of type 2 diabetes mellitus. Bioorganic Med. Chem. Lett. (2013) 71540843 902
GKA35-16i GKA35-16i GKA: Systemic 2013 Benzamide 477.47 3.9 Yuhan Research Institute (SOUTH KOREA) C25H23N3O7 Park, K. et al. Discovery of a novel phenylethyl benzamide glucokinase activator for the treatment of type 2 diabetes mellitus. Bioorganic Med. Chem. Lett. (2013) 71540842 903
GKA35-16j GKA35-16j GKA: Systemic 2013 Benzamide 477.47 3.9 Yuhan Research Institute (SOUTH KOREA) C25H23N3O7 Park, K. et al. Discovery of a novel phenylethyl benzamide glucokinase activator for the treatment of type 2 diabetes mellitus. Bioorganic Med. Chem. Lett. (2013) 71540841 904
GKA35-16k GKA35-16k GKA: Systemic 2013 Benzamide,Pyridine 423.5 3.85 Yuhan Research Institute (SOUTH KOREA) C24H29N3O4 Park, K. et al. Discovery of a novel phenylethyl benzamide glucokinase activator for the treatment of type 2 diabetes mellitus. Bioorganic Med. Chem. Lett. (2013) 67305655 905
GKA35-16l GKA35-16l GKA: Systemic 2013 Benzamide 447.45 4.18 Yuhan Research Institute (SOUTH KOREA) C23H24F3N3O3 Park, K. et al. Discovery of a novel phenylethyl benzamide glucokinase activator for the treatment of type 2 diabetes mellitus. Bioorganic Med. Chem. Lett. (2013) 78104287 906
GKA35-16m GKA35-16m GKA: Systemic 2013 Benzamide 429.46 4.08 Yuhan Research Institute (SOUTH KOREA) C23H25F2N3O3 Park, K. et al. Discovery of a novel phenylethyl benzamide glucokinase activator for the treatment of type 2 diabetes mellitus. Bioorganic Med. Chem. Lett. (2013) 71540726 907
GKA35-16n GKA35-16n GKA: Systemic 2013 Benzamide 429.46 4.08 Yuhan Research Institute (SOUTH KOREA) C23H25F2N3O3 Park, K. et al. Discovery of a novel phenylethyl benzamide glucokinase activator for the treatment of type 2 diabetes mellitus. Bioorganic Med. Chem. Lett. (2013) 67306982 908
GKA35-16o GKA35-16o GKA: Systemic 2013 Benzamide 411.47 3.97 Yuhan Research Institute (SOUTH KOREA) C23H26FN3O3 Park, K. et al. Discovery of a novel phenylethyl benzamide glucokinase activator for the treatment of type 2 diabetes mellitus. Bioorganic Med. Chem. Lett. (2013) 67305810 909
GKA35-16p GKA35-16p GKA: Systemic 2013 Benzamide 411.47 3.97 Yuhan Research Institute (SOUTH KOREA) C23H26FN3O3 Park, K. et al. Discovery of a novel phenylethyl benzamide glucokinase activator for the treatment of type 2 diabetes mellitus. Bioorganic Med. Chem. Lett. (2013) 67307127 910
GKA35-16q GKA35-16q GKA: Systemic 2013 Benzamide 406.48 3.29 Yuhan Research Institute (SOUTH KOREA) C23H26N4O3 Park, K. et al. Discovery of a novel phenylethyl benzamide glucokinase activator for the treatment of type 2 diabetes mellitus. Bioorganic Med. Chem. Lett. (2013) 71540615 911
GKA35-20a GKA35-20a GKA: Systemic 2013 Benzamide,Pyridine 421.49 3.9 Yuhan Research Institute (SOUTH KOREA) C24H27N3O4 Park, K. et al. Discovery of a novel phenylethyl benzamide glucokinase activator for the treatment of type 2 diabetes mellitus. Bioorganic Med. Chem. Lett. (2013) 71540614 912
GKA35-20b GKA35-20b GKA: Systemic 2013 Benzamide,Pyridine 445.43 4.23 Yuhan Research Institute (SOUTH KOREA) C23H22F3N3O3 Park, K. et al. Discovery of a novel phenylethyl benzamide glucokinase activator for the treatment of type 2 diabetes mellitus. Bioorganic Med. Chem. Lett. (2013) 71540613 913
GKA35-20c GKA35-20c GKA: Systemic 2013 Benzamide,Pyridine 427.44 4.13 Yuhan Research Institute (SOUTH KOREA) C23H23F2N3O3 Park, K. et al. Discovery of a novel phenylethyl benzamide glucokinase activator for the treatment of type 2 diabetes mellitus. Bioorganic Med. Chem. Lett. (2013) 71540612 914
GKA35-20d GKA35-20d GKA: Systemic 2013 Benzamide,Pyridine 427.44 4.13 Yuhan Research Institute (SOUTH KOREA) C23H23F2N3O3 Park, K. et al. Discovery of a novel phenylethyl benzamide glucokinase activator for the treatment of type 2 diabetes mellitus. Bioorganic Med. Chem. Lett. (2013) 71540611 915
GKA35-20e GKA35-20e GKA: Systemic 2013 Benzamide,Pyridine 427.44 4.13 Yuhan Research Institute (SOUTH KOREA) C23H23F2N3O3 Park, K. et al. Discovery of a novel phenylethyl benzamide glucokinase activator for the treatment of type 2 diabetes mellitus. Bioorganic Med. Chem. Lett. (2013) 71540610 916
GKA35-20f GKA35-20f GKA: Systemic 2013 Benzamide,Pyridine 409.45 4.03 Yuhan Research Institute (SOUTH KOREA) C23H24FN3O3 Park, K. et al. Discovery of a novel phenylethyl benzamide glucokinase activator for the treatment of type 2 diabetes mellitus. Bioorganic Med. Chem. Lett. (2013) 71540511 917
GKA35-20g GKA35-20g GKA: Systemic 2013 Benzamide,Pyridine 409.45 4.03 Yuhan Research Institute (SOUTH KOREA) C23H24FN3O3 Park, K. et al. Discovery of a novel phenylethyl benzamide glucokinase activator for the treatment of type 2 diabetes mellitus. Bioorganic Med. Chem. Lett. (2013) 71540510 918
GKA35-20h GKA35-20h GKA: Systemic 2013 Benzamide,Pyridine 436.46 3.76 Yuhan Research Institute (SOUTH KOREA) C23H24N4O5 Park, K. et al. Discovery of a novel phenylethyl benzamide glucokinase activator for the treatment of type 2 diabetes mellitus. Bioorganic Med. Chem. Lett. (2013) 71540509 919
GKA35-20i GKA35-20i GKA: Systemic 2013 Benzamide,Pyridine 436.46 3.76 Yuhan Research Institute (SOUTH KOREA) C23H24N4O5 Park, K. et al. Discovery of a novel phenylethyl benzamide glucokinase activator for the treatment of type 2 diabetes mellitus. Bioorganic Med. Chem. Lett. (2013) 71540508 920
GKA35-20j GKA35-20j GKA: Systemic 2013 Benzamide,Pyridine 436.46 3.76 Yuhan Research Institute (SOUTH KOREA) C23H24N4O5 Park, K. et al. Discovery of a novel phenylethyl benzamide glucokinase activator for the treatment of type 2 diabetes mellitus. Bioorganic Med. Chem. Lett. (2013) 71540507 921
GKA36-1 GKA36-1 GKA: Systemic 2014 Urea,Pyridine 328.41 3.07 Amgen Inc. & Array BioPharma (USA) C18H24N4O2 Du, X. et al. C5-Alkyl-2-methylurea-substituted pyridines as a new class of glucokinase activators. ACS Med. Chem. Lett. (2014) 118722859 922
GKA36-10 GKA36-10 GKA: Systemic 2014 Urea,Pyridine 347.41 1.49 Amgen Inc. & Array BioPharma (USA) C17H25N5O3 Du, X. et al. C5-Alkyl-2-methylurea-substituted pyridines as a new class of glucokinase activators. ACS Med. Chem. Lett. (2014) 118722868 931
GKA36-11 GKA36-11 GKA: Systemic 2014 Urea,Pyridine 361.44 1.57 Amgen Inc. & Array BioPharma (USA) C18H27N5O3 Du, X. et al. C5-Alkyl-2-methylurea-substituted pyridines as a new class of glucokinase activators. ACS Med. Chem. Lett. (2014) 118722869 932
GKA36-12 GKA36-12 GKA: Systemic 2014 Urea,Pyridine 359.42 1.52 Amgen Inc. & Array BioPharma (USA) C18H25N5O3 Du, X. et al. C5-Alkyl-2-methylurea-substituted pyridines as a new class of glucokinase activators. ACS Med. Chem. Lett. (2014) 71603584 933
GKA36-13 GKA36-13 GKA: Systemic 2014 Urea,Pyridine 375.42 0.41 Amgen Inc. & Array BioPharma (USA) C18H25N5O4 Du, X. et al. C5-Alkyl-2-methylurea-substituted pyridines as a new class of glucokinase activators. ACS Med. Chem. Lett. (2014) 118722870 934
GKA36-14 GKA36-14 GKA: Systemic 2014 Urea,Pyridine 360.41 0.13 Amgen Inc. & Array BioPharma (USA) C17H24N6O3 Du, X. et al. C5-Alkyl-2-methylurea-substituted pyridines as a new class of glucokinase activators. ACS Med. Chem. Lett. (2014) 118722871 935
GKA36-15 GKA36-15 GKA: Systemic 2014 Urea,Pyridine 403.48 1.44 Amgen Inc. & Array BioPharma (USA) C20H29N5O4 Du, X. et al. C5-Alkyl-2-methylurea-substituted pyridines as a new class of glucokinase activators. ACS Med. Chem. Lett. (2014) 118722872 936
GKA36-16 GKA36-16 GKA: Systemic 2014 Urea,Pyridine 403.48 1.44 Amgen Inc. & Array BioPharma (USA) C20H29N5O4 Du, X. et al. C5-Alkyl-2-methylurea-substituted pyridines as a new class of glucokinase activators. ACS Med. Chem. Lett. (2014) 118722873 937
GKA36-17 GKA36-17 GKA: Systemic 2014 Urea,Pyridine 373.45 1.92 Amgen Inc. & Array BioPharma (USA) C19H27N5O3 Du, X. et al. C5-Alkyl-2-methylurea-substituted pyridines as a new class of glucokinase activators. ACS Med. Chem. Lett. (2014) 118722874 938
GKA36-18 GKA36-18 GKA: Systemic 2014 Urea,Pyridine 403.48 1.21 Amgen Inc. & Array BioPharma (USA) C20H29N5O4 Du, X. et al. C5-Alkyl-2-methylurea-substituted pyridines as a new class of glucokinase activators. ACS Med. Chem. Lett. (2014) 118722875 939
GKA36-19 GKA36-19 GKA: Systemic 2014 Urea,Pyridine 373.45 1.77 Amgen Inc. & Array BioPharma (USA) C19H27N5O3 Du, X. et al. C5-Alkyl-2-methylurea-substituted pyridines as a new class of glucokinase activators. ACS Med. Chem. Lett. (2014) 118722876 940
GKA36-2 GKA36-2 GKA: Systemic 2014 Urea,Pyridine 344.41 1.96 Amgen Inc. & Array BioPharma (USA) C18H24N4O3 Du, X. et al. C5-Alkyl-2-methylurea-substituted pyridines as a new class of glucokinase activators. ACS Med. Chem. Lett. (2014) 118722860 923
GKA36-20 GKA36-20 GKA: Systemic 2014 Urea,Pyridine 373.45 1.77 Amgen Inc. & Array BioPharma (USA) C19H27N5O3 Du, X. et al. C5-Alkyl-2-methylurea-substituted pyridines as a new class of glucokinase activators. ACS Med. Chem. Lett. (2014) 118722876 941
GKA36-21 GKA36-21 GKA: Systemic 2014 Urea,Pyridine 387.48 1.95 Amgen Inc. & Array BioPharma (USA) C20H29N5O3 Du, X. et al. C5-Alkyl-2-methylurea-substituted pyridines as a new class of glucokinase activators. ACS Med. Chem. Lett. (2014) 118722877 942
GKA36-22 GKA36-22 GKA: Systemic 2014 Urea,Pyridine 387.48 1.95 Amgen Inc. & Array BioPharma (USA) C20H29N5O3 Du, X. et al. C5-Alkyl-2-methylurea-substituted pyridines as a new class of glucokinase activators. ACS Med. Chem. Lett. (2014) 118722877 943
GKA36-23 GKA36-23 GKA: Systemic 2014 Urea,Pyridine 345.4 1.05 Amgen Inc. & Array BioPharma (USA) C17H23N5O3 Du, X. et al. C5-Alkyl-2-methylurea-substituted pyridines as a new class of glucokinase activators. ACS Med. Chem. Lett. (2014) 118723158 944
GKA36-24 GKA36-24 GKA: Systemic 2014 Urea,Pyridine 345.4 1.05 Amgen Inc. & Array BioPharma (USA) C17H23N5O3 Du, X. et al. C5-Alkyl-2-methylurea-substituted pyridines as a new class of glucokinase activators. ACS Med. Chem. Lett. (2014) 118723158 945
GKA36-25 GKA36-25 GKA: Systemic 2014 Urea,Pyridine 359.42 1.24 Amgen Inc. & Array BioPharma (USA) C18H25N5O3 Du, X. et al. C5-Alkyl-2-methylurea-substituted pyridines as a new class of glucokinase activators. ACS Med. Chem. Lett. (2014) 77460994 946
GKA36-26 GKA36-26 GKA: Systemic 2014 Urea,Pyridine 359.42 1.24 Amgen Inc. & Array BioPharma (USA) C18H25N5O3 Du, X. et al. C5-Alkyl-2-methylurea-substituted pyridines as a new class of glucokinase activators. ACS Med. Chem. Lett. (2014) 77460994 947
GKA36-3 GKA36-3 GKA: Systemic 2014 Urea,Pyridine 344.41 1.95 Amgen Inc. & Array BioPharma (USA) C18H24N4O3 Du, X. et al. C5-Alkyl-2-methylurea-substituted pyridines as a new class of glucokinase activators. ACS Med. Chem. Lett. (2014) 118722861 924
GKA36-4 GKA36-4 GKA: Systemic 2014 Urea,Pyridine 358.43 2.31 Amgen Inc. & Array BioPharma (USA) C19H26N4O3 Du, X. et al. C5-Alkyl-2-methylurea-substituted pyridines as a new class of glucokinase activators. ACS Med. Chem. Lett. (2014) 118722862 925
GKA36-5 GKA36-5 GKA: Systemic 2014 Urea,Pyridine 316.36 1.06 Amgen Inc. & Array BioPharma (USA) C16H20N4O3 Du, X. et al. C5-Alkyl-2-methylurea-substituted pyridines as a new class of glucokinase activators. ACS Med. Chem. Lett. (2014) 118722863 926
GKA36-6 GKA36-6 GKA: Systemic 2014 Urea,Pyridine 344.41 1.77 Amgen Inc. & Array BioPharma (USA) C18H24N4O3 Du, X. et al. C5-Alkyl-2-methylurea-substituted pyridines as a new class of glucokinase activators. ACS Med. Chem. Lett. (2014) 118722864 927
GKA36-7 GKA36-7 GKA: Systemic 2014 Urea,Pyridine 372.46 2.39 Amgen Inc. & Array BioPharma (USA) C20H28N4O3 Du, X. et al. C5-Alkyl-2-methylurea-substituted pyridines as a new class of glucokinase activators. ACS Med. Chem. Lett. (2014) 118722865 928
GKA36-8 GKA36-8 GKA: Systemic 2014 Urea,Pyridine 368.47 4.48 Amgen Inc. & Array BioPharma (USA) C21H28N4O2 Du, X. et al. C5-Alkyl-2-methylurea-substituted pyridines as a new class of glucokinase activators. ACS Med. Chem. Lett. (2014) 118722866 929
GKA36-9 GKA36-9 GKA: Systemic 2014 Urea,Pyridine 370.45 2.34 Amgen Inc. & Array BioPharma (USA) C20H26N4O3 Du, X. et al. C5-Alkyl-2-methylurea-substituted pyridines as a new class of glucokinase activators. ACS Med. Chem. Lett. (2014) 118722867 930
GKA37-12a GKA37-12a GKA: Systemic 2014 Pyridine 381.45 2.82 Amgen Inc. & Array BioPharma (USA) C19H19N5O2S Hinklin, R. J. et al. Discovery of 2-Pyridylureas as Glucokinase Activators. J. Med. Chem. (2014) 78350461 948
GKA37-13a GKA37-13a GKA: Systemic 2014 Pyridine 367.42 2.38 Amgen Inc. & Array BioPharma (USA) C18H17N5O2S Hinklin, R. J. et al. Discovery of 2-Pyridylureas as Glucokinase Activators. J. Med. Chem. (2014) 118715103 949
GKA37-14a GKA37-14a GKA: Systemic 2014 Pyridine 370.43 2 Amgen Inc. & Array BioPharma (USA) C17H18N6O2S Hinklin, R. J. et al. Discovery of 2-Pyridylureas as Glucokinase Activators. J. Med. Chem. (2014) 118715104 950
GKA37-15a GKA37-15a GKA: Systemic 2014 Urea,Pyridine 395.48 3.18 Amgen Inc. & Array BioPharma (USA) C20H21N5O2S Hinklin, R. J. et al. Discovery of 2-Pyridylureas as Glucokinase Activators. J. Med. Chem. (2014) 118715093 951
GKA37-16a GKA37-16a GKA: Systemic 2014 Urea,Pyridine 381.45 2.82 Amgen Inc. & Array BioPharma (USA) C19H19N5O2S Hinklin, R. J. et al. Discovery of 2-Pyridylureas as Glucokinase Activators. J. Med. Chem. (2014) 78350461 952
GKA37-16b GKA37-16b GKA: Systemic 2014 Urea,Pyridine 366.44 2.99 Amgen Inc. & Array BioPharma (USA) C19H18N4O2S Hinklin, R. J. et al. Discovery of 2-Pyridylureas as Glucokinase Activators. J. Med. Chem. (2014) 118715091 953
GKA37-16c GKA37-16c GKA: Systemic 2014 Urea,Pyridine 396.46 3.76 Amgen Inc. & Array BioPharma (USA) C20H20N4O3S Hinklin, R. J. et al. Discovery of 2-Pyridylureas as Glucokinase Activators. J. Med. Chem. (2014) 118715092 954
GKA37-16d GKA37-16d GKA: Systemic 2014 Urea,Pyridine 395.48 3.18 Amgen Inc. & Array BioPharma (USA) C20H21N5O2S Hinklin, R. J. et al. Discovery of 2-Pyridylureas as Glucokinase Activators. J. Med. Chem. (2014) 118715093 955
GKA37-17a GKA37-17a GKA: Systemic 2014 Urea,Pyridine 367.42 2.41 Amgen Inc. & Array BioPharma (USA) C18H17N5O2S Hinklin, R. J. et al. Discovery of 2-Pyridylureas as Glucokinase Activators. J. Med. Chem. (2014) 118715094 956
GKA37-18a GKA37-18a GKA: Systemic 2014 Urea,Pyridine 409.5 3.61 Amgen Inc. & Array BioPharma (USA) C21H23N5O2S Hinklin, R. J. et al. Discovery of 2-Pyridylureas as Glucokinase Activators. J. Med. Chem. (2014) 118715095 957
GKA37-19a GKA37-19a GKA: Systemic 2014 Urea,Pyridine 411.48 2.13 Amgen Inc. & Array BioPharma (USA) C20H21N5O3S Hinklin, R. J. et al. Discovery of 2-Pyridylureas as Glucokinase Activators. J. Med. Chem. (2014) 118715096 958
GKA37-20a GKA37-20a GKA: Systemic 2014 Urea,Pyridine 458.54 3.27 Amgen Inc. & Array BioPharma (USA) C24H22N6O2S Hinklin, R. J. et al. Discovery of 2-Pyridylureas as Glucokinase Activators. J. Med. Chem. (2014) 118715097 959
GKA37-21a GKA37-21a GKA: Systemic 2014 Urea,Pyridine 458.54 3.24 Amgen Inc. & Array BioPharma (USA) C24H22N6O2S Hinklin, R. J. et al. Discovery of 2-Pyridylureas as Glucokinase Activators. J. Med. Chem. (2014) 118715098 960
GKA37-22a GKA37-22a GKA: Systemic 2014 Urea,Pyridine 458.54 3.24 Amgen Inc. & Array BioPharma (USA) C24H22N6O2S Hinklin, R. J. et al. Discovery of 2-Pyridylureas as Glucokinase Activators. J. Med. Chem. (2014) 118715099 961
GKA37-23a GKA37-23a GKA: Systemic 2014 Urea,Pyridine 473.55 4.51 Amgen Inc. & Array BioPharma (USA) C25H23N5O3S Hinklin, R. J. et al. Discovery of 2-Pyridylureas as Glucokinase Activators. J. Med. Chem. (2014) 118715100 962
GKA37-24a GKA37-24a GKA: Systemic 2014 Urea,Pyridine 473.55 3.95 Amgen Inc. & Array BioPharma (USA) C25H23N5O3S Hinklin, R. J. et al. Discovery of 2-Pyridylureas as Glucokinase Activators. J. Med. Chem. (2014) 118715101 963
GKA37-25a GKA37-25a GKA: Systemic 2014 Urea,Pyridine 473.55 3.95 Amgen Inc. & Array BioPharma (USA) C25H23N5O3S Hinklin, R. J. et al. Discovery of 2-Pyridylureas as Glucokinase Activators. J. Med. Chem. (2014) 118715102 964
GKA37-30 GKA37-30 GKA: Systemic 2014 Urea,Pyridine 381.45 2.02 Amgen Inc. & Array BioPharma (USA) C19H19N5O2S Hinklin, R. J. et al. Discovery of 2-Pyridylureas as Glucokinase Activators. J. Med. Chem. (2014) 118715106 965
GKA37-31 GKA37-31 GKA: Systemic 2014 Urea,Pyridine 380.46 3.06 Amgen Inc. & Array BioPharma (USA) C20H20N4O2S Hinklin, R. J. et al. Discovery of 2-Pyridylureas as Glucokinase Activators. J. Med. Chem. (2014) 118715107 966
GKA37-32 GKA37-32 GKA: Systemic 2014 Urea,Pyridine 348.42 1.23 Amgen Inc. & Array BioPharma (USA) C16H20N4O3S Hinklin, R. J. et al. Discovery of 2-Pyridylureas as Glucokinase Activators. J. Med. Chem. (2014) 118715108 967
GKA37-33 GKA37-33 GKA: Systemic 2014 Urea,Pyridine 362.45 1.77 Amgen Inc. & Array BioPharma (USA) C17H22N4O3S Hinklin, R. J. et al. Discovery of 2-Pyridylureas as Glucokinase Activators. J. Med. Chem. (2014) 118715109 968
GKA37-34 GKA37-34 GKA: Systemic 2014 Urea,Pyridine 388.48 2.16 Amgen Inc. & Array BioPharma (USA) C19H24N4O3S Hinklin, R. J. et al. Discovery of 2-Pyridylureas as Glucokinase Activators. J. Med. Chem. (2014) 118715110 969
GKA37-35 GKA37-35 GKA: Systemic 2014 Urea,Pyridine 374.46 1.97 Amgen Inc. & Array BioPharma (USA) C18H22N4O3S Hinklin, R. J. et al. Discovery of 2-Pyridylureas as Glucokinase Activators. J. Med. Chem. (2014) 118715126 970
GKA37-36 GKA37-36 GKA: Systemic 2014 Urea,Pyridine 473.59 3 Amgen Inc. & Array BioPharma (USA) C23H31N5O4S Hinklin, R. J. et al. Discovery of 2-Pyridylureas as Glucokinase Activators. J. Med. Chem. (2014) 118715127 971
GKA37-37 GKA37-37 GKA: Systemic 2014 Urea,Pyridine 415.51 1.61 Amgen Inc. & Array BioPharma (USA) C20H25N5O3S Hinklin, R. J. et al. Discovery of 2-Pyridylureas as Glucokinase Activators. J. Med. Chem. (2014) 118715128 972
GKA37-38 GKA37-38 GKA: Systemic 2014 Urea,Pyridine 451.56 1.4 Amgen Inc. & Array BioPharma (USA) C19H25N5O4S2 Hinklin, R. J. et al. Discovery of 2-Pyridylureas as Glucokinase Activators. J. Med. Chem. (2014) 118715129 973
GKA3-8 GKA3-8 GKA: Systemic 2006 Benzamide,Pyridine 420.46 4.18 AstraZeneca (UK) C24H24N2O5 McKerrecher, D. et al. Design of a potent, soluble glucokinase activator with excellent in vivo efficacy. Bioorganic Med. Chem. Lett. (2006) 44410834 69
GKA38-14a GKA38-14a GKA: Systemic 2014 Urea,Benzo/Pyrido-thiazole 427.52 4.67 Chinese Academy of Medical Sciences (Beijing, CHINA) C22H25N3O4S Li, Y. et al. Discovery of novel urea derivatives as dual-target hypoglycemic agents that activate glucokinase and PPARγ. Eur. J. Med. Chem. (2014) 71816290 974
GKA38-14b GKA38-14b GKA: Systemic 2014 Urea,Benzo/Pyrido-thiazole 469.6 5.99 Chinese Academy of Medical Sciences (Beijing, CHINA) C25H31N3O4S Li, Y. et al. Discovery of novel urea derivatives as dual-target hypoglycemic agents that activate glucokinase and PPARγ. Eur. J. Med. Chem. (2014) 71816207 975
GKA38-14c GKA38-14c GKA: Systemic 2014 Urea,Benzo/Pyrido-thiazole 471.57 4.53 Chinese Academy of Medical Sciences (Beijing, CHINA) C24H29N3O5S Li, Y. et al. Discovery of novel urea derivatives as dual-target hypoglycemic agents that activate glucokinase and PPARγ. Eur. J. Med. Chem. (2014) 76332739 976
GKA38-14d GKA38-14d GKA: Systemic 2014 Urea,Benzo/Pyrido-thiazole 439.53 4.95 Chinese Academy of Medical Sciences (Beijing, CHINA) C23H25N3O4S Li, Y. et al. Discovery of novel urea derivatives as dual-target hypoglycemic agents that activate glucokinase and PPARγ. Eur. J. Med. Chem. (2014) 71816220 977
GKA38-14e GKA38-14e GKA: Systemic 2014 Urea,Benzo/Pyrido-thiazole 467.58 5.81 Chinese Academy of Medical Sciences (Beijing, CHINA) C25H29N3O4S Li, Y. et al. Discovery of novel urea derivatives as dual-target hypoglycemic agents that activate glucokinase and PPARγ. Eur. J. Med. Chem. (2014) 71816299 978
GKA38-14f GKA38-14f GKA: Systemic 2014 Urea,Benzo/Pyrido-thiazole 481.61 6.14 Chinese Academy of Medical Sciences (Beijing, CHINA) C26H31N3O4S Li, Y. et al. Discovery of novel urea derivatives as dual-target hypoglycemic agents that activate glucokinase and PPARγ. Eur. J. Med. Chem. (2014) 71816215 979
GKA38-14g GKA38-14g GKA: Systemic 2014 Urea,Benzo/Pyrido-thiazole 495.63 6.68 Chinese Academy of Medical Sciences (Beijing, CHINA) C27H33N3O4S Li, Y. et al. Discovery of novel urea derivatives as dual-target hypoglycemic agents that activate glucokinase and PPARγ. Eur. J. Med. Chem. (2014) 71816217 980
GKA38-14h GKA38-14h GKA: Systemic 2014 Urea,Benzo/Pyrido-thiazole 479.55 4.9 Chinese Academy of Medical Sciences (Beijing, CHINA) C25H25N3O5S Li, Y. et al. Discovery of novel urea derivatives as dual-target hypoglycemic agents that activate glucokinase and PPARγ. Eur. J. Med. Chem. (2014) 71816209 981
GKA38-14i GKA38-14i GKA: Systemic 2014 Urea,Benzo/Pyrido-thiazole 507.58 5.9 Chinese Academy of Medical Sciences (Beijing, CHINA) C27H26FN3O4S Li, Y. et al. Discovery of novel urea derivatives as dual-target hypoglycemic agents that activate glucokinase and PPARγ. Eur. J. Med. Chem. (2014) 71816308 982
GKA38-14j GKA38-14j GKA: Systemic 2014 Thiazole/Thiadiazole,Urea 419.54 4.67 Chinese Academy of Medical Sciences (Beijing, CHINA) C21H29N3O4S Li, Y. et al. Discovery of novel urea derivatives as dual-target hypoglycemic agents that activate glucokinase and PPARγ. Eur. J. Med. Chem. (2014) 71816246 983
GKA38-14k GKA38-14k GKA: Systemic 2014 Thiazole/Thiadiazole,Urea 419.54 4.57 Chinese Academy of Medical Sciences (Beijing, CHINA) C21H29N3O4S Li, Y. et al. Discovery of novel urea derivatives as dual-target hypoglycemic agents that activate glucokinase and PPARγ. Eur. J. Med. Chem. (2014) 71816312 984
GKA38-14l GKA38-14l GKA: Systemic 2014 Thiazole/Thiadiazole,Urea 421.51 3.1 Chinese Academy of Medical Sciences (Beijing, CHINA) C20H27N3O5S Li, Y. et al. Discovery of novel urea derivatives as dual-target hypoglycemic agents that activate glucokinase and PPARγ. Eur. J. Med. Chem. (2014) 76332740 985
GKA38-14m GKA38-14m GKA: Systemic 2014 Thiazole/Thiadiazole,Urea 389.47 3.52 Chinese Academy of Medical Sciences (Beijing, CHINA) C19H23N3O4S Li, Y. et al. Discovery of novel urea derivatives as dual-target hypoglycemic agents that activate glucokinase and PPARγ. Eur. J. Med. Chem. (2014) 71816223 986
GKA38-14n GKA38-14n GKA: Systemic 2014 Thiazole/Thiadiazole,Urea 417.52 4.38 Chinese Academy of Medical Sciences (Beijing, CHINA) C21H27N3O4S Li, Y. et al. Discovery of novel urea derivatives as dual-target hypoglycemic agents that activate glucokinase and PPARγ. Eur. J. Med. Chem. (2014) 71816301 987
GKA38-14o GKA38-14o GKA: Systemic 2014 Thiazole/Thiadiazole,Urea 431.55 4.71 Chinese Academy of Medical Sciences (Beijing, CHINA) C22H29N3O4S Li, Y. et al. Discovery of novel urea derivatives as dual-target hypoglycemic agents that activate glucokinase and PPARγ. Eur. J. Med. Chem. (2014) 71816213 988
GKA38-14p GKA38-14p GKA: Systemic 2014 Thiazole/Thiadiazole,Urea 445.57 5.25 Chinese Academy of Medical Sciences (Beijing, CHINA) C23H31N3O4S Li, Y. et al. Discovery of novel urea derivatives as dual-target hypoglycemic agents that activate glucokinase and PPARγ. Eur. J. Med. Chem. (2014) 71816219 989
GKA38-14q GKA38-14q GKA: Systemic 2014 Thiazole/Thiadiazole,Urea 429.49 3.48 Chinese Academy of Medical Sciences (Beijing, CHINA) C21H23N3O5S Li, Y. et al. Discovery of novel urea derivatives as dual-target hypoglycemic agents that activate glucokinase and PPARγ. Eur. J. Med. Chem. (2014) 71816210 990
GKA38-14r GKA38-14r GKA: Systemic 2014 Thiazole/Thiadiazole,Urea 457.52 4.48 Chinese Academy of Medical Sciences (Beijing, CHINA) C23H24FN3O4S Li, Y. et al. Discovery of novel urea derivatives as dual-target hypoglycemic agents that activate glucokinase and PPARγ. Eur. J. Med. Chem. (2014) 71816310 991
GKA38-14s GKA38-14s GKA: Systemic 2014 Urea,Benzo/Pyrido-thiazole 483.62 6.46 Chinese Academy of Medical Sciences (Beijing, CHINA) C26H33N3O4S Li, Y. et al. Discovery of novel urea derivatives as dual-target hypoglycemic agents that activate glucokinase and PPARγ. Eur. J. Med. Chem. (2014) 71816240 992
GKA38-14u GKA38-14u GKA: Systemic 2014 Thiazole/Thiadiazole,Urea 437.94 4.59 Chinese Academy of Medical Sciences (Beijing, CHINA) C20H24ClN3O4S Li, Y. et al. Discovery of novel urea derivatives as dual-target hypoglycemic agents that activate glucokinase and PPARγ. Eur. J. Med. Chem. (2014) 71816230 993
GKA38-15a GKA38-15a GKA: Systemic 2014 Urea,Benzo/Pyrido-thiazole 399.46 3.98 Chinese Academy of Medical Sciences (Beijing, CHINA) C20H21N3O4S Li, Y. et al. Discovery of novel urea derivatives as dual-target hypoglycemic agents that activate glucokinase and PPARγ. Eur. J. Med. Chem. (2014) 71816289 994
GKA38-15b GKA38-15b GKA: Systemic 2014 Urea,Benzo/Pyrido-thiazole 441.54 5.3 Chinese Academy of Medical Sciences (Beijing, CHINA) C23H27N3O4S Li, Y. et al. Discovery of novel urea derivatives as dual-target hypoglycemic agents that activate glucokinase and PPARγ. Eur. J. Med. Chem. (2014) 71816206 995
GKA38-15c GKA38-15c GKA: Systemic 2014 Urea,Benzo/Pyrido-thiazole 443.52 3.83 Chinese Academy of Medical Sciences (Beijing, CHINA) C22H25N3O5S Li, Y. et al. Discovery of novel urea derivatives as dual-target hypoglycemic agents that activate glucokinase and PPARγ. Eur. J. Med. Chem. (2014) 76336377 996
GKA38-15d GKA38-15d GKA: Systemic 2014 Urea,Benzo/Pyrido-thiazole 411.47 4.26 Chinese Academy of Medical Sciences (Beijing, CHINA) C21H21N3O4S Li, Y. et al. Discovery of novel urea derivatives as dual-target hypoglycemic agents that activate glucokinase and PPARγ. Eur. J. Med. Chem. (2014) 71816221 997
GKA38-15e GKA38-15e GKA: Systemic 2014 Urea,Benzo/Pyrido-thiazole 439.53 5.11 Chinese Academy of Medical Sciences (Beijing, CHINA) C23H25N3O4S Li, Y. et al. Discovery of novel urea derivatives as dual-target hypoglycemic agents that activate glucokinase and PPARγ. Eur. J. Med. Chem. (2014) 71816298 998
GKA38-15g GKA38-15g GKA: Systemic 2014 Urea,Benzo/Pyrido-thiazole 467.58 5.98 Chinese Academy of Medical Sciences (Beijing, CHINA) C25H29N3O4S Li, Y. et al. Discovery of novel urea derivatives as dual-target hypoglycemic agents that activate glucokinase and PPARγ. Eur. J. Med. Chem. (2014) 71816216 999
GKA38-15h GKA38-15h GKA: Systemic 2014 Urea,Benzo/Pyrido-thiazole 451.49 4.21 Chinese Academy of Medical Sciences (Beijing, CHINA) C23H21N3O5S Li, Y. et al. Discovery of novel urea derivatives as dual-target hypoglycemic agents that activate glucokinase and PPARγ. Eur. J. Med. Chem. (2014) 71816208 1000
GKA38-15i GKA38-15i GKA: Systemic 2014 Urea,Benzo/Pyrido-thiazole 479.52 5.21 Chinese Academy of Medical Sciences (Beijing, CHINA) C25H22FN3O4S Li, Y. et al. Discovery of novel urea derivatives as dual-target hypoglycemic agents that activate glucokinase and PPARγ. Eur. J. Med. Chem. (2014) 71816307 1001
GKA38-15j GKA38-15j GKA: Systemic 2014 Thiazole/Thiadiazole,Urea 391.48 3.98 Chinese Academy of Medical Sciences (Beijing, CHINA) C19H25N3O4S Li, Y. et al. Discovery of novel urea derivatives as dual-target hypoglycemic agents that activate glucokinase and PPARγ. Eur. J. Med. Chem. (2014) 71816245 1002
GKA38-15k GKA38-15k GKA: Systemic 2014 Thiazole/Thiadiazole,Urea 391.48 3.88 Chinese Academy of Medical Sciences (Beijing, CHINA) C19H25N3O4S Li, Y. et al. Discovery of novel urea derivatives as dual-target hypoglycemic agents that activate glucokinase and PPARγ. Eur. J. Med. Chem. (2014) 71816311 1003
GKA38-15l GKA38-15l GKA: Systemic 2014 Thiazole/Thiadiazole,Urea 393.46 2.41 Chinese Academy of Medical Sciences (Beijing, CHINA) C18H23N3O5S Li, Y. et al. Discovery of novel urea derivatives as dual-target hypoglycemic agents that activate glucokinase and PPARγ. Eur. J. Med. Chem. (2014) 76321894 1004
GKA38-15n GKA38-15n GKA: Systemic 2014 Thiazole/Thiadiazole,Urea 389.47 3.69 Chinese Academy of Medical Sciences (Beijing, CHINA) C19H23N3O4S Li, Y. et al. Discovery of novel urea derivatives as dual-target hypoglycemic agents that activate glucokinase and PPARγ. Eur. J. Med. Chem. (2014) 71816300 1005
GKA38-15o GKA38-15o GKA: Systemic 2014 Thiazole/Thiadiazole,Urea 403.5 4.02 Chinese Academy of Medical Sciences (Beijing, CHINA) C20H25N3O4S Li, Y. et al. Discovery of novel urea derivatives as dual-target hypoglycemic agents that activate glucokinase and PPARγ. Eur. J. Med. Chem. (2014) 71816212 1006
GKA38-15p GKA38-15p GKA: Systemic 2014 Thiazole/Thiadiazole,Urea 417.52 4.56 Chinese Academy of Medical Sciences (Beijing, CHINA) C21H27N3O4S Li, Y. et al. Discovery of novel urea derivatives as dual-target hypoglycemic agents that activate glucokinase and PPARγ. Eur. J. Med. Chem. (2014) 71816218 1007
GKA38-15q GKA38-15q GKA: Systemic 2014 Thiazole/Thiadiazole,Urea 401.44 2.78 Chinese Academy of Medical Sciences (Beijing, CHINA) C19H19N3O5S Li, Y. et al. Discovery of novel urea derivatives as dual-target hypoglycemic agents that activate glucokinase and PPARγ. Eur. J. Med. Chem. (2014) 71816211 1008
GKA38-15r GKA38-15r GKA: Systemic 2014 Thiazole/Thiadiazole,Urea 429.46 3.78 Chinese Academy of Medical Sciences (Beijing, CHINA) C21H20FN3O4S Li, Y. et al. Discovery of novel urea derivatives as dual-target hypoglycemic agents that activate glucokinase and PPARγ. Eur. J. Med. Chem. (2014) 71816309 1009
GKA38-15s GKA38-15s GKA: Systemic 2014 Urea,Benzo/Pyrido-thiazole 455.57 5.77 Chinese Academy of Medical Sciences (Beijing, CHINA) C24H29N3O4S Li, Y. et al. Discovery of novel urea derivatives as dual-target hypoglycemic agents that activate glucokinase and PPARγ. Eur. J. Med. Chem. (2014) 71816239 1010
GKA38-15t GKA38-15t GKA: Systemic 2014 Urea,Benzo/Pyrido-thiazole 427.52 4.87 Chinese Academy of Medical Sciences (Beijing, CHINA) C22H25N3O4S Li, Y. et al. Discovery of novel urea derivatives as dual-target hypoglycemic agents that activate glucokinase and PPARγ. Eur. J. Med. Chem. (2014) 71816241 1011
GKA38-15v GKA38-15v GKA: Systemic 2014 Urea,Pyridine 413.42 2.36 Chinese Academy of Medical Sciences (Beijing, CHINA) C21H23N3O6 Li, Y. et al. Discovery of novel urea derivatives as dual-target hypoglycemic agents that activate glucokinase and PPARγ. Eur. J. Med. Chem. (2014) 71816225 1012
GKA38-15w GKA38-15w GKA: Systemic 2014 Thiazole/Thiadiazole,Urea 377.46 3.48 Chinese Academy of Medical Sciences (Beijing, CHINA) C18H23N3O4S Li, Y. et al. Discovery of novel urea derivatives as dual-target hypoglycemic agents that activate glucokinase and PPARγ. Eur. J. Med. Chem. (2014) 71816237 1013
GKA38-15x GKA38-15x GKA: Systemic 2014 Urea 361.39 2.9 Chinese Academy of Medical Sciences (Beijing, CHINA) C18H23N3O5 Li, Y. et al. Discovery of novel urea derivatives as dual-target hypoglycemic agents that activate glucokinase and PPARγ. Eur. J. Med. Chem. (2014) 71816235 1014
GKA38-15y GKA38-15y GKA: Systemic 2014 Urea,Pyridine 357.4 2.98 Chinese Academy of Medical Sciences (Beijing, CHINA) C19H23N3O4 Li, Y. et al. Discovery of novel urea derivatives as dual-target hypoglycemic agents that activate glucokinase and PPARγ. Eur. J. Med. Chem. (2014) 71816233 1015
GKA3-9 GKA3-9 GKA: Systemic 2006 Benzamide,Pyridine 420.46 4.18 AstraZeneca (UK) C24H24N2O5 McKerrecher, D. et al. Design of a potent, soluble glucokinase activator with excellent in vivo efficacy. Bioorganic Med. Chem. Lett. (2006) 75022608 70
GKA39-13a GKA39-13a GKA: Systemic 2014 Benzamide,Pyridine 441.46 2.99 Chinese Academy of Medical Sciences (Beijing, CHINA) C21H19N3O6S Lu, J. et al. Design, synthesis, and activity evaluation of GK/PPARγ Dual-target-directed ligands as hypoglycemic agents. ChemMedChem (2014) 1023
GKA39-13b GKA39-13b GKA: Systemic 2014 Benzamide,Pyridine 427.43 2.55 Chinese Academy of Medical Sciences (Beijing, CHINA) C20H17N3O6S Lu, J. et al. Design, synthesis, and activity evaluation of GK/PPARγ Dual-target-directed ligands as hypoglycemic agents. ChemMedChem (2014) 1024
GKA39-18a GKA39-18a GKA: Systemic 2014 Benzamide,Pyridine 441.46 2.99 Chinese Academy of Medical Sciences (Beijing, CHINA) C21H19N3O6S Lu, J. et al. Design, synthesis, and activity evaluation of GK/PPARγ Dual-target-directed ligands as hypoglycemic agents. ChemMedChem (2014) 1025
GKA39-18b GKA39-18b GKA: Systemic 2014 Benzamide,Pyridine 427.43 2.55 Chinese Academy of Medical Sciences (Beijing, CHINA) C20H17N3O6S Lu, J. et al. Design, synthesis, and activity evaluation of GK/PPARγ Dual-target-directed ligands as hypoglycemic agents. ChemMedChem (2014) 1026
GKA39-23a GKA39-23a GKA: Systemic 2014 Benzamide,Pyridine 486.45 2.81 Chinese Academy of Medical Sciences (Beijing, CHINA) C21H18N4O8S Lu, J. et al. Design, synthesis, and activity evaluation of GK/PPARγ Dual-target-directed ligands as hypoglycemic agents. ChemMedChem (2014) 1027
GKA39-23b GKA39-23b GKA: Systemic 2014 Benzamide,Pyridine 472.43 2.38 Chinese Academy of Medical Sciences (Beijing, CHINA) C20H16N4O8S Lu, J. et al. Design, synthesis, and activity evaluation of GK/PPARγ Dual-target-directed ligands as hypoglycemic agents. ChemMedChem (2014) 1028
GKA39-26a GKA39-26a GKA: Systemic 2014 Benzamide,Pyridine 470.46 2.71 Chinese Academy of Medical Sciences (Beijing, CHINA) C21H18N4O7S Lu, J. et al. Design, synthesis, and activity evaluation of GK/PPARγ Dual-target-directed ligands as hypoglycemic agents. ChemMedChem (2014) 71483737 1029
GKA39-26b GKA39-26b GKA: Systemic 2014 Benzamide,Pyridine 456.43 2.28 Chinese Academy of Medical Sciences (Beijing, CHINA) C20H16N4O7S Lu, J. et al. Design, synthesis, and activity evaluation of GK/PPARγ Dual-target-directed ligands as hypoglycemic agents. ChemMedChem (2014) 71483738 1030
GKA39-26c GKA39-26c GKA: Systemic 2014 Benzamide,Pyridine 442.4 1.91 Chinese Academy of Medical Sciences (Beijing, CHINA) C19H14N4O7S Lu, J. et al. Design, synthesis, and activity evaluation of GK/PPARγ Dual-target-directed ligands as hypoglycemic agents. ChemMedChem (2014) 71483755 1031
GKA39-26d GKA39-26d GKA: Systemic 2014 Benzamide,Pyridine 384.37 2.06 Chinese Academy of Medical Sciences (Beijing, CHINA) C17H12N4O5S Lu, J. et al. Design, synthesis, and activity evaluation of GK/PPARγ Dual-target-directed ligands as hypoglycemic agents. ChemMedChem (2014) 71483734 1032
GKA39-26e GKA39-26e GKA: Systemic 2014 Benzamide,Pyridine 398.39 2.42 Chinese Academy of Medical Sciences (Beijing, CHINA) C18H14N4O5S Lu, J. et al. Design, synthesis, and activity evaluation of GK/PPARγ Dual-target-directed ligands as hypoglycemic agents. ChemMedChem (2014) 71483735 1033
GKA39-26f GKA39-26f GKA: Systemic 2014 Benzamide,Pyridine 418.81 2.69 Chinese Academy of Medical Sciences (Beijing, CHINA) C17H11ClN4O5S Lu, J. et al. Design, synthesis, and activity evaluation of GK/PPARγ Dual-target-directed ligands as hypoglycemic agents. ChemMedChem (2014) 71483736 1034
GKA39-26g GKA39-26g GKA: Systemic 2014 Benzamide,Pyrimidine 385.35 1.41 Chinese Academy of Medical Sciences (Beijing, CHINA) C16H11N5O5S Lu, J. et al. Design, synthesis, and activity evaluation of GK/PPARγ Dual-target-directed ligands as hypoglycemic agents. ChemMedChem (2014) 71483756 1035
GKA39-26h GKA39-26h GKA: Systemic 2014 Benzamide,Quinoline/Quinazoline 434.42 3.4 Chinese Academy of Medical Sciences (Beijing, CHINA) C21H14N4O5S Lu, J. et al. Design, synthesis, and activity evaluation of GK/PPARγ Dual-target-directed ligands as hypoglycemic agents. ChemMedChem (2014) 71483758 1036
GKA39-26i GKA39-26i GKA: Systemic 2014 Benzamide 388.35 1.95 Chinese Academy of Medical Sciences (Beijing, CHINA) C16H12N4O6S Lu, J. et al. Design, synthesis, and activity evaluation of GK/PPARγ Dual-target-directed ligands as hypoglycemic agents. ChemMedChem (2014) 1037
GKA39-26j GKA39-26j GKA: Systemic 2014 Thiazole/Thiadiazole,Benzamide 404.42 2.56 Chinese Academy of Medical Sciences (Beijing, CHINA) C16H12N4O5S2 Lu, J. et al. Design, synthesis, and activity evaluation of GK/PPARγ Dual-target-directed ligands as hypoglycemic agents. ChemMedChem (2014) 71483733 1038
GKA39-26k GKA39-26k GKA: Systemic 2014 Thiazole/Thiadiazole,Benzamide 390.39 2.16 Chinese Academy of Medical Sciences (Beijing, CHINA) C15H10N4O5S2 Lu, J. et al. Design, synthesis, and activity evaluation of GK/PPARγ Dual-target-directed ligands as hypoglycemic agents. ChemMedChem (2014) 71483710 1039
GKA39-26l GKA39-26l GKA: Systemic 2014 Benzamide,Benzo/Pyrido-thiazole 440.45 3.59 Chinese Academy of Medical Sciences (Beijing, CHINA) C19H12N4O5S2 Lu, J. et al. Design, synthesis, and activity evaluation of GK/PPARγ Dual-target-directed ligands as hypoglycemic agents. ChemMedChem (2014) 71483757 1040
GKA39-27a GKA39-27a GKA: Systemic 2014 Benzamide,Pyridine 472.47 2.58 Chinese Academy of Medical Sciences (Beijing, CHINA) C21H20N4O7S Lu, J. et al. Design, synthesis, and activity evaluation of GK/PPARγ Dual-target-directed ligands as hypoglycemic agents. ChemMedChem (2014) 1041
GKA39-27b GKA39-27b GKA: Systemic 2014 Thiazole/Thiadiazole,Benzamide 406.44 2.43 Chinese Academy of Medical Sciences (Beijing, CHINA) C16H14N4O5S2 Lu, J. et al. Design, synthesis, and activity evaluation of GK/PPARγ Dual-target-directed ligands as hypoglycemic agents. ChemMedChem (2014) 1042
GKA39-27c GKA39-27c GKA: Systemic 2014 Benzamide 390.37 1.84 Chinese Academy of Medical Sciences (Beijing, CHINA) C16H14N4O6S Lu, J. et al. Design, synthesis, and activity evaluation of GK/PPARγ Dual-target-directed ligands as hypoglycemic agents. ChemMedChem (2014) 1043
GKA39-4a GKA39-4a GKA: Systemic 2014 Benzamide,Pyridine 325.34 2.29 Chinese Academy of Medical Sciences (Beijing, CHINA) C16H11N3O3S Lu, J. et al. Design, synthesis, and activity evaluation of GK/PPARγ Dual-target-directed ligands as hypoglycemic agents. ChemMedChem (2014) 1016
GKA39-4b GKA39-4b GKA: Systemic 2014 Benzamide,Pyridine 411.43 2.95 Chinese Academy of Medical Sciences (Beijing, CHINA) C20H17N3O5S Lu, J. et al. Design, synthesis, and activity evaluation of GK/PPARγ Dual-target-directed ligands as hypoglycemic agents. ChemMedChem (2014) 1017
GKA39-8a GKA39-8a GKA: Systemic 2014 Benzamide,Pyridine 325.34 2.29 Chinese Academy of Medical Sciences (Beijing, CHINA) C16H11N3O3S Lu, J. et al. Design, synthesis, and activity evaluation of GK/PPARγ Dual-target-directed ligands as hypoglycemic agents. ChemMedChem (2014) 16392076 1018
GKA39-8b GKA39-8b GKA: Systemic 2014 Benzamide,Pyridine 411.43 2.95 Chinese Academy of Medical Sciences (Beijing, CHINA) C20H17N3O5S Lu, J. et al. Design, synthesis, and activity evaluation of GK/PPARγ Dual-target-directed ligands as hypoglycemic agents. ChemMedChem (2014) 71483841 1019
GKA39-8c GKA39-8c GKA: Systemic 2014 Thiazole/Thiadiazole,Benzamide 331.37 2.4 Chinese Academy of Medical Sciences (Beijing, CHINA) C14H9N3O3S2 Lu, J. et al. Design, synthesis, and activity evaluation of GK/PPARγ Dual-target-directed ligands as hypoglycemic agents. ChemMedChem (2014) 17564990 1020
GKA39-8d GKA39-8d GKA: Systemic 2014 Benzamide,Pyridine 339.37 2.66 Chinese Academy of Medical Sciences (Beijing, CHINA) C17H13N3O3S Lu, J. et al. Design, synthesis, and activity evaluation of GK/PPARγ Dual-target-directed ligands as hypoglycemic agents. ChemMedChem (2014) 35024794 1021
GKA39-8e GKA39-8e GKA: Systemic 2014 Benzamide 329.33 2.21 Chinese Academy of Medical Sciences (Beijing, CHINA) C15H11N3O4S Lu, J. et al. Design, synthesis, and activity evaluation of GK/PPARγ Dual-target-directed ligands as hypoglycemic agents. ChemMedChem (2014) 98328731 1022
GKA40-15a GKA40-15a GKA: Systemic 2014 Thiazole/Thiadiazole,Benzamide,Pyridine,Sulfoxide/Sulfone derivatives 562.66 4.41 Yuhan Research Institute (SOUTH KOREA) C28H26N4O5S2 Park, K. et al. Discovery of 3-(4-methanesulfonylphenoxy)-N-[1-(2-methoxy-ethoxymethyl)-1H- pyrazol-3-yl]-5-(3-methylpyridin-2-yl)-benzamide as a novel glucokinase activator (GKA) for the treatment of type 2 diabetes mellitus. Bioorganic Med. Chem. (2014) 142720283 1044
GKA40-15b GKA40-15b GKA: Systemic 2014 Thiazole/Thiadiazole,Benzamide,Pyridine,Sulfoxide/Sulfone derivatives 550.65 4.22 Yuhan Research Institute (SOUTH KOREA) C27H26N4O5S2 Park, K. et al. Discovery of 3-(4-methanesulfonylphenoxy)-N-[1-(2-methoxy-ethoxymethyl)-1H- pyrazol-3-yl]-5-(3-methylpyridin-2-yl)-benzamide as a novel glucokinase activator (GKA) for the treatment of type 2 diabetes mellitus. Bioorganic Med. Chem. (2014) 142720286 1045
GKA40-16a GKA40-16a GKA: Systemic 2014 Thiazole/Thiadiazole,Benzamide,Pyridine,Sulfoxide/Sulfone derivatives 465.54 3.84 Yuhan Research Institute (SOUTH KOREA) C23H19N3O4S2 Park, K. et al. Discovery of 3-(4-methanesulfonylphenoxy)-N-[1-(2-methoxy-ethoxymethyl)-1H- pyrazol-3-yl]-5-(3-methylpyridin-2-yl)-benzamide as a novel glucokinase activator (GKA) for the treatment of type 2 diabetes mellitus. Bioorganic Med. Chem. (2014) 76685222 1046
GKA40-16b GKA40-16b GKA: Systemic 2014 Thiazole/Thiadiazole,Benzamide,Pyridine,Sulfoxide/Sulfone derivatives 483.54 4.28 Yuhan Research Institute (SOUTH KOREA) C23H18FN3O4S2 Park, K. et al. Discovery of 3-(4-methanesulfonylphenoxy)-N-[1-(2-methoxy-ethoxymethyl)-1H- pyrazol-3-yl]-5-(3-methylpyridin-2-yl)-benzamide as a novel glucokinase activator (GKA) for the treatment of type 2 diabetes mellitus. Bioorganic Med. Chem. (2014) 77107475 1047
GKA40-18a GKA40-18a GKA: Systemic 2014 Thiazole/Thiadiazole,Benzamide,Pyridine,Sulfoxide/Sulfone derivatives 550.69 5.43 Yuhan Research Institute (SOUTH KOREA) C28H30N4O4S2 Park, K. et al. Discovery of 3-(4-methanesulfonylphenoxy)-N-[1-(2-methoxy-ethoxymethyl)-1H- pyrazol-3-yl]-5-(3-methylpyridin-2-yl)-benzamide as a novel glucokinase activator (GKA) for the treatment of type 2 diabetes mellitus. Bioorganic Med. Chem. (2014) 160951064 1048
GKA40-18b GKA40-18b GKA: Systemic 2014 Thiazole/Thiadiazole,Benzamide,Pyridine,Sulfoxide/Sulfone derivatives 564.68 3.34 Yuhan Research Institute (SOUTH KOREA) C28H28N4O5S2 Park, K. et al. Discovery of 3-(4-methanesulfonylphenoxy)-N-[1-(2-methoxy-ethoxymethyl)-1H- pyrazol-3-yl]-5-(3-methylpyridin-2-yl)-benzamide as a novel glucokinase activator (GKA) for the treatment of type 2 diabetes mellitus. Bioorganic Med. Chem. (2014) 77105090 1049
GKA40-18c GKA40-18c GKA: Systemic 2014 Thiazole/Thiadiazole,Benzamide,Pyridine,Sulfoxide/Sulfone derivatives 577.72 3.53 Yuhan Research Institute (SOUTH KOREA) C29H31N5O4S2 Park, K. et al. Discovery of 3-(4-methanesulfonylphenoxy)-N-[1-(2-methoxy-ethoxymethyl)-1H- pyrazol-3-yl]-5-(3-methylpyridin-2-yl)-benzamide as a novel glucokinase activator (GKA) for the treatment of type 2 diabetes mellitus. Bioorganic Med. Chem. (2014) 90655316 1050
GKA40-18d GKA40-18d GKA: Systemic 2014 Thiazole/Thiadiazole,Benzamide,Pyridine,Sulfoxide/Sulfone derivatives 610.74 3.42 Yuhan Research Institute (SOUTH KOREA) C30H34N4O6S2 Park, K. et al. Discovery of 3-(4-methanesulfonylphenoxy)-N-[1-(2-methoxy-ethoxymethyl)-1H- pyrazol-3-yl]-5-(3-methylpyridin-2-yl)-benzamide as a novel glucokinase activator (GKA) for the treatment of type 2 diabetes mellitus. Bioorganic Med. Chem. (2014) 90655317 1051
GKA40-18e GKA40-18e GKA: Systemic 2014 Thiazole/Thiadiazole,Benzamide,Pyridine,Sulfoxide/Sulfone derivatives 566.69 3.57 Yuhan Research Institute (SOUTH KOREA) C28H30N4O5S2 Park, K. et al. Discovery of 3-(4-methanesulfonylphenoxy)-N-[1-(2-methoxy-ethoxymethyl)-1H- pyrazol-3-yl]-5-(3-methylpyridin-2-yl)-benzamide as a novel glucokinase activator (GKA) for the treatment of type 2 diabetes mellitus. Bioorganic Med. Chem. (2014) 77105092 1052
GKA40-18f GKA40-18f GKA: Systemic 2014 Thiazole/Thiadiazole,Benzamide,Pyridine,Sulfoxide/Sulfone derivatives 563.69 3.06 Yuhan Research Institute (SOUTH KOREA) C28H29N5O4S2 Park, K. et al. Discovery of 3-(4-methanesulfonylphenoxy)-N-[1-(2-methoxy-ethoxymethyl)-1H- pyrazol-3-yl]-5-(3-methylpyridin-2-yl)-benzamide as a novel glucokinase activator (GKA) for the treatment of type 2 diabetes mellitus. Bioorganic Med. Chem. (2014) 77105088 1053
GKA40-18g GKA40-18g GKA: Systemic 2014 Thiazole/Thiadiazole,Benzamide,Pyridine,Sulfoxide/Sulfone derivatives 566.69 3.53 Yuhan Research Institute (SOUTH KOREA) C28H30N4O5S2 Park, K. et al. Discovery of 3-(4-methanesulfonylphenoxy)-N-[1-(2-methoxy-ethoxymethyl)-1H- pyrazol-3-yl]-5-(3-methylpyridin-2-yl)-benzamide as a novel glucokinase activator (GKA) for the treatment of type 2 diabetes mellitus. Bioorganic Med. Chem. (2014) 90655318 1054
GKA40-18h GKA40-18h GKA: Systemic 2014 Thiazole/Thiadiazole,Benzamide,Pyridine,Sulfoxide/Sulfone derivatives 582.69 3.12 Yuhan Research Institute (SOUTH KOREA) C28H30N4O6S2 Park, K. et al. Discovery of 3-(4-methanesulfonylphenoxy)-N-[1-(2-methoxy-ethoxymethyl)-1H- pyrazol-3-yl]-5-(3-methylpyridin-2-yl)-benzamide as a novel glucokinase activator (GKA) for the treatment of type 2 diabetes mellitus. Bioorganic Med. Chem. (2014) 90655319 1055
GKA40-18i GKA40-18i GKA: Systemic 2014 Thiazole/Thiadiazole,Benzamide,Pyridine,Sulfoxide/Sulfone derivatives 536.67 4.05 Yuhan Research Institute (SOUTH KOREA) C27H28N4O4S2 Park, K. et al. Discovery of 3-(4-methanesulfonylphenoxy)-N-[1-(2-methoxy-ethoxymethyl)-1H- pyrazol-3-yl]-5-(3-methylpyridin-2-yl)-benzamide as a novel glucokinase activator (GKA) for the treatment of type 2 diabetes mellitus. Bioorganic Med. Chem. (2014) 90655320 1056
GKA40-18j GKA40-18j GKA: Systemic 2014 Thiazole/Thiadiazole,Benzamide,Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 532.63 3.36 Yuhan Research Institute (SOUTH KOREA) C27H24N4O4S2 Park, K. et al. Discovery of 3-(4-methanesulfonylphenoxy)-N-[1-(2-methoxy-ethoxymethyl)-1H- pyrazol-3-yl]-5-(3-methylpyridin-2-yl)-benzamide as a novel glucokinase activator (GKA) for the treatment of type 2 diabetes mellitus. Bioorganic Med. Chem. (2014) 90655321 1057
GKA40-18k GKA40-18k GKA: Systemic 2014 Thiazole/Thiadiazole,Benzamide,Pyridine,Sulfoxide/Sulfone derivatives 536.67 4.14 Yuhan Research Institute (SOUTH KOREA) C27H28N4O4S2 Park, K. et al. Discovery of 3-(4-methanesulfonylphenoxy)-N-[1-(2-methoxy-ethoxymethyl)-1H- pyrazol-3-yl]-5-(3-methylpyridin-2-yl)-benzamide as a novel glucokinase activator (GKA) for the treatment of type 2 diabetes mellitus. Bioorganic Med. Chem. (2014) 77105468 1058
GKA40-19a GKA40-19a GKA: Systemic 2014 Benzamide,Pyridine,Sulfoxide/Sulfone derivatives 462.52 3.12 Yuhan Research Institute (SOUTH KOREA) C24H22N4O4S Park, K. et al. Discovery of 3-(4-methanesulfonylphenoxy)-N-[1-(2-methoxy-ethoxymethyl)-1H- pyrazol-3-yl]-5-(3-methylpyridin-2-yl)-benzamide as a novel glucokinase activator (GKA) for the treatment of type 2 diabetes mellitus. Bioorganic Med. Chem. (2014) 77107671 1059
GKA40-19b GKA40-19b GKA: Systemic 2014 Benzamide,Pyridine,Sulfoxide/Sulfone derivatives 506.57 3.37 Yuhan Research Institute (SOUTH KOREA) C26H26N4O5S Park, K. et al. Discovery of 3-(4-methanesulfonylphenoxy)-N-[1-(2-methoxy-ethoxymethyl)-1H- pyrazol-3-yl]-5-(3-methylpyridin-2-yl)-benzamide as a novel glucokinase activator (GKA) for the treatment of type 2 diabetes mellitus. Bioorganic Med. Chem. (2014) 77107471 1060
GKA40-19c GKA40-19c GKA: Systemic 2014 Benzamide,Pyridine,Sulfoxide/Sulfone derivatives 547.67 3.83 Yuhan Research Institute (SOUTH KOREA) C29H33N5O4S Park, K. et al. Discovery of 3-(4-methanesulfonylphenoxy)-N-[1-(2-methoxy-ethoxymethyl)-1H- pyrazol-3-yl]-5-(3-methylpyridin-2-yl)-benzamide as a novel glucokinase activator (GKA) for the treatment of type 2 diabetes mellitus. Bioorganic Med. Chem. (2014) 77107274 1061
GKA40-19d GKA40-19d GKA: Systemic 2014 Benzamide,Pyridine,Sulfoxide/Sulfone derivatives 561.65 2.72 Yuhan Research Institute (SOUTH KOREA) C29H31N5O5S Park, K. et al. Discovery of 3-(4-methanesulfonylphenoxy)-N-[1-(2-methoxy-ethoxymethyl)-1H- pyrazol-3-yl]-5-(3-methylpyridin-2-yl)-benzamide as a novel glucokinase activator (GKA) for the treatment of type 2 diabetes mellitus. Bioorganic Med. Chem. (2014) 77107672 1062
GKA40-19e GKA40-19e GKA: Systemic 2014 Benzamide,Pyridine,Sulfoxide/Sulfone derivatives 536.6 2.86 Yuhan Research Institute (SOUTH KOREA) C27H28N4O6S Park, K. et al. Discovery of 3-(4-methanesulfonylphenoxy)-N-[1-(2-methoxy-ethoxymethyl)-1H- pyrazol-3-yl]-5-(3-methylpyridin-2-yl)-benzamide as a novel glucokinase activator (GKA) for the treatment of type 2 diabetes mellitus. Bioorganic Med. Chem. (2014) 77107273 1063
GKA4-11 GKA4-11 GKA: Systemic 2008 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 392.49 2.19 OSI Pharmaceuticals (USA); Prosidion Limited (UK) C18H20N2O4S2 Bertram, L. S. et al. SAR, pharmacokinetics, safety, and efficacy of glucokinase activating 2-(4-sulfonylphenyl)-N-thiazol-2-ylacetamides: Discovery of PSN-GK1. J. Med. Chem. (2008) 10385853 78
GKA41-13a GKA41-13a GKA: Systemic 2015 Benzamide,Subsituted ethynyl 357.4 1.7 Yuhan Research Institute (SOUTH KOREA) C19H23N3O4 Park, K. et al. Design and synthesis of acetylenyl benzamide derivatives as novel glucokinase activators for the treatment of t2dm. ACS Med. Chem. Lett. (2015) 122177975 1064
GKA41-13b GKA41-13b GKA: Systemic 2015 Benzamide,Subsituted ethynyl 427.49 2.56 Yuhan Research Institute (SOUTH KOREA) C23H29N3O5 Park, K. et al. Design and synthesis of acetylenyl benzamide derivatives as novel glucokinase activators for the treatment of t2dm. ACS Med. Chem. Lett. (2015) 78319068 1065
GKA41-16a GKA41-16a GKA: Systemic 2015 Benzamide,Subsituted ethynyl 370.45 1.89 Yuhan Research Institute (SOUTH KOREA) C20H26N4O3 Park, K. et al. Design and synthesis of acetylenyl benzamide derivatives as novel glucokinase activators for the treatment of t2dm. ACS Med. Chem. Lett. (2015) 122177976 1066
GKA41-16b GKA41-16b GKA: Systemic 2015 Benzamide,Pyrimidine,Subsituted ethynyl 420.46 2.14 Yuhan Research Institute (SOUTH KOREA) C22H24N6O3 Park, K. et al. Design and synthesis of acetylenyl benzamide derivatives as novel glucokinase activators for the treatment of t2dm. ACS Med. Chem. Lett. (2015) 122177977 1067
GKA41-16c GKA41-16c GKA: Systemic 2015 Benzamide,Subsituted ethynyl 427.56 3.77 Yuhan Research Institute (SOUTH KOREA) C23H29N3O3S Park, K. et al. Design and synthesis of acetylenyl benzamide derivatives as novel glucokinase activators for the treatment of t2dm. ACS Med. Chem. Lett. (2015) 122177978 1068
GKA41-18a GKA41-18a GKA: Systemic 2015 Benzamide,Subsituted ethynyl 419.47 3.65 Yuhan Research Institute (SOUTH KOREA) C24H25N3O4 Park, K. et al. Design and synthesis of acetylenyl benzamide derivatives as novel glucokinase activators for the treatment of t2dm. ACS Med. Chem. Lett. (2015) 142720240 1069
GKA41-18b GKA41-18b GKA: Systemic 2015 Benzamide,Indole/Benzimidazole/Indazole,Subsituted ethynyl 428.48 3.81 Yuhan Research Institute (SOUTH KOREA) C25H24N4O3 Park, K. et al. Design and synthesis of acetylenyl benzamide derivatives as novel glucokinase activators for the treatment of t2dm. ACS Med. Chem. Lett. (2015) 122177980 1070
GKA41-18c GKA41-18c GKA: Systemic 2015 Benzamide,Subsituted ethynyl 433.46 3.49 Yuhan Research Institute (SOUTH KOREA) C24H23N3O5 Park, K. et al. Design and synthesis of acetylenyl benzamide derivatives as novel glucokinase activators for the treatment of t2dm. ACS Med. Chem. Lett. (2015) 122177981 1071
GKA41-18d GKA41-18d GKA: Systemic 2015 Benzamide,Subsituted ethynyl 404.46 3 Yuhan Research Institute (SOUTH KOREA) C23H24N4O3 Park, K. et al. Design and synthesis of acetylenyl benzamide derivatives as novel glucokinase activators for the treatment of t2dm. ACS Med. Chem. Lett. (2015) 78319067 1072
GKA41-19 GKA41-19 GKA: Systemic 2015 Benzamide,Subsituted ethynyl 404.46 3 Yuhan Research Institute (SOUTH KOREA) C23H24N4O3 Park, K. et al. Design and synthesis of acetylenyl benzamide derivatives as novel glucokinase activators for the treatment of t2dm. ACS Med. Chem. Lett. (2015) 78319009 1073
GKA4-12 GKA4-12 GKA: Systemic 2008 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 394.51 2.28 OSI Pharmaceuticals (USA); Prosidion Limited (UK) C18H22N2O4S2 Bertram, L. S. et al. SAR, pharmacokinetics, safety, and efficacy of glucokinase activating 2-(4-sulfonylphenyl)-N-thiazol-2-ylacetamides: Discovery of PSN-GK1. J. Med. Chem. (2008) 10250045 79
GKA41-20a GKA41-20a GKA: Systemic 2015 Benzamide,Subsituted ethynyl 432.51 3.8 Yuhan Research Institute (SOUTH KOREA) C25H28N4O3 Park, K. et al. Design and synthesis of acetylenyl benzamide derivatives as novel glucokinase activators for the treatment of t2dm. ACS Med. Chem. Lett. (2015) 122177983 1074
GKA41-20b GKA41-20b GKA: Systemic 2015 Benzamide,Subsituted ethynyl 460.57 4.53 Yuhan Research Institute (SOUTH KOREA) C27H32N4O3 Park, K. et al. Design and synthesis of acetylenyl benzamide derivatives as novel glucokinase activators for the treatment of t2dm. ACS Med. Chem. Lett. (2015) 122177984 1075
GKA41-20c GKA41-20c GKA: Systemic 2015 Benzamide,Subsituted ethynyl 475.58 3.7 Yuhan Research Institute (SOUTH KOREA) C27H33N5O3 Park, K. et al. Design and synthesis of acetylenyl benzamide derivatives as novel glucokinase activators for the treatment of t2dm. ACS Med. Chem. Lett. (2015) 76685070 1076
GKA41-20d GKA41-20d GKA: Systemic 2015 Benzamide,Subsituted ethynyl 501.62 4.19 Yuhan Research Institute (SOUTH KOREA) C29H35N5O3 Park, K. et al. Design and synthesis of acetylenyl benzamide derivatives as novel glucokinase activators for the treatment of t2dm. ACS Med. Chem. Lett. (2015) 122177985 1077
GKA41-20e GKA41-20e GKA: Systemic 2015 Benzamide,Subsituted ethynyl 515.65 4.55 Yuhan Research Institute (SOUTH KOREA) C30H37N5O3 Park, K. et al. Design and synthesis of acetylenyl benzamide derivatives as novel glucokinase activators for the treatment of t2dm. ACS Med. Chem. Lett. (2015) 122177986 1078
GKA41-20f GKA41-20f GKA: Systemic 2015 Benzamide,Subsituted ethynyl 517.62 3.33 Yuhan Research Institute (SOUTH KOREA) C29H35N5O4 Park, K. et al. Design and synthesis of acetylenyl benzamide derivatives as novel glucokinase activators for the treatment of t2dm. ACS Med. Chem. Lett. (2015) 122177987 1079
GKA41-20g GKA41-20g GKA: Systemic 2015 Benzamide,Subsituted ethynyl 462.54 3.52 Yuhan Research Institute (SOUTH KOREA) C26H30N4O4 Park, K. et al. Design and synthesis of acetylenyl benzamide derivatives as novel glucokinase activators for the treatment of t2dm. ACS Med. Chem. Lett. (2015) 122177988 1080
GKA41-20h GKA41-20h GKA: Systemic 2015 Benzamide,Subsituted ethynyl 512.6 3.78 Yuhan Research Institute (SOUTH KOREA) C29H32N6O3 Park, K. et al. Design and synthesis of acetylenyl benzamide derivatives as novel glucokinase activators for the treatment of t2dm. ACS Med. Chem. Lett. (2015) 122177989 1081
GKA41-21 GKA41-21 GKA: Systemic 2015 Benzamide,Subsituted ethynyl 405.45 3.32 Yuhan Research Institute (SOUTH KOREA) C23H23N3O4 Park, K. et al. Design and synthesis of acetylenyl benzamide derivatives as novel glucokinase activators for the treatment of t2dm. ACS Med. Chem. Lett. (2015) 122177982 1082
GKA41-22a GKA41-22a GKA: Systemic 2015 Benzamide,Subsituted ethynyl 447.53 4.45 Yuhan Research Institute (SOUTH KOREA) C26H29N3O4 Park, K. et al. Design and synthesis of acetylenyl benzamide derivatives as novel glucokinase activators for the treatment of t2dm. ACS Med. Chem. Lett. (2015) 122177990 1083
GKA41-22b GKA41-22b GKA: Systemic 2015 Benzamide,Subsituted ethynyl 444.48 3.44 Yuhan Research Institute (SOUTH KOREA) C25H24N4O4 Park, K. et al. Design and synthesis of acetylenyl benzamide derivatives as novel glucokinase activators for the treatment of t2dm. ACS Med. Chem. Lett. (2015) 122177991 1084
GKA41-22c GKA41-22c GKA: Systemic 2015 Benzamide,Subsituted ethynyl 502.6 4.18 Yuhan Research Institute (SOUTH KOREA) C29H34N4O4 Park, K. et al. Design and synthesis of acetylenyl benzamide derivatives as novel glucokinase activators for the treatment of t2dm. ACS Med. Chem. Lett. (2015) 122177992 1085
GKA41-22d GKA41-22d GKA: Systemic 2015 Benzamide,Subsituted ethynyl 516.63 4.53 Yuhan Research Institute (SOUTH KOREA) C30H36N4O4 Park, K. et al. Design and synthesis of acetylenyl benzamide derivatives as novel glucokinase activators for the treatment of t2dm. ACS Med. Chem. Lett. (2015) 122177993 1086
GKA41-22e GKA41-22e GKA: Systemic 2015 Benzamide,Subsituted ethynyl 518.6 3.31 Yuhan Research Institute (SOUTH KOREA) C29H34N4O5 Park, K. et al. Design and synthesis of acetylenyl benzamide derivatives as novel glucokinase activators for the treatment of t2dm. ACS Med. Chem. Lett. (2015) 122177994 1087
GKA4-13 GKA4-13 GKA: Systemic 2008 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 394.51 2.28 OSI Pharmaceuticals (USA); Prosidion Limited (UK) C18H22N2O4S2 Bertram, L. S. et al. SAR, pharmacokinetics, safety, and efficacy of glucokinase activating 2-(4-sulfonylphenyl)-N-thiazol-2-ylacetamides: Discovery of PSN-GK1. J. Med. Chem. (2008) 10250045 80
GKA4-14 GKA4-14 GKA: Systemic 2008 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 394.51 2.28 OSI Pharmaceuticals (USA); Prosidion Limited (UK) C18H22N2O4S2 Bertram, L. S. et al. SAR, pharmacokinetics, safety, and efficacy of glucokinase activating 2-(4-sulfonylphenyl)-N-thiazol-2-ylacetamides: Discovery of PSN-GK1. J. Med. Chem. (2008) 24906074 81
GKA4-15 GKA4-15 GKA: Systemic 2008 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 412.5 2.72 OSI Pharmaceuticals (USA); Prosidion Limited (UK) C18H21FN2O4S2 Bertram, L. S. et al. SAR, pharmacokinetics, safety, and efficacy of glucokinase activating 2-(4-sulfonylphenyl)-N-thiazol-2-ylacetamides: Discovery of PSN-GK1. J. Med. Chem. (2008) 24906118 82
GKA42-31 GKA42-31 GKA: Systemic 2015 Sulfoxide/Sulfone derivatives 426.27 4.05 University of Jordan (Amman, JORDAN) C18H13Cl2NO5S Taha, M. O., Habash, M., Hatmal, M. M., Abdelazeem, A. H. & Qandil, A. Ligand-based modeling followed by in vitro bioassay yielded new potent glucokinase activators. J. Mol. Graph. Model. (2015) 302819 1088
GKA42-32 GKA42-32 GKA: Systemic 2015 370.18 3.68 University of Jordan (Amman, JORDAN) C16H13Cl2NO5 Taha, M. O., Habash, M., Hatmal, M. M., Abdelazeem, A. H. & Qandil, A. Ligand-based modeling followed by in vitro bioassay yielded new potent glucokinase activators. J. Mol. Graph. Model. (2015) 309597 1089
GKA42-33 GKA42-33 GKA: Systemic 2015 Sulfoxide/Sulfone derivatives 426.45 4.24 University of Jordan (Amman, JORDAN) C20H18N4O5S Taha, M. O., Habash, M., Hatmal, M. M., Abdelazeem, A. H. & Qandil, A. Ligand-based modeling followed by in vitro bioassay yielded new potent glucokinase activators. J. Mol. Graph. Model. (2015) 407913 1090
GKA42-34 GKA42-34 GKA: Systemic 2015 Sulfoxide/Sulfone derivatives 360.21 3.16 University of Jordan (Amman, JORDAN) C14H11Cl2NO4S Taha, M. O., Habash, M., Hatmal, M. M., Abdelazeem, A. H. & Qandil, A. Ligand-based modeling followed by in vitro bioassay yielded new potent glucokinase activators. J. Mol. Graph. Model. (2015) 227302 1091
GKA42-35 GKA42-35 GKA: Systemic 2015 385.41 1.21 University of Jordan (Amman, JORDAN) C20H23N3O5 Taha, M. O., Habash, M., Hatmal, M. M., Abdelazeem, A. H. & Qandil, A. Ligand-based modeling followed by in vitro bioassay yielded new potent glucokinase activators. J. Mol. Graph. Model. (2015) 410906 1092
GKA42-36 GKA42-36 GKA: Systemic 2015 493.51 5.27 University of Jordan (Amman, JORDAN) C27H27NO8 Taha, M. O., Habash, M., Hatmal, M. M., Abdelazeem, A. H. & Qandil, A. Ligand-based modeling followed by in vitro bioassay yielded new potent glucokinase activators. J. Mol. Graph. Model. (2015) 384849 1093
GKA42-37 GKA42-37 GKA: Systemic 2015 Indole/Benzimidazole/Indazole 336.17 3.78 University of Jordan (Amman, JORDAN) C15H11Cl2N3O2 Taha, M. O., Habash, M., Hatmal, M. M., Abdelazeem, A. H. & Qandil, A. Ligand-based modeling followed by in vitro bioassay yielded new potent glucokinase activators. J. Mol. Graph. Model. (2015) 414500 1094
GKA42-38 GKA42-38 GKA: Systemic 2015 Sulfoxide/Sulfone derivatives 578.57 4.76 University of Jordan (Amman, JORDAN) C26H18N4O8S2 Taha, M. O., Habash, M., Hatmal, M. M., Abdelazeem, A. H. & Qandil, A. Ligand-based modeling followed by in vitro bioassay yielded new potent glucokinase activators. J. Mol. Graph. Model. (2015) 22111 1095
GKA42-39 GKA42-39 GKA: Systemic 2015 451.39 2.15 University of Jordan (Amman, JORDAN) C21H17N5O7 Taha, M. O., Habash, M., Hatmal, M. M., Abdelazeem, A. H. & Qandil, A. Ligand-based modeling followed by in vitro bioassay yielded new potent glucokinase activators. J. Mol. Graph. Model. (2015) 98540984 1096
GKA4-24 GKA4-24 GKA: Systemic 2008 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 420.55 2.84 OSI Pharmaceuticals (USA); Prosidion Limited (UK) C20H24N2O4S2 Bertram, L. S. et al. SAR, pharmacokinetics, safety, and efficacy of glucokinase activating 2-(4-sulfonylphenyl)-N-thiazol-2-ylacetamides: Discovery of PSN-GK1. J. Med. Chem. (2008) 24906119 83
GKA42-40 GKA42-40 GKA: Systemic 2015 Benzamide,Sulfoxide/Sulfone derivatives 491.52 5.1 University of Jordan (Amman, JORDAN) C25H21N3O6S Taha, M. O., Habash, M., Hatmal, M. M., Abdelazeem, A. H. & Qandil, A. Ligand-based modeling followed by in vitro bioassay yielded new potent glucokinase activators. J. Mol. Graph. Model. (2015) 84715 1097
GKA42-41 GKA42-41 GKA: Systemic 2015 Pyrimidine 477.54 3.57 University of Jordan (Amman, JORDAN) C24H23N5O4S Taha, M. O., Habash, M., Hatmal, M. M., Abdelazeem, A. H. & Qandil, A. Ligand-based modeling followed by in vitro bioassay yielded new potent glucokinase activators. J. Mol. Graph. Model. (2015) 293300 1098
GKA4-25 GKA4-25 GKA: Systemic 2008 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 434.57 3.24 OSI Pharmaceuticals (USA); Prosidion Limited (UK) C21H26N2O4S2 Bertram, L. S. et al. SAR, pharmacokinetics, safety, and efficacy of glucokinase activating 2-(4-sulfonylphenyl)-N-thiazol-2-ylacetamides: Discovery of PSN-GK1. J. Med. Chem. (2008) 24906075 84
GKA4-27 GKA4-27 GKA: Systemic 2008 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 452.56 3.63 OSI Pharmaceuticals (USA); Prosidion Limited (UK) C21H25FN2O4S2 Bertram, L. S. et al. SAR, pharmacokinetics, safety, and efficacy of glucokinase activating 2-(4-sulfonylphenyl)-N-thiazol-2-ylacetamides: Discovery of PSN-GK1. J. Med. Chem. (2008) 24906076 85
GKA4-28 GKA4-28 GKA: Systemic 2008 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 466.59 3.99 OSI Pharmaceuticals (USA); Prosidion Limited (UK) C22H27FN2O4S2 Bertram, L. S. et al. SAR, pharmacokinetics, safety, and efficacy of glucokinase activating 2-(4-sulfonylphenyl)-N-thiazol-2-ylacetamides: Discovery of PSN-GK1. J. Med. Chem. (2008) 24906120 86
GKA4-3 GKA4-3 GKA: Systemic 2008 Pyrazine 307.37 2.73 OSI Pharmaceuticals (USA); Prosidion Limited (UK) C17H13N3OS Bertram, L. S. et al. SAR, pharmacokinetics, safety, and efficacy of glucokinase activating 2-(4-sulfonylphenyl)-N-thiazol-2-ylacetamides: Discovery of PSN-GK1. J. Med. Chem. (2008) 44568124 75
GKA43-1 GKA43-1 GKA: Systemic 2016 Urea,Pyridine 243.26 1.72 Amgen Inc. & Array BioPharma (USA) C13H13N3O2 Dransfield, P. J. et al. Novel Series of Potent Glucokinase Activators Leading to the Discovery of AM-2394. ACS Med. Chem. Lett. (2016) 155511463 1099
GKA43-10 GKA43-10 GKA: Systemic 2016 Urea,Pyridine 356.33 2.48 Amgen Inc. & Array BioPharma (USA) C18H14F2N4O2 Dransfield, P. J. et al. Novel Series of Potent Glucokinase Activators Leading to the Discovery of AM-2394. ACS Med. Chem. Lett. (2016) 155555013 1108
GKA43-11 GKA43-11 GKA: Systemic 2016 Urea,Pyridine 356.33 2.48 Amgen Inc. & Array BioPharma (USA) C18H14F2N4O2 Dransfield, P. J. et al. Novel Series of Potent Glucokinase Activators Leading to the Discovery of AM-2394. ACS Med. Chem. Lett. (2016) 155532809 1109
GKA43-12 GKA43-12 GKA: Systemic 2016 Urea,Pyridine 386.35 2.78 Amgen Inc. & Array BioPharma (USA) C19H16F2N4O3 Dransfield, P. J. et al. Novel Series of Potent Glucokinase Activators Leading to the Discovery of AM-2394. ACS Med. Chem. Lett. (2016) 155541450 1110
GKA43-13 GKA43-13 GKA: Systemic 2016 Urea,Pyridine 400.38 3.15 Amgen Inc. & Array BioPharma (USA) C20H18F2N4O3 Dransfield, P. J. et al. Novel Series of Potent Glucokinase Activators Leading to the Discovery of AM-2394. ACS Med. Chem. Lett. (2016) 155544957 1111
GKA43-14 GKA43-14 GKA: Systemic 2016 Urea,Pyridine 416.38 2.1 Amgen Inc. & Array BioPharma (USA) C20H18F2N4O4 Dransfield, P. J. et al. Novel Series of Potent Glucokinase Activators Leading to the Discovery of AM-2394. ACS Med. Chem. Lett. (2016) 155544468 1112
GKA43-15 GKA43-15 GKA: Systemic 2016 Urea,Pyridine 381.39 1.16 Amgen Inc. & Array BioPharma (USA) C19H19N5O4 Dransfield, P. J. et al. Novel Series of Potent Glucokinase Activators Leading to the Discovery of AM-2394. ACS Med. Chem. Lett. (2016) 155517272 1113
GKA43-16 GKA43-16 GKA: Systemic 2016 Urea,Pyridine 381.39 0.83 Amgen Inc. & Array BioPharma (USA) C19H19N5O4 Dransfield, P. J. et al. Novel Series of Potent Glucokinase Activators Leading to the Discovery of AM-2394. ACS Med. Chem. Lett. (2016) 155511835 1114
GKA43-17 GKA43-17 GKA: Systemic 2016 Urea,Pyridine 381.39 0.83 Amgen Inc. & Array BioPharma (USA) C19H19N5O4 Dransfield, P. J. et al. Novel Series of Potent Glucokinase Activators Leading to the Discovery of AM-2394. ACS Med. Chem. Lett. (2016) 155563881 1115
GKA43-18 GKA43-18 GKA: Systemic 2016 Urea,Pyridine 395.41 1.23 Amgen Inc. & Array BioPharma (USA) C20H21N5O4 Dransfield, P. J. et al. Novel Series of Potent Glucokinase Activators Leading to the Discovery of AM-2394. ACS Med. Chem. Lett. (2016) 155535024 1116
GKA43-19 GKA43-19 GKA: Systemic 2016 Urea,Pyridine 395.41 1.23 Amgen Inc. & Array BioPharma (USA) C20H21N5O4 Dransfield, P. J. et al. Novel Series of Potent Glucokinase Activators Leading to the Discovery of AM-2394. ACS Med. Chem. Lett. (2016) 155514513 1117
GKA43-2 GKA43-2 GKA: Systemic 2016 Urea,Pyridine 261.25 1.82 Amgen Inc. & Array BioPharma (USA) C13H12FN3O2 Dransfield, P. J. et al. Novel Series of Potent Glucokinase Activators Leading to the Discovery of AM-2394. ACS Med. Chem. Lett. (2016) 155512123 1100
GKA43-20 GKA43-20 GKA: Systemic 2016 Urea,Pyridine 395.41 1.19 Amgen Inc. & Array BioPharma (USA) C20H21N5O4 Dransfield, P. J. et al. Novel Series of Potent Glucokinase Activators Leading to the Discovery of AM-2394. ACS Med. Chem. Lett. (2016) 155543920 1118
GKA43-21 GKA43-21 GKA: Systemic 2016 Urea,Pyridine 395.41 1.19 Amgen Inc. & Array BioPharma (USA) C20H21N5O4 Dransfield, P. J. et al. Novel Series of Potent Glucokinase Activators Leading to the Discovery of AM-2394. ACS Med. Chem. Lett. (2016) 155518537 1119
GKA43-22 GKA43-22 GKA: Systemic 2016 Urea,Pyridine 409.44 1.62 Amgen Inc. & Array BioPharma (USA) C21H23N5O4 Dransfield, P. J. et al. Novel Series of Potent Glucokinase Activators Leading to the Discovery of AM-2394. ACS Med. Chem. Lett. (2016) 155563873 1120
GKA43-23 GKA43-23 GKA: Systemic 2016 Urea,Pyridine 411.41 0.8 Amgen Inc. & Array BioPharma (USA) C20H21N5O5 Dransfield, P. J. et al. Novel Series of Potent Glucokinase Activators Leading to the Discovery of AM-2394. ACS Med. Chem. Lett. (2016) 155533971 1121
GKA43-24 GKA43-24 GKA: Systemic 2016 Urea,Pyridine 425.44 1.16 Amgen Inc. & Array BioPharma (USA) C21H23N5O5 Dransfield, P. J. et al. Novel Series of Potent Glucokinase Activators Leading to the Discovery of AM-2394. ACS Med. Chem. Lett. (2016) 155563130 1122
GKA43-25 GKA43-25 GKA: Systemic 2016 Urea,Pyridine 409.44 1.62 Amgen Inc. & Array BioPharma (USA) C21H23N5O4 Dransfield, P. J. et al. Novel Series of Potent Glucokinase Activators Leading to the Discovery of AM-2394. ACS Med. Chem. Lett. (2016) 155561677 1123
GKA43-26 GKA43-26 GKA: Systemic 2016 Urea,Pyridine 409.44 1.62 Amgen Inc. & Array BioPharma (USA) C21H23N5O4 Dransfield, P. J. et al. Novel Series of Potent Glucokinase Activators Leading to the Discovery of AM-2394. ACS Med. Chem. Lett. (2016) 155545997 1124
GKA43-3 GKA43-3 GKA: Systemic 2016 Urea,Pyridine 295.7 2.45 Amgen Inc. & Array BioPharma (USA) C13H11ClFN3O2 Dransfield, P. J. et al. Novel Series of Potent Glucokinase Activators Leading to the Discovery of AM-2394. ACS Med. Chem. Lett. (2016) 155548914 1101
GKA43-4 GKA43-4 GKA: Systemic 2016 Urea,Pyridine 279.24 1.92 Amgen Inc. & Array BioPharma (USA) C13H11F2N3O2 Dransfield, P. J. et al. Novel Series of Potent Glucokinase Activators Leading to the Discovery of AM-2394. ACS Med. Chem. Lett. (2016) 155533510 1102
GKA43-5 GKA43-5 GKA: Systemic 2016 Urea,Pyridine 358.14 2.61 Amgen Inc. & Array BioPharma (USA) C13H10BrF2N3O2 Dransfield, P. J. et al. Novel Series of Potent Glucokinase Activators Leading to the Discovery of AM-2394. ACS Med. Chem. Lett. (2016) 155511256 1103
GKA43-6 GKA43-6 GKA: Systemic 2016 Urea,Pyridine 293.27 2.29 Amgen Inc. & Array BioPharma (USA) C14H13F2N3O2 Dransfield, P. J. et al. Novel Series of Potent Glucokinase Activators Leading to the Discovery of AM-2394. ACS Med. Chem. Lett. (2016) 155522913 1104
GKA43-7 GKA43-7 GKA: Systemic 2016 Urea,Pyridine 319.31 2.83 Amgen Inc. & Array BioPharma (USA) C16H15F2N3O2 Dransfield, P. J. et al. Novel Series of Potent Glucokinase Activators Leading to the Discovery of AM-2394. ACS Med. Chem. Lett. (2016) 155558714 1105
GKA43-8 GKA43-8 GKA: Systemic 2016 Urea,Pyridine 355.34 3.55 Amgen Inc. & Array BioPharma (USA) C19H15F2N3O2 Dransfield, P. J. et al. Novel Series of Potent Glucokinase Activators Leading to the Discovery of AM-2394. ACS Med. Chem. Lett. (2016) 150575761 1106
GKA43-9 GKA43-9 GKA: Systemic 2016 Urea,Pyridine 356.33 2.51 Amgen Inc. & Array BioPharma (USA) C18H14F2N4O2 Dransfield, P. J. et al. Novel Series of Potent Glucokinase Activators Leading to the Discovery of AM-2394. ACS Med. Chem. Lett. (2016) 150436720 1107
GKA4-4 GKA4-4 GKA: Systemic 2008 Thiazole/Thiadiazole 312.41 3.9 OSI Pharmaceuticals (USA); Prosidion Limited (UK) C16H12N2OS2 Bertram, L. S. et al. SAR, pharmacokinetics, safety, and efficacy of glucokinase activating 2-(4-sulfonylphenyl)-N-thiazol-2-ylacetamides: Discovery of PSN-GK1. J. Med. Chem. (2008) 10448235 76
GKA44-10 GKA44-10 GKA: Systemic 2016 Urea,Pyridine 370.45 1.75 Amgen Inc. & Array BioPharma (USA) C20H26N4O3 Kohn, T. J. et al. 5-Alkyl-2-urea-Substituted Pyridines: Identification of Efficacious Glucokinase Activators with Improved Properties. ACS Med. Chem. Lett. (2016) 155568928 1133
GKA44-11 GKA44-11 GKA: Systemic 2016 Urea,Pyridine 342.39 1.12 Amgen Inc. & Array BioPharma (USA) C18H22N4O3 Kohn, T. J. et al. 5-Alkyl-2-urea-Substituted Pyridines: Identification of Efficacious Glucokinase Activators with Improved Properties. ACS Med. Chem. Lett. (2016) 155568209 1134
GKA44-12 GKA44-12 GKA: Systemic 2016 Urea,Pyridine 344.37 -0.14 Amgen Inc. & Array BioPharma (USA) C17H20N4O4 Kohn, T. J. et al. 5-Alkyl-2-urea-Substituted Pyridines: Identification of Efficacious Glucokinase Activators with Improved Properties. ACS Med. Chem. Lett. (2016) 155545349 1135
GKA44-13 GKA44-13 GKA: Systemic 2016 Urea,Pyridine 328.37 0.77 Amgen Inc. & Array BioPharma (USA) C17H20N4O3 Kohn, T. J. et al. 5-Alkyl-2-urea-Substituted Pyridines: Identification of Efficacious Glucokinase Activators with Improved Properties. ACS Med. Chem. Lett. (2016) 155550743 1136
GKA44-14 GKA44-14 GKA: Systemic 2016 Urea,Pyridine 356.42 1.39 Amgen Inc. & Array BioPharma (USA) C19H24N4O3 Kohn, T. J. et al. 5-Alkyl-2-urea-Substituted Pyridines: Identification of Efficacious Glucokinase Activators with Improved Properties. ACS Med. Chem. Lett. (2016) 155568860 1137
GKA44-15 GKA44-15 GKA: Systemic 2016 Urea,Pyridine 342.39 1.29 Amgen Inc. & Array BioPharma (USA) C18H22N4O3 Kohn, T. J. et al. 5-Alkyl-2-urea-Substituted Pyridines: Identification of Efficacious Glucokinase Activators with Improved Properties. ACS Med. Chem. Lett. (2016) 155535512 1138
GKA44-16 GKA44-16 GKA: Systemic 2016 Urea,Pyridine 356.42 1.84 Amgen Inc. & Array BioPharma (USA) C19H24N4O3 Kohn, T. J. et al. 5-Alkyl-2-urea-Substituted Pyridines: Identification of Efficacious Glucokinase Activators with Improved Properties. ACS Med. Chem. Lett. (2016) 155556274 1139
GKA44-17 GKA44-17 GKA: Systemic 2016 Urea,Pyridine 344.37 0.66 Amgen Inc. & Array BioPharma (USA) C17H20N4O4 Kohn, T. J. et al. 5-Alkyl-2-urea-Substituted Pyridines: Identification of Efficacious Glucokinase Activators with Improved Properties. ACS Med. Chem. Lett. (2016) 155539930 1140
GKA44-18 GKA44-18 GKA: Systemic 2016 Urea,Pyridine 356.38 0.65 Amgen Inc. & Array BioPharma (USA) C18H20N4O4 Kohn, T. J. et al. 5-Alkyl-2-urea-Substituted Pyridines: Identification of Efficacious Glucokinase Activators with Improved Properties. ACS Med. Chem. Lett. (2016) 155522427 1141
GKA44-19 GKA44-19 GKA: Systemic 2016 Urea,Pyridine 358.39 1.01 Amgen Inc. & Array BioPharma (USA) C18H22N4O4 Kohn, T. J. et al. 5-Alkyl-2-urea-Substituted Pyridines: Identification of Efficacious Glucokinase Activators with Improved Properties. ACS Med. Chem. Lett. (2016) 155515486 1142
GKA44-2 GKA44-2 GKA: Systemic 2016 Urea,Pyridine 302.33 0.59 Amgen Inc. & Array BioPharma (USA) C15H18N4O3 Kohn, T. J. et al. 5-Alkyl-2-urea-Substituted Pyridines: Identification of Efficacious Glucokinase Activators with Improved Properties. ACS Med. Chem. Lett. (2016) 71603583 1125
GKA44-20 GKA44-20 GKA: Systemic 2016 Urea,Pyridine 356.38 0.65 Amgen Inc. & Array BioPharma (USA) C18H20N4O4 Kohn, T. J. et al. 5-Alkyl-2-urea-Substituted Pyridines: Identification of Efficacious Glucokinase Activators with Improved Properties. ACS Med. Chem. Lett. (2016) 71603582 1143
GKA44-21 GKA44-21 GKA: Systemic 2016 Urea,Pyridine 358.39 1.01 Amgen Inc. & Array BioPharma (USA) C18H22N4O4 Kohn, T. J. et al. 5-Alkyl-2-urea-Substituted Pyridines: Identification of Efficacious Glucokinase Activators with Improved Properties. ACS Med. Chem. Lett. (2016) 71603520 1144
GKA44-22 GKA44-22 GKA: Systemic 2016 Urea,Pyridine 358.39 1.01 Amgen Inc. & Array BioPharma (USA) C18H22N4O4 Kohn, T. J. et al. 5-Alkyl-2-urea-Substituted Pyridines: Identification of Efficacious Glucokinase Activators with Improved Properties. ACS Med. Chem. Lett. (2016) 155547616 1145
GKA44-23 GKA44-23 GKA: Systemic 2016 Urea,Pyridine 371.43 1.2 Amgen Inc. & Array BioPharma (USA) C19H25N5O3 Kohn, T. J. et al. 5-Alkyl-2-urea-Substituted Pyridines: Identification of Efficacious Glucokinase Activators with Improved Properties. ACS Med. Chem. Lett. (2016) 155545330 1146
GKA44-24 GKA44-24 GKA: Systemic 2016 Urea,Pyridine 374.39 0.04 Amgen Inc. & Array BioPharma (USA) C18H22N4O5 Kohn, T. J. et al. 5-Alkyl-2-urea-Substituted Pyridines: Identification of Efficacious Glucokinase Activators with Improved Properties. ACS Med. Chem. Lett. (2016) 155534084 1147
GKA44-25 GKA44-25 GKA: Systemic 2016 Urea,Pyridine 376.38 1.07 Amgen Inc. & Array BioPharma (USA) C18H21FN4O4 Kohn, T. J. et al. 5-Alkyl-2-urea-Substituted Pyridines: Identification of Efficacious Glucokinase Activators with Improved Properties. ACS Med. Chem. Lett. (2016) 155525686 1148
GKA44-26 GKA44-26 GKA: Systemic 2016 Urea,Pyridine 394.37 1.33 Amgen Inc. & Array BioPharma (USA) C18H20F2N4O4 Kohn, T. J. et al. 5-Alkyl-2-urea-Substituted Pyridines: Identification of Efficacious Glucokinase Activators with Improved Properties. ACS Med. Chem. Lett. (2016) 155564114 1149
GKA44-3 GKA44-3 GKA: Systemic 2016 Urea,Pyridine 316.36 0.95 Amgen Inc. & Array BioPharma (USA) C16H20N4O3 Kohn, T. J. et al. 5-Alkyl-2-urea-Substituted Pyridines: Identification of Efficacious Glucokinase Activators with Improved Properties. ACS Med. Chem. Lett. (2016) 155540236 1126
GKA44-4 GKA44-4 GKA: Systemic 2016 Urea,Pyridine 330.38 1.3 Amgen Inc. & Array BioPharma (USA) C17H22N4O3 Kohn, T. J. et al. 5-Alkyl-2-urea-Substituted Pyridines: Identification of Efficacious Glucokinase Activators with Improved Properties. ACS Med. Chem. Lett. (2016) 155545320 1127
GKA44-5 GKA44-5 GKA: Systemic 2016 Urea,Pyridine 316.36 0.92 Amgen Inc. & Array BioPharma (USA) C16H20N4O3 Kohn, T. J. et al. 5-Alkyl-2-urea-Substituted Pyridines: Identification of Efficacious Glucokinase Activators with Improved Properties. ACS Med. Chem. Lett. (2016) 151355906 1128
GKA44-6 GKA44-6 GKA: Systemic 2016 Urea,Pyridine 330.38 1.49 Amgen Inc. & Array BioPharma (USA) C17H22N4O3 Kohn, T. J. et al. 5-Alkyl-2-urea-Substituted Pyridines: Identification of Efficacious Glucokinase Activators with Improved Properties. ACS Med. Chem. Lett. (2016) 155543626 1129
GKA44-7 GKA44-7 GKA: Systemic 2016 Urea,Pyridine 328.37 0.94 Amgen Inc. & Array BioPharma (USA) C17H20N4O3 Kohn, T. J. et al. 5-Alkyl-2-urea-Substituted Pyridines: Identification of Efficacious Glucokinase Activators with Improved Properties. ACS Med. Chem. Lett. (2016) 71603523 1130
GKA44-8 GKA44-8 GKA: Systemic 2016 Urea,Pyridine 328.37 0.94 Amgen Inc. & Array BioPharma (USA) C17H20N4O3 Kohn, T. J. et al. 5-Alkyl-2-urea-Substituted Pyridines: Identification of Efficacious Glucokinase Activators with Improved Properties. ACS Med. Chem. Lett. (2016) 71603523 1131
GKA44-9 GKA44-9 GKA: Systemic 2016 Urea,Pyridine 342.39 1.13 Amgen Inc. & Array BioPharma (USA) C18H22N4O3 Kohn, T. J. et al. 5-Alkyl-2-urea-Substituted Pyridines: Identification of Efficacious Glucokinase Activators with Improved Properties. ACS Med. Chem. Lett. (2016) 155545937 1132
GKA4-5 GKA4-5 GKA: Systemic 2008 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 390.5 3.14 OSI Pharmaceuticals (USA); Prosidion Limited (UK) C17H14N2O3S3 Bertram, L. S. et al. SAR, pharmacokinetics, safety, and efficacy of glucokinase activating 2-(4-sulfonylphenyl)-N-thiazol-2-ylacetamides: Discovery of PSN-GK1. J. Med. Chem. (2008) 11741138 77
GKA45-14__racemic_ GKA45-14 (racemic) GKA: Systemic 2016 Sulfoxide/Sulfone derivatives,Azaindole 402.94 5.48 Servier Research Institute (Budapest, HUNGARY & Suresnes, FRANCE) C21H23ClN2O2S Paczal, A. et al. Structure-Activity Relationship of Azaindole-Based Glucokinase Activators. J. Med. Chem. (2016) 127039203 1150
GKA45-14a GKA45-14a GKA: Systemic 2016 Sulfoxide/Sulfone derivatives,Azaindole 402.94 5.48 Servier Research Institute (Budapest, HUNGARY & Suresnes, FRANCE) C21H23ClN2O2S Paczal, A. et al. Structure-Activity Relationship of Azaindole-Based Glucokinase Activators. J. Med. Chem. (2016) 127039203 1151
GKA45-14b GKA45-14b GKA: Systemic 2016 Sulfoxide/Sulfone derivatives,Azaindole 402.94 5.48 Servier Research Institute (Budapest, HUNGARY & Suresnes, FRANCE) C21H23ClN2O2S Paczal, A. et al. Structure-Activity Relationship of Azaindole-Based Glucokinase Activators. J. Med. Chem. (2016) 127039203 1152
GKA45-16b GKA45-16b GKA: Systemic 2017 Sulfoxide/Sulfone derivatives,Azaindole 386.94 5.37 Servier Research Institute (Budapest, HUNGARY & Suresnes, FRANCE) C21H23ClN2OS Paczal, A. et al. Structure-Activity Relationship of Azaindole-Based Glucokinase Activators. J. Med. Chem. (2016) 127042493 1153
GKA45-16c GKA45-16c GKA: Systemic 2018 Sulfoxide/Sulfone derivatives,Azaindole 386.94 5.37 Servier Research Institute (Budapest, HUNGARY & Suresnes, FRANCE) C21H23ClN2OS Paczal, A. et al. Structure-Activity Relationship of Azaindole-Based Glucokinase Activators. J. Med. Chem. (2016) 127042493 1154
GKA45-16d GKA45-16d GKA: Systemic 2019 Sulfoxide/Sulfone derivatives,Azaindole 386.94 5.37 Servier Research Institute (Budapest, HUNGARY & Suresnes, FRANCE) C21H23ClN2OS Paczal, A. et al. Structure-Activity Relationship of Azaindole-Based Glucokinase Activators. J. Med. Chem. (2016) 127042493 1155
GKA45-19a GKA45-19a GKA: Systemic 2016 Azaindole 340.85 5.89 Servier Research Institute (Budapest, HUNGARY & Suresnes, FRANCE) C20H21ClN2O Paczal, A. et al. Structure-Activity Relationship of Azaindole-Based Glucokinase Activators. J. Med. Chem. (2016) 127040024 1156
GKA45-19b GKA45-19b GKA: Systemic 2016 Azaindole 369.3 6.31 Servier Research Institute (Budapest, HUNGARY & Suresnes, FRANCE) C20H21BrN2 Paczal, A. et al. Structure-Activity Relationship of Azaindole-Based Glucokinase Activators. J. Med. Chem. (2016) 127040025 1157
GKA45-21 GKA45-21 GKA: Systemic 2016 Azaindole 349.86 5.96 Servier Research Institute (Budapest, HUNGARY & Suresnes, FRANCE) C21H20ClN3 Paczal, A. et al. Structure-Activity Relationship of Azaindole-Based Glucokinase Activators. J. Med. Chem. (2016) 127040026 1158
GKA45-22 GKA45-22 GKA: Systemic 2016 Azaindole 324.85 6.24 Servier Research Institute (Budapest, HUNGARY & Suresnes, FRANCE) C20H21ClN2 Paczal, A. et al. Structure-Activity Relationship of Azaindole-Based Glucokinase Activators. J. Med. Chem. (2016) 127040027 1159
GKA45-23 GKA45-23 GKA: Systemic 2016 Benzamide,Azaindole 367.87 5.12 Servier Research Institute (Budapest, HUNGARY & Suresnes, FRANCE) C21H22ClN3O Paczal, A. et al. Structure-Activity Relationship of Azaindole-Based Glucokinase Activators. J. Med. Chem. (2016) 127040028 1160
GKA45-24 GKA45-24 GKA: Systemic 2016 Azaindole 366.88 5.93 Servier Research Institute (Budapest, HUNGARY & Suresnes, FRANCE) C22H23ClN2O Paczal, A. et al. Structure-Activity Relationship of Azaindole-Based Glucokinase Activators. J. Med. Chem. (2016) 127040029 1161
GKA45-25 GKA45-25 GKA: Systemic 2016 Azaindole 368.86 5.77 Servier Research Institute (Budapest, HUNGARY & Suresnes, FRANCE) C21H21ClN2O2 Paczal, A. et al. Structure-Activity Relationship of Azaindole-Based Glucokinase Activators. J. Med. Chem. (2016) 127040030 1162
GKA45-26a GKA45-26a GKA: Systemic 2016 Azaindole 472.94 6.32 Servier Research Institute (Budapest, HUNGARY & Suresnes, FRANCE) C25H30ClN2O3P Paczal, A. et al. Structure-Activity Relationship of Azaindole-Based Glucokinase Activators. J. Med. Chem. (2016) 127041333 1163
GKA45-27 GKA45-27 GKA: Systemic 2016 Azaindole 460.93 6.09 Servier Research Institute (Budapest, HUNGARY & Suresnes, FRANCE) C24H30ClN2O3P Paczal, A. et al. Structure-Activity Relationship of Azaindole-Based Glucokinase Activators. J. Med. Chem. (2016) 127041335 1164
GKA45-28a GKA45-28a GKA: Systemic 2016 Azaindole 354.87 6.22 Servier Research Institute (Budapest, HUNGARY & Suresnes, FRANCE) C21H23ClN2O Paczal, A. et al. Structure-Activity Relationship of Azaindole-Based Glucokinase Activators. J. Med. Chem. (2016) 127041336 1165
GKA45-28b GKA45-28b GKA: Systemic 2016 Azaindole 382.93 7.01 Servier Research Institute (Budapest, HUNGARY & Suresnes, FRANCE) C23H27ClN2O Paczal, A. et al. Structure-Activity Relationship of Azaindole-Based Glucokinase Activators. J. Med. Chem. (2016) 127041337 1166
GKA45-28c GKA45-28c GKA: Systemic 2016 Azaindole 412.95 6.5 Servier Research Institute (Budapest, HUNGARY & Suresnes, FRANCE) C24H29ClN2O2 Paczal, A. et al. Structure-Activity Relationship of Azaindole-Based Glucokinase Activators. J. Med. Chem. (2016) 127041338 1167
GKA45-29 GKA45-29 GKA: Systemic 2016 Azaindole 382.88 6.1 Servier Research Institute (Budapest, HUNGARY & Suresnes, FRANCE) C22H23ClN2O2 Paczal, A. et al. Structure-Activity Relationship of Azaindole-Based Glucokinase Activators. J. Med. Chem. (2016) 127042444 1168
GKA45-30 GKA45-30 GKA: Systemic 2016 Azaindole 354.87 5.36 Servier Research Institute (Budapest, HUNGARY & Suresnes, FRANCE) C21H23ClN2O Paczal, A. et al. Structure-Activity Relationship of Azaindole-Based Glucokinase Activators. J. Med. Chem. (2016) 127042445 1169
GKA45-34a GKA45-34a GKA: Systemic 2016 Sulfoxide/Sulfone derivatives,Azaindole 388.91 3.71 Servier Research Institute (Budapest, HUNGARY & Suresnes, FRANCE) C20H21ClN2O2S Paczal, A. et al. Structure-Activity Relationship of Azaindole-Based Glucokinase Activators. J. Med. Chem. (2016) 127042446 1170
GKA45-34b GKA45-34b GKA: Systemic 2016 Sulfoxide/Sulfone derivatives,Azaindole 402.94 4.26 Servier Research Institute (Budapest, HUNGARY & Suresnes, FRANCE) C21H23ClN2O2S Paczal, A. et al. Structure-Activity Relationship of Azaindole-Based Glucokinase Activators. J. Med. Chem. (2016) 127042447 1171
GKA45-34d GKA45-34d GKA: Systemic 2016 Sulfoxide/Sulfone derivatives,Azaindole 387.93 3.43 Servier Research Institute (Budapest, HUNGARY & Suresnes, FRANCE) C20H22ClN3OS Paczal, A. et al. Structure-Activity Relationship of Azaindole-Based Glucokinase Activators. J. Med. Chem. (2016) 127038882 1172
GKA45-34e GKA45-34e GKA: Systemic 2016 Sulfoxide/Sulfone derivatives,Azaindole 401.95 3.97 Servier Research Institute (Budapest, HUNGARY & Suresnes, FRANCE) C21H24ClN3OS Paczal, A. et al. Structure-Activity Relationship of Azaindole-Based Glucokinase Activators. J. Med. Chem. (2016) 127041529 1173
GKA45-38a GKA45-38a GKA: Systemic 2016 Sulfoxide/Sulfone derivatives,Azaindole 402.94 4.29 Servier Research Institute (Budapest, HUNGARY & Suresnes, FRANCE) C21H23ClN2O2S Paczal, A. et al. Structure-Activity Relationship of Azaindole-Based Glucokinase Activators. J. Med. Chem. (2016) 127041530 1174
GKA45-38b GKA45-38b GKA: Systemic 2016 Sulfoxide/Sulfone derivatives,Azaindole 481.83 4.98 Servier Research Institute (Budapest, HUNGARY & Suresnes, FRANCE) C21H22BrClN2O2S Paczal, A. et al. Structure-Activity Relationship of Azaindole-Based Glucokinase Activators. J. Med. Chem. (2016) 127041531 1175
GKA45-39a GKA45-39a GKA: Systemic 2016 Sulfoxide/Sulfone derivatives,Azaindole 418.94 4.4 Servier Research Institute (Budapest, HUNGARY & Suresnes, FRANCE) C21H23ClN2O3S Paczal, A. et al. Structure-Activity Relationship of Azaindole-Based Glucokinase Activators. J. Med. Chem. (2016) 127041532 1176
GKA45-39b GKA45-39b GKA: Systemic 2016 Sulfoxide/Sulfone derivatives,Azaindole 497.83 5.09 Servier Research Institute (Budapest, HUNGARY & Suresnes, FRANCE) C21H22BrClN2O3S Paczal, A. et al. Structure-Activity Relationship of Azaindole-Based Glucokinase Activators. J. Med. Chem. (2016) 127041828 1177
GKA45-40a GKA45-40a GKA: Systemic 2016 Sulfoxide/Sulfone derivatives,Azaindole 384.92 5.62 Servier Research Institute (Budapest, HUNGARY & Suresnes, FRANCE) C21H21ClN2OS Paczal, A. et al. Structure-Activity Relationship of Azaindole-Based Glucokinase Activators. J. Med. Chem. (2016) 127039539 1178
GKA45-41a GKA45-41a GKA: Systemic 2016 Sulfoxide/Sulfone derivatives,Azaindole 400.92 5.74 Servier Research Institute (Budapest, HUNGARY & Suresnes, FRANCE) C21H21ClN2O2S Paczal, A. et al. Structure-Activity Relationship of Azaindole-Based Glucokinase Activators. J. Med. Chem. (2016) 127042495 1179
GKA45-41b GKA45-41b GKA: Systemic 2016 Sulfoxide/Sulfone derivatives,Azaindole 479.82 6.43 Servier Research Institute (Budapest, HUNGARY & Suresnes, FRANCE) C21H20BrClN2O2S Paczal, A. et al. Structure-Activity Relationship of Azaindole-Based Glucokinase Activators. J. Med. Chem. (2016) 127042497 1180
GKA45-41c GKA45-41c GKA: Systemic 2016 Sulfoxide/Sulfone derivatives,Azaindole 479.82 6.43 Servier Research Institute (Budapest, HUNGARY & Suresnes, FRANCE) C21H20BrClN2O2S Paczal, A. et al. Structure-Activity Relationship of Azaindole-Based Glucokinase Activators. J. Med. Chem. (2016) 127042497 1181
GKA45-42 GKA45-42 GKA: Systemic 2016 Sulfoxide/Sulfone derivatives,Azaindole 481.83 6.17 Servier Research Institute (Budapest, HUNGARY & Suresnes, FRANCE) C21H22BrClN2O2S Paczal, A. et al. Structure-Activity Relationship of Azaindole-Based Glucokinase Activators. J. Med. Chem. (2016) 127042498 1182
GKA45-43 GKA45-43 GKA: Systemic 2016 Sulfoxide/Sulfone derivatives,Azaindole 487.01 5.76 Servier Research Institute (Budapest, HUNGARY & Suresnes, FRANCE) C25H27ClN2O4S Paczal, A. et al. Structure-Activity Relationship of Azaindole-Based Glucokinase Activators. J. Med. Chem. (2016) 127042499 1183
GKA45-44a GKA45-44a GKA: Systemic 2016 Sulfoxide/Sulfone derivatives,Azaindole 485 6.01 Servier Research Institute (Budapest, HUNGARY & Suresnes, FRANCE) C25H25ClN2O4S Paczal, A. et al. Structure-Activity Relationship of Azaindole-Based Glucokinase Activators. J. Med. Chem. (2016) 127040362 1184
GKA45-44b GKA45-44b GKA: Systemic 2016 Sulfoxide/Sulfone derivatives,Azaindole 485 6.01 Servier Research Institute (Budapest, HUNGARY & Suresnes, FRANCE) C25H25ClN2O4S Paczal, A. et al. Structure-Activity Relationship of Azaindole-Based Glucokinase Activators. J. Med. Chem. (2016) 127042500 1185
GKA45-45 GKA45-45 GKA: Systemic 2016 Azaindole 312.45 4.05 Servier Research Institute (Budapest, HUNGARY & Suresnes, FRANCE) C20H28N2O Paczal, A. et al. Structure-Activity Relationship of Azaindole-Based Glucokinase Activators. J. Med. Chem. (2016) 127037853 1186
GKA45-47 GKA45-47 GKA: Systemic 2016 Sulfoxide/Sulfone derivatives,Azaindole 416.96 4.48 Servier Research Institute (Budapest, HUNGARY & Suresnes, FRANCE) C22H25ClN2O2S Paczal, A. et al. Structure-Activity Relationship of Azaindole-Based Glucokinase Activators. J. Med. Chem. (2016) 127038556 1187
GKA45-48 GKA45-48 GKA: Systemic 2016 Sulfoxide/Sulfone derivatives,Azaindole 421.38 6 Servier Research Institute (Budapest, HUNGARY & Suresnes, FRANCE) C21H22Cl2N2OS Paczal, A. et al. Structure-Activity Relationship of Azaindole-Based Glucokinase Activators. J. Med. Chem. (2016) 127037884 1188
GKA45-49 GKA45-49 GKA: Systemic 2016 Sulfoxide/Sulfone derivatives,Azaindole 465.83 6.06 Servier Research Institute (Budapest, HUNGARY & Suresnes, FRANCE) C21H22BrClN2OS Paczal, A. et al. Structure-Activity Relationship of Azaindole-Based Glucokinase Activators. J. Med. Chem. (2016) 127039549 1189
GKA45-50 GKA45-50 GKA: Systemic 2016 Sulfoxide/Sulfone derivatives,Azaindole 512.83 6.02 Servier Research Institute (Budapest, HUNGARY & Suresnes, FRANCE) C21H22ClIN2OS Paczal, A. et al. Structure-Activity Relationship of Azaindole-Based Glucokinase Activators. J. Med. Chem. (2016) 127038219 1190
GKA45-53 GKA45-53 GKA: Systemic 2016 Sulfoxide/Sulfone derivatives,Azaindole 300.33 2.23 Servier Research Institute (Budapest, HUNGARY & Suresnes, FRANCE) C15H12N2O3S Paczal, A. et al. Structure-Activity Relationship of Azaindole-Based Glucokinase Activators. J. Med. Chem. (2016) 127038928 1191
GKA45-55 GKA45-55 GKA: Systemic 2016 Sulfoxide/Sulfone derivatives,Azaindole 304.79 3.02 Servier Research Institute (Budapest, HUNGARY & Suresnes, FRANCE) C15H13ClN2OS Paczal, A. et al. Structure-Activity Relationship of Azaindole-Based Glucokinase Activators. J. Med. Chem. (2016) 127039540 1192
GKA45-57 GKA45-57 GKA: Systemic 2016 Sulfoxide/Sulfone derivatives,Azaindole 403.93 4.92 Servier Research Institute (Budapest, HUNGARY & Suresnes, FRANCE) C20H22ClN3O2S Paczal, A. et al. Structure-Activity Relationship of Azaindole-Based Glucokinase Activators. J. Med. Chem. (2016) 127038536 1193
GKA46-1 GKA46-1 GKA: Hepatoselective 2017 Thiazole/Thiadiazole,Benzamide,Pyridine 546.67 4.11 Merck & Co. (USA) C21H18N6O4S4 Xu, J. et al. Discovery of orally active hepatoselective glucokinase activators for treatment of Type II Diabetes Mellitus. Bioorganic Med. Chem. Lett. (2017) 76902401 1195
GKA46-2 GKA46-2 GKA: Hepatoselective 2017 Thiazole/Thiadiazole,Benzamide,Pyridine 542.67 5.53 Merck & Co. (USA) C23H18N4O4S4 Xu, J. et al. Discovery of orally active hepatoselective glucokinase activators for treatment of Type II Diabetes Mellitus. Bioorganic Med. Chem. Lett. (2017) 76902786 1196
GKA46-3 GKA46-3 GKA: Hepatoselective 2017 Thiazole/Thiadiazole,Benzamide,Pyridine 524.63 4.89 Merck & Co. (USA) C24H20N4O4S3 Xu, J. et al. Discovery of orally active hepatoselective glucokinase activators for treatment of Type II Diabetes Mellitus. Bioorganic Med. Chem. Lett. (2017) 76902972 1197
GKA46-4 GKA46-4 GKA: Hepatoselective 2017 Thiazole/Thiadiazole,Benzamide,Pyridine 510.61 4.59 Merck & Co. (USA) C23H18N4O4S3 Xu, J. et al. Discovery of orally active hepatoselective glucokinase activators for treatment of Type II Diabetes Mellitus. Bioorganic Med. Chem. Lett. (2017) 76902974 1198
GKA46-5 GKA46-5 GKA: Hepatoselective 2017 Thiazole/Thiadiazole,Benzamide,Pyridine 545.05 5.55 Merck & Co. (USA) C23H17ClN4O4S3 Xu, J. et al. Discovery of orally active hepatoselective glucokinase activators for treatment of Type II Diabetes Mellitus. Bioorganic Med. Chem. Lett. (2017) 76902970 1199
GKA46-6 GKA46-6 GKA: Hepatoselective 2017 Thiazole/Thiadiazole,Benzamide,Pyridine 533.02 5.68 Merck & Co. (USA) C22H14ClFN4O3S3 Xu, J. et al. Discovery of orally active hepatoselective glucokinase activators for treatment of Type II Diabetes Mellitus. Bioorganic Med. Chem. Lett. (2017) 76900521 1200
GKA46-S GKA46-S GKA: Systemic 2017 Thiazole/Thiadiazole,Benzamide,Pyridine 428.51 2.88 Merck & Co. (USA) C16H12N8OS3 Xu, J. et al. Discovery of orally active hepatoselective glucokinase activators for treatment of Type II Diabetes Mellitus. Bioorganic Med. Chem. Lett. (2017) 10365275 1194
GKA47-10 GKA47-10 GKA: Systemic 2017 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 473.01 3.06 Takeda California Inc. (USA) C19H25ClN4O4S2 Cheruvallath, Z. S. et al. Discovery of potent and orally active 1,4-disubstituted indazoles as novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2017) 44513479 1206
GKA47-11 GKA47-11 GKA: Systemic 2017 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 498.98 3.45 Takeda California Inc. (USA) C20H20ClFN4O4S2 Cheruvallath, Z. S. et al. Discovery of potent and orally active 1,4-disubstituted indazoles as novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2017) 137634006 1207
GKA47-12 GKA47-12 GKA: Systemic 2017 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 444.54 2.25 Takeda California Inc. (USA) C18H25FN4O4S2 Cheruvallath, Z. S. et al. Discovery of potent and orally active 1,4-disubstituted indazoles as novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2017) 57964133 1208
GKA47-13 GKA47-13 GKA: Systemic 2017 Thiazole/Thiadiazole,Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 495.01 3.68 Takeda California Inc. (USA) C21H23ClN4O4S2 Cheruvallath, Z. S. et al. Discovery of potent and orally active 1,4-disubstituted indazoles as novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2017) 57963961 1209
GKA47-14 GKA47-14 GKA: Systemic 2017 Thiazole/Thiadiazole,Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 495.01 3.68 Takeda California Inc. (USA) C21H23ClN4O4S2 Cheruvallath, Z. S. et al. Discovery of potent and orally active 1,4-disubstituted indazoles as novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2017) 57964003 1210
GKA47-15 GKA47-15 GKA: Systemic 2017 Thiazole/Thiadiazole,Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 495.01 3.68 Takeda California Inc. (USA) C21H23ClN4O4S2 Cheruvallath, Z. S. et al. Discovery of potent and orally active 1,4-disubstituted indazoles as novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2017) 57964021 1211
GKA47-16 GKA47-16 GKA: Systemic 2017 Thiazole/Thiadiazole,Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 478.56 3.15 Takeda California Inc. (USA) C21H23FN4O4S2 Cheruvallath, Z. S. et al. Discovery of potent and orally active 1,4-disubstituted indazoles as novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2017) 57964129 1212
GKA47-17 GKA47-17 GKA: Systemic 2017 Pyrazine,Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 455.53 1.55 Takeda California Inc. (USA) C22H25N5O4S Cheruvallath, Z. S. et al. Discovery of potent and orally active 1,4-disubstituted indazoles as novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2017) 57964007 1213
GKA47-18 GKA47-18 GKA: Systemic 2017 Pyridine,Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 497.57 2.05 Takeda California Inc. (USA) C24H27N5O5S Cheruvallath, Z. S. et al. Discovery of potent and orally active 1,4-disubstituted indazoles as novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2017) 137642601 1214
GKA47-19 GKA47-19 GKA: Systemic 2017 Thiazole/Thiadiazole,Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 503.59 1.93 Takeda California Inc. (USA) C22H25N5O5S2 Cheruvallath, Z. S. et al. Discovery of potent and orally active 1,4-disubstituted indazoles as novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2017) 137638835 1215
GKA47-20 GKA47-20 GKA: Systemic 2017 Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 457.55 2 Takeda California Inc. (USA) C22H27N5O4S Cheruvallath, Z. S. et al. Discovery of potent and orally active 1,4-disubstituted indazoles as novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2017) 57963988 1216
GKA47-21 GKA47-21 GKA: Systemic 2017 Thiazole/Thiadiazole,Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 475.58 2.53 Takeda California Inc. (USA) C21H25N5O4S2 Cheruvallath, Z. S. et al. Discovery of potent and orally active 1,4-disubstituted indazoles as novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2017) 137646945 1217
GKA47-22 GKA47-22 GKA: Systemic 2017 Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 469.56 2.01 Takeda California Inc. (USA) C23H27N5O4S Cheruvallath, Z. S. et al. Discovery of potent and orally active 1,4-disubstituted indazoles as novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2017) 44513802 1218
GKA47-23 GKA47-23 GKA: Systemic 2017 Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 487.57 1.25 Takeda California Inc. (USA) C23H29N5O5S Cheruvallath, Z. S. et al. Discovery of potent and orally active 1,4-disubstituted indazoles as novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2017) 137640045 1219
GKA47-24 GKA47-24 GKA: Systemic 2017 Thiazole/Thiadiazole,Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 496.55 3.25 Takeda California Inc. (USA) C21H22F2N4O4S2 Cheruvallath, Z. S. et al. Discovery of potent and orally active 1,4-disubstituted indazoles as novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2017) 57963993 1220
GKA47-25 GKA47-25 GKA: Systemic 2017 Thiazole/Thiadiazole,Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 503.57 2.87 Takeda California Inc. (USA) C22H22FN5O4S2 Cheruvallath, Z. S. et al. Discovery of potent and orally active 1,4-disubstituted indazoles as novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2017) 87647891 1221
GKA47-26 GKA47-26 GKA: Systemic 2017 Thiazole/Thiadiazole,Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 521.58 2.03 Takeda California Inc. (USA) C22H24FN5O5S2 Cheruvallath, Z. S. et al. Discovery of potent and orally active 1,4-disubstituted indazoles as novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2017) 137648705 1222
GKA47-27 GKA47-27 GKA: Systemic 2017 Thiazole/Thiadiazole,Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 508.59 3.13 Takeda California Inc. (USA) C22H25FN4O5S2 Cheruvallath, Z. S. et al. Discovery of potent and orally active 1,4-disubstituted indazoles as novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2017) 57964111 1223
GKA47-28 GKA47-28 GKA: Systemic 2017 Thiazole/Thiadiazole,Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 494.56 2.8 Takeda California Inc. (USA) C21H23FN4O5S2 Cheruvallath, Z. S. et al. Discovery of potent and orally active 1,4-disubstituted indazoles as novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2017) 136017450 1224
GKA47-29 GKA47-29 GKA: Systemic 2017 Thiazole/Thiadiazole,Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 479.55 2.08 Takeda California Inc. (USA) C20H22FN5O4S2 Cheruvallath, Z. S. et al. Discovery of potent and orally active 1,4-disubstituted indazoles as novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2017) 56968094 1225
GKA47-30 GKA47-30 GKA: Systemic 2017 Thiazole/Thiadiazole,Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 479.55 2.42 Takeda California Inc. (USA) C20H22FN5O4S2 Cheruvallath, Z. S. et al. Discovery of potent and orally active 1,4-disubstituted indazoles as novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2017) 57964017 1226
GKA47-5 GKA47-5 GKA: Systemic 2017 Thiazole/Thiadiazole,Pyridone/Pyrimidone/Pyrazinone,Sulfoxide/Sulfone derivatives 463.61 4.01 Takeda California Inc. (USA) C22H29N3O4S2 Cheruvallath, Z. S. et al. Discovery of potent and orally active 1,4-disubstituted indazoles as novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2017) 24962521 1201
GKA47-6 GKA47-6 GKA: Systemic 2017 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 412.5 3.42 Takeda California Inc. (USA) C17H21FN4O3S2 Cheruvallath, Z. S. et al. Discovery of potent and orally active 1,4-disubstituted indazoles as novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2017) 57964125 1202
GKA47-7 GKA47-7 GKA: Systemic 2017 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 428.96 3.94 Takeda California Inc. (USA) C17H21ClN4O3S2 Cheruvallath, Z. S. et al. Discovery of potent and orally active 1,4-disubstituted indazoles as novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2017) 57964102 1203
GKA47-8 GKA47-8 GKA: Systemic 2017 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 428.5 1.82 Takeda California Inc. (USA) C17H21FN4O4S2 Cheruvallath, Z. S. et al. Discovery of potent and orally active 1,4-disubstituted indazoles as novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2017) 57963985 1204
GKA47-9 GKA47-9 GKA: Systemic 2017 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 444.96 2.34 Takeda California Inc. (USA) C17H21ClN4O4S2 Cheruvallath, Z. S. et al. Discovery of potent and orally active 1,4-disubstituted indazoles as novel allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2017) 57964104 1205
GKA48-1 GKA48-1 GKA: Systemic 2017 Thiazole/Thiadiazole 390.79 3.41 Advinus Therapeutics Ltd. (Pune, INDIA) C15H13ClF2N2O4S Deshpande, A. M. et al. Discovery of liver-directed glucokinase activator having anti-hyperglycemic effect without hypoglycemia. Eur. J. Med. Chem. (2017) 24957927 1228
GKA48-14a GKA48-14a GKA: Part of a hepatoselective lead optimization effort (see reference) 2017 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 600.05 4.7 Advinus Therapeutics Ltd. (Pune, INDIA) C25H24ClF2N3O6S2 Deshpande, A. M. et al. Discovery of liver-directed glucokinase activator having anti-hyperglycemic effect without hypoglycemia. Eur. J. Med. Chem. (2017) 1230
GKA48-14b GKA48-14b GKA: Part of a hepatoselective lead optimization effort (see reference) 2017 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 586.03 4.51 Advinus Therapeutics Ltd. (Pune, INDIA) C24H22ClF2N3O6S2 Deshpande, A. M. et al. Discovery of liver-directed glucokinase activator having anti-hyperglycemic effect without hypoglycemia. Eur. J. Med. Chem. (2017) 87075881 1231
GKA48-14c GKA48-14c GKA: Part of a hepatoselective lead optimization effort (see reference) 2017 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 629.65 5.44 Advinus Therapeutics Ltd. (Pune, INDIA) C29H25F2N3O7S2 Deshpande, A. M. et al. Discovery of liver-directed glucokinase activator having anti-hyperglycemic effect without hypoglycemia. Eur. J. Med. Chem. (2017) 87075941 1232
GKA48-14d GKA48-14d GKA: Part of a hepatoselective lead optimization effort (see reference) 2017 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 631.62 4.22 Advinus Therapeutics Ltd. (Pune, INDIA) C28H23F2N3O8S2 Deshpande, A. M. et al. Discovery of liver-directed glucokinase activator having anti-hyperglycemic effect without hypoglycemia. Eur. J. Med. Chem. (2017) 87075957 1233
GKA48-14e GKA48-14e GKA: Part of a hepatoselective lead optimization effort (see reference) 2017 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 615.62 5.08 Advinus Therapeutics Ltd. (Pune, INDIA) C28H23F2N3O7S2 Deshpande, A. M. et al. Discovery of liver-directed glucokinase activator having anti-hyperglycemic effect without hypoglycemia. Eur. J. Med. Chem. (2017) 87075980 1234
GKA48-25a GKA48-25a GKA: Hepatoselective 2017 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 586.58 5.24 Advinus Therapeutics Ltd. (Pune, INDIA) C27H20F2N2O7S2 Deshpande, A. M. et al. Discovery of liver-directed glucokinase activator having anti-hyperglycemic effect without hypoglycemia. Eur. J. Med. Chem. (2017) 137628629 1235
GKA48-25b GKA48-25b GKA: Part of a hepatoselective lead optimization effort (see reference) 2017 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 630.64 5.09 Advinus Therapeutics Ltd. (Pune, INDIA) C29H24F2N2O8S2 Deshpande, A. M. et al. Discovery of liver-directed glucokinase activator having anti-hyperglycemic effect without hypoglycemia. Eur. J. Med. Chem. (2017) 87075956 1236
GKA48-25c GKA48-25c GKA: Part of a hepatoselective lead optimization effort (see reference) 2017 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 586.58 5.24 Advinus Therapeutics Ltd. (Pune, INDIA) C27H20F2N2O7S2 Deshpande, A. M. et al. Discovery of liver-directed glucokinase activator having anti-hyperglycemic effect without hypoglycemia. Eur. J. Med. Chem. (2017) 56592015 1237
GKA48-25d GKA48-25d GKA: Part of a hepatoselective lead optimization effort (see reference) 2017 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 600.61 5.17 Advinus Therapeutics Ltd. (Pune, INDIA) C28H22F2N2O7S2 Deshpande, A. M. et al. Discovery of liver-directed glucokinase activator having anti-hyperglycemic effect without hypoglycemia. Eur. J. Med. Chem. (2017) 87075919 1238
GKA48-25e GKA48-25e GKA: Part of a hepatoselective lead optimization effort (see reference) 2017 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 584.61 5.33 Advinus Therapeutics Ltd. (Pune, INDIA) C28H22F2N2O6S2 Deshpande, A. M. et al. Discovery of liver-directed glucokinase activator having anti-hyperglycemic effect without hypoglycemia. Eur. J. Med. Chem. (2017) 87571224 1239
GKA48-25f GKA48-25f GKA: Part of a hepatoselective lead optimization effort (see reference) 2017 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 591.65 1.46 Advinus Therapeutics Ltd. (Pune, INDIA) C27H27F2N3O6S2 Deshpande, A. M. et al. Discovery of liver-directed glucokinase activator having anti-hyperglycemic effect without hypoglycemia. Eur. J. Med. Chem. (2017) 87571233 1240
GKA48-25g GKA48-25g GKA: Part of a hepatoselective lead optimization effort (see reference) 2017 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 577.62 1.56 Advinus Therapeutics Ltd. (Pune, INDIA) C26H25F2N3O6S2 Deshpande, A. M. et al. Discovery of liver-directed glucokinase activator having anti-hyperglycemic effect without hypoglycemia. Eur. J. Med. Chem. (2017) 87571470 1241
GKA48-25h GKA48-25h GKA: Part of a hepatoselective lead optimization effort (see reference) 2017 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 518.51 4.01 Advinus Therapeutics Ltd. (Pune, INDIA) C23H16F2N2O6S2 Deshpande, A. M. et al. Discovery of liver-directed glucokinase activator having anti-hyperglycemic effect without hypoglycemia. Eur. J. Med. Chem. (2017) 87573224 1242
GKA48-26 GKA48-26 GKA: Hepatoselective 2017 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 586.58 5.24 Advinus Therapeutics Ltd. (Pune, INDIA) C27H20F2N2O7S2 Deshpande, A. M. et al. Discovery of liver-directed glucokinase activator having anti-hyperglycemic effect without hypoglycemia. Eur. J. Med. Chem. (2017) 137628629 1243
GKA48-27 GKA48-27 GKA: Hepatoselective 2017 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 586.58 5.24 Advinus Therapeutics Ltd. (Pune, INDIA) C27H20F2N2O7S2 Deshpande, A. M. et al. Discovery of liver-directed glucokinase activator having anti-hyperglycemic effect without hypoglycemia. Eur. J. Med. Chem. (2017) 56589687 1244
GKA48-6 GKA48-6 GKA: Hepatoselective 2017 Thiazole/Thiadiazole 434.41 4.34 Advinus Therapeutics Ltd. (Pune, INDIA) C20H16F2N2O5S Deshpande, A. M. et al. Discovery of liver-directed glucokinase activator having anti-hyperglycemic effect without hypoglycemia. Eur. J. Med. Chem. (2017) 1229
GKA48-hit GKA48-hit GKA: Systemic 2017 Thiazole/Thiadiazole 332.75 3.91 Advinus Therapeutics Ltd. (Pune, INDIA) C13H11ClF2N2O2S Deshpande, A. M. et al. Discovery of liver-directed glucokinase activator having anti-hyperglycemic effect without hypoglycemia. Eur. J. Med. Chem. (2017) 24962688 1227
GKA49-5 GKA49-5 GKA: Systemic 2017 Pyridine 396.46 -0.56 Kazan Federal University & Volgograd State Medical University (RUSSIA) C18H24N2O6S Dzyurkevich, M. S. et al. Pyridoxine dipharmacophore derivatives as potent glucokinase activators for the treatment of type 2 diabetes mellitus. Sci. Rep. (2017) 142770867 1245
GKA49-6 GKA49-6 GKA: Systemic 2017 Pyridine 428.52 -0.52 Kazan Federal University & Volgograd State Medical University (RUSSIA) C18H24N2O6S2 Dzyurkevich, M. S. et al. Pyridoxine dipharmacophore derivatives as potent glucokinase activators for the treatment of type 2 diabetes mellitus. Sci. Rep. (2017) 142770863 1246
GKA49-7 GKA49-7 GKA: Systemic 2017 Pyridine,Sulfoxide/Sulfone derivatives 412.46 -1.84 Kazan Federal University & Volgograd State Medical University (RUSSIA) C18H24N2O7S Dzyurkevich, M. S. et al. Pyridoxine dipharmacophore derivatives as potent glucokinase activators for the treatment of type 2 diabetes mellitus. Sci. Rep. (2017) 160224050 1247
GKA49-8 GKA49-8 GKA: Systemic 2017 Pyridine,Sulfoxide/Sulfone derivatives 428.46 -1.83 Kazan Federal University & Volgograd State Medical University (RUSSIA) C18H24N2O8S Dzyurkevich, M. S. et al. Pyridoxine dipharmacophore derivatives as potent glucokinase activators for the treatment of type 2 diabetes mellitus. Sci. Rep. (2017) 142770865 1248
GKA50-40 GKA50-40 GKA: Systemic 2017 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 502.6 3.87 China Pharmaceutical University, Nanjing & Chinese Academy of Sciences, Shanghai (CHINA) C24H26N2O6S2 Wang, Z. et al. Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. Eur. J. Med. Chem. (2017) 122417311 1249
GKA50-41 GKA50-41 GKA: Systemic 2017 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 516.63 4.22 China Pharmaceutical University, Nanjing & Chinese Academy of Sciences, Shanghai (CHINA) C25H28N2O6S2 Wang, Z. et al. Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. Eur. J. Med. Chem. (2017) 122417386 1250
GKA50-42 GKA50-42 GKA: Systemic 2017 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 518.6 2.9 China Pharmaceutical University, Nanjing & Chinese Academy of Sciences, Shanghai (CHINA) C24H26N2O7S2 Wang, Z. et al. Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. Eur. J. Med. Chem. (2017) 122417306 1251
GKA50-43 GKA50-43 GKA: Systemic 2017 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 530.61 3.61 China Pharmaceutical University, Nanjing & Chinese Academy of Sciences, Shanghai (CHINA) C25H26N2O7S2 Wang, Z. et al. Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. Eur. J. Med. Chem. (2017) 122417307 1252
GKA50-44 GKA50-44 GKA: Systemic 2017 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 531.64 3.09 China Pharmaceutical University, Nanjing & Chinese Academy of Sciences, Shanghai (CHINA) C25H29N3O6S2 Wang, Z. et al. Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. Eur. J. Med. Chem. (2017) 122417314 1253
GKA50-45 GKA50-45 GKA: Systemic 2017 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 545.67 3.45 China Pharmaceutical University, Nanjing & Chinese Academy of Sciences, Shanghai (CHINA) C26H31N3O6S2 Wang, Z. et al. Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. Eur. J. Med. Chem. (2017) 122417289 1254
GKA50-46 GKA50-46 GKA: Systemic 2017 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 559.7 3.89 China Pharmaceutical University, Nanjing & Chinese Academy of Sciences, Shanghai (CHINA) C27H33N3O6S2 Wang, Z. et al. Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. Eur. J. Med. Chem. (2017) 122417309 1255
GKA50-47 GKA50-47 GKA: Systemic 2017 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 559.65 2.55 China Pharmaceutical University, Nanjing & Chinese Academy of Sciences, Shanghai (CHINA) C26H29N3O7S2 Wang, Z. et al. Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. Eur. J. Med. Chem. (2017) 122417334 1256
GKA50-48 GKA50-48 GKA: Systemic 2017 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 617.73 3.93 China Pharmaceutical University, Nanjing & Chinese Academy of Sciences, Shanghai (CHINA) C29H35N3O8S2 Wang, Z. et al. Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. Eur. J. Med. Chem. (2017) 145120681 1257
GKA50-49 GKA50-49 GKA: Systemic 2017 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 593.71 4.87 China Pharmaceutical University, Nanjing & Chinese Academy of Sciences, Shanghai (CHINA) C30H31N3O6S2 Wang, Z. et al. Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. Eur. J. Med. Chem. (2017) 122417331 1258
GKA50-50 GKA50-50 GKA: Systemic 2017 Thiazole/Thiadiazole,Benzamide,Pyridine,Sulfoxide/Sulfone derivatives 594.7 4.13 China Pharmaceutical University, Nanjing & Chinese Academy of Sciences, Shanghai (CHINA) C29H30N4O6S2 Wang, Z. et al. Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. Eur. J. Med. Chem. (2017) 122417336 1259
GKA50-51 GKA50-51 GKA: Systemic 2017 Thiazole/Thiadiazole,Benzamide,Pyridine,Sulfoxide/Sulfone derivatives 594.7 3.8 China Pharmaceutical University, Nanjing & Chinese Academy of Sciences, Shanghai (CHINA) C29H30N4O6S2 Wang, Z. et al. Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. Eur. J. Med. Chem. (2017) 122417387 1260
GKA50-52 GKA50-52 GKA: Systemic 2017 Thiazole/Thiadiazole,Benzamide,Pyridine,Sulfoxide/Sulfone derivatives 594.7 3.8 China Pharmaceutical University, Nanjing & Chinese Academy of Sciences, Shanghai (CHINA) C29H30N4O6S2 Wang, Z. et al. Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. Eur. J. Med. Chem. (2017) 122417341 1261
GKA50-53 GKA50-53 GKA: Systemic 2017 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 607.74 4.58 China Pharmaceutical University, Nanjing & Chinese Academy of Sciences, Shanghai (CHINA) C31H33N3O6S2 Wang, Z. et al. Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. Eur. J. Med. Chem. (2017) 122417292 1262
GKA50-54 GKA50-54 GKA: Systemic 2017 Thiazole/Thiadiazole,Benzamide,Pyridine,Sulfoxide/Sulfone derivatives 618.72 3.2 China Pharmaceutical University, Nanjing & Chinese Academy of Sciences, Shanghai (CHINA) C28H34N4O8S2 Wang, Z. et al. Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. Eur. J. Med. Chem. (2017) 145120691 1263
GKA50-55 GKA50-55 GKA: Systemic 2017 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 617.73 3.93 China Pharmaceutical University, Nanjing & Chinese Academy of Sciences, Shanghai (CHINA) C29H35N3O8S2 Wang, Z. et al. Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. Eur. J. Med. Chem. (2017) 145975820 1264
GKA50-56 GKA50-56 GKA: Systemic 2017 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 617.73 3.93 China Pharmaceutical University, Nanjing & Chinese Academy of Sciences, Shanghai (CHINA) C29H35N3O8S2 Wang, Z. et al. Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. Eur. J. Med. Chem. (2017) 122417381 1265
GKA50-57 GKA50-57 GKA: Systemic 2017 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 631.76 4.3 China Pharmaceutical University, Nanjing & Chinese Academy of Sciences, Shanghai (CHINA) C30H37N3O8S2 Wang, Z. et al. Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. Eur. J. Med. Chem. (2017) 145120731 1266
GKA50-58 GKA50-58 GKA: Systemic 2017 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 643.77 4.49 China Pharmaceutical University, Nanjing & Chinese Academy of Sciences, Shanghai (CHINA) C31H37N3O8S2 Wang, Z. et al. Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. Eur. J. Med. Chem. (2017) 145120712 1267
GKA50-59 GKA50-59 GKA: Systemic 2017 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 658.79 3.98 China Pharmaceutical University, Nanjing & Chinese Academy of Sciences, Shanghai (CHINA) C31H38N4O8S2 Wang, Z. et al. Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. Eur. J. Med. Chem. (2017) 145120713 1268
GKA50-60 GKA50-60 GKA: Systemic 2017 Thiazole/Thiadiazole,Benzamide 622.73 4.29 China Pharmaceutical University, Nanjing & Chinese Academy of Sciences, Shanghai (CHINA) C32H38N4O7S Wang, Z. et al. Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. Eur. J. Med. Chem. (2017) 145973008 1269
GKA50-61 GKA50-61 GKA: Systemic 2017 Thiazole/Thiadiazole,Benzamide 610.72 4.16 China Pharmaceutical University, Nanjing & Chinese Academy of Sciences, Shanghai (CHINA) C31H38N4O7S Wang, Z. et al. Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. Eur. J. Med. Chem. (2017) 122417291 1270
GKA50-62 GKA50-62 GKA: Systemic 2017 Thiazole/Thiadiazole,Benzamide,Pyridine 623.72 3.55 China Pharmaceutical University, Nanjing & Chinese Academy of Sciences, Shanghai (CHINA) C31H37N5O7S Wang, Z. et al. Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. Eur. J. Med. Chem. (2017) 122417335 1271
GKA50-63 GKA50-63 GKA: Systemic 2017 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 603.71 3.5 China Pharmaceutical University, Nanjing & Chinese Academy of Sciences, Shanghai (CHINA) C28H33N3O8S2 Wang, Z. et al. Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. Eur. J. Med. Chem. (2017) 145965258 1272
GKA50-64 GKA50-64 GKA: Systemic 2017 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 587.71 4.45 China Pharmaceutical University, Nanjing & Chinese Academy of Sciences, Shanghai (CHINA) C28H33N3O7S2 Wang, Z. et al. Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. Eur. J. Med. Chem. (2017) 145120693 1273
GKA50-65 GKA50-65 GKA: Systemic 2017 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 613.74 4.92 China Pharmaceutical University, Nanjing & Chinese Academy of Sciences, Shanghai (CHINA) C30H35N3O7S2 Wang, Z. et al. Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. Eur. J. Med. Chem. (2017) 145120718 1274
GKA50-66 GKA50-66 GKA: Systemic 2017 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 627.77 5.46 China Pharmaceutical University, Nanjing & Chinese Academy of Sciences, Shanghai (CHINA) C31H37N3O7S2 Wang, Z. et al. Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. Eur. J. Med. Chem. (2017) 145120732 1275
GKA50-67 GKA50-67 GKA: Systemic 2017 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 627.77 5.48 China Pharmaceutical University, Nanjing & Chinese Academy of Sciences, Shanghai (CHINA) C31H37N3O7S2 Wang, Z. et al. Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. Eur. J. Med. Chem. (2017) 145977772 1276
GKA50-68 GKA50-68 GKA: Systemic 2017 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 635.75 5.14 China Pharmaceutical University, Nanjing & Chinese Academy of Sciences, Shanghai (CHINA) C32H33N3O7S2 Wang, Z. et al. Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. Eur. J. Med. Chem. (2017) 145973011 1277
GKA50-69 GKA50-69 GKA: Systemic 2017 Thiazole/Thiadiazole,Benzamide 575.62 4.9 China Pharmaceutical University, Nanjing & Chinese Academy of Sciences, Shanghai (CHINA) C28H31F2N3O6S Wang, Z. et al. Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. Eur. J. Med. Chem. (2017) 122417310 1278
GKA50-70 GKA50-70 GKA: Systemic 2017 Thiazole/Thiadiazole,Benzamide 640.72 4.39 China Pharmaceutical University, Nanjing & Chinese Academy of Sciences, Shanghai (CHINA) C32H37FN4O7S Wang, Z. et al. Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. Eur. J. Med. Chem. (2017) 145978396 1279
GKA50-71 GKA50-71 GKA: Systemic 2017 Thiazole/Thiadiazole,Benzamide 622.73 4.29 China Pharmaceutical University, Nanjing & Chinese Academy of Sciences, Shanghai (CHINA) C32H38N4O7S Wang, Z. et al. Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. Eur. J. Med. Chem. (2017) 145973008 1280
GKA50-72 GKA50-72 GKA: Systemic 2017 Thiazole/Thiadiazole,Benzamide 622.73 4.29 China Pharmaceutical University, Nanjing & Chinese Academy of Sciences, Shanghai (CHINA) C32H38N4O7S Wang, Z. et al. Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. Eur. J. Med. Chem. (2017) 145977527 1281
GKA50-73 GKA50-73 GKA: Systemic 2017 Thiazole/Thiadiazole,Benzamide 522.62 2.97 China Pharmaceutical University, Nanjing & Chinese Academy of Sciences, Shanghai (CHINA) C27H30N4O5S Wang, Z. et al. Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. Eur. J. Med. Chem. (2017) 145964360 1282
GKA50-74 GKA50-74 GKA: Systemic 2017 Thiazole/Thiadiazole,Benzamide 580.65 3.3 China Pharmaceutical University, Nanjing & Chinese Academy of Sciences, Shanghai (CHINA) C29H32N4O7S Wang, Z. et al. Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. Eur. J. Med. Chem. (2017) 145971883 1283
GKA50-75 GKA50-75 GKA: Systemic 2017 Thiazole/Thiadiazole,Benzamide 594.68 3.67 China Pharmaceutical University, Nanjing & Chinese Academy of Sciences, Shanghai (CHINA) C30H34N4O7S Wang, Z. et al. Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. Eur. J. Med. Chem. (2017) 145976429 1284
GKA50-76 GKA50-76 GKA: Systemic 2017 Thiazole/Thiadiazole,Urea,Benzamide 593.69 2.91 China Pharmaceutical University, Nanjing & Chinese Academy of Sciences, Shanghai (CHINA) C30H35N5O6S Wang, Z. et al. Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. Eur. J. Med. Chem. (2017) 145964383 1285
GKA50-77 GKA50-77 GKA: Systemic 2017 Thiazole/Thiadiazole,Benzamide 580.7 3.29 China Pharmaceutical University, Nanjing & Chinese Academy of Sciences, Shanghai (CHINA) C30H36N4O6S Wang, Z. et al. Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. Eur. J. Med. Chem. (2017) 145978251 1286
GKA50-78 GKA50-78 GKA: Systemic 2017 Thiazole/Thiadiazole,Benzamide 566.67 2.76 China Pharmaceutical University, Nanjing & Chinese Academy of Sciences, Shanghai (CHINA) C29H34N4O6S Wang, Z. et al. Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. Eur. J. Med. Chem. (2017) 145978148 1287
GKA50-79 GKA50-79 GKA: Systemic 2017 Thiazole/Thiadiazole,Benzamide,Pyridine 599.7 4.48 China Pharmaceutical University, Nanjing & Chinese Academy of Sciences, Shanghai (CHINA) C32H33N5O5S Wang, Z. et al. Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. Eur. J. Med. Chem. (2017) 145965347 1288
GKA50-80 GKA50-80 GKA: Systemic 2017 Thiazole/Thiadiazole,Benzamide,Pyrimidine 600.69 3.83 China Pharmaceutical University, Nanjing & Chinese Academy of Sciences, Shanghai (CHINA) C31H32N6O5S Wang, Z. et al. Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. Eur. J. Med. Chem. (2017) 145967041 1289
GKA50-81 GKA50-81 GKA: Systemic 2017 Thiazole/Thiadiazole,Benzamide,Pyrimidine 600.69 3.83 China Pharmaceutical University, Nanjing & Chinese Academy of Sciences, Shanghai (CHINA) C31H32N6O5S Wang, Z. et al. Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. Eur. J. Med. Chem. (2017) 145964031 1290
GKA50-82 GKA50-82 GKA: Systemic 2017 Thiazole/Thiadiazole,Benzamide,Pyridone/Pyrimidone/Pyrazinone 615.7 3.22 China Pharmaceutical University, Nanjing & Chinese Academy of Sciences, Shanghai (CHINA) C32H33N5O6S Wang, Z. et al. Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. Eur. J. Med. Chem. (2017) 145978500 1291
GKA50-83 GKA50-83 GKA: Systemic 2017 Thiazole/Thiadiazole,Benzamide 622.73 4.29 China Pharmaceutical University, Nanjing & Chinese Academy of Sciences, Shanghai (CHINA) C32H38N4O7S Wang, Z. et al. Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. Eur. J. Med. Chem. (2017) 145975880 1292
GKA50-84 GKA50-84 GKA: Systemic 2017 Thiazole/Thiadiazole,Benzamide 622.73 5.01 China Pharmaceutical University, Nanjing & Chinese Academy of Sciences, Shanghai (CHINA) C32H38N4O7S Wang, Z. et al. Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. Eur. J. Med. Chem. (2017) 145974954 1293
GKA50-85 GKA50-85 GKA: Systemic 2017 Thiazole/Thiadiazole,Benzamide 608.71 3.75 China Pharmaceutical University, Nanjing & Chinese Academy of Sciences, Shanghai (CHINA) C31H36N4O7S Wang, Z. et al. Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation. Eur. J. Med. Chem. (2017) 145966971 1294
GKA5-1 GKA5-1 GKA: Part of a hepatoselective lead optimization effort (see reference) 2009 Benzamide,Benzo/Pyrido-thiazole 255.3 2.81 Novartis (USA) & Torrent research centre (India) C13H9N3OS Bebernitz, G. R. et al. Investigation of functionally liver selective glucokinase activators for the treatment of type 2 diabetes. J. Med. Chem. (2009) 45086952 87
GKA51-1 GKA51-1 GKA: Systemic 2017 Pyridine,Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 462.52 2.1 Merck & Co. (USA) C24H22N4O4S Xu, J. et al. Novel, highly potent systemic glucokinase activators for the treatment of Type 2 Diabetes Mellitus. Bioorganic Med. Chem. Lett. (2017) 77050669 1295
GKA51-1en GKA51-1en GKA: Systemic 2017 Pyridine,Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 462.52 2.1 Merck & Co. (USA) C24H22N4O4S Xu, J. et al. Novel, highly potent systemic glucokinase activators for the treatment of Type 2 Diabetes Mellitus. Bioorganic Med. Chem. Lett. (2017) 77050669 1296
GKA51-2 GKA51-2 GKA: Systemic 2017 Thiazole/Thiadiazole,Pyridine,Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 482.58 2.6 Merck & Co. (USA) C23H22N4O4S2 Xu, J. et al. Novel, highly potent systemic glucokinase activators for the treatment of Type 2 Diabetes Mellitus. Bioorganic Med. Chem. Lett. (2017) 137641773 1297
GKA51-2en GKA51-2en GKA: Systemic 2017 Thiazole/Thiadiazole,Pyridine,Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 482.58 2.6 Merck & Co. (USA) C23H22N4O4S2 Xu, J. et al. Novel, highly potent systemic glucokinase activators for the treatment of Type 2 Diabetes Mellitus. Bioorganic Med. Chem. Lett. (2017) 137641773 1298
GKA51-3 GKA51-3 GKA: Systemic 2017 Pyridine,Pyrimidine,Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 463.51 1.03 Merck & Co. (USA) C23H21N5O4S Xu, J. et al. Novel, highly potent systemic glucokinase activators for the treatment of Type 2 Diabetes Mellitus. Bioorganic Med. Chem. Lett. (2017) 137650798 1299
GKA5-13a GKA5-13a GKA: Part of a hepatoselective lead optimization effort (see reference) 2009 Benzo/Pyrido-thiazole,Sulfoxide/Sulfone derivatives 460.57 4.21 Novartis (USA) & Torrent research centre (India) C21H24N4O4S2 Bebernitz, G. R. et al. Investigation of functionally liver selective glucokinase activators for the treatment of type 2 diabetes. J. Med. Chem. (2009) 11532712 88
GKA5-13b GKA5-13b GKA: Part of a hepatoselective lead optimization effort (see reference) 2009 Benzo/Pyrido-thiazole,Sulfoxide/Sulfone derivatives 516.63 4.86 Novartis (USA) & Torrent research centre (India) C24H28N4O5S2 Bebernitz, G. R. et al. Investigation of functionally liver selective glucokinase activators for the treatment of type 2 diabetes. J. Med. Chem. (2009) 44475561 89
GKA5-13c GKA5-13c GKA: Part of a hepatoselective lead optimization effort (see reference) 2009 Benzo/Pyrido-thiazole,Sulfoxide/Sulfone derivatives 530.66 5.22 Novartis (USA) & Torrent research centre (India) C25H30N4O5S2 Bebernitz, G. R. et al. Investigation of functionally liver selective glucokinase activators for the treatment of type 2 diabetes. J. Med. Chem. (2009) 87548724 90
GKA51-3en GKA51-3en GKA: Systemic 2017 Pyridine,Pyrimidine,Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 463.51 1.03 Merck & Co. (USA) C23H21N5O4S Xu, J. et al. Novel, highly potent systemic glucokinase activators for the treatment of Type 2 Diabetes Mellitus. Bioorganic Med. Chem. Lett. (2017) 137650798 1300
GKA51-4 GKA51-4 GKA: Systemic 2017 Pyridine,Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 520.6 1.81 Merck & Co. (USA) C27H28N4O5S Xu, J. et al. Novel, highly potent systemic glucokinase activators for the treatment of Type 2 Diabetes Mellitus. Bioorganic Med. Chem. Lett. (2017) 137632890 1301
GKA5-14a GKA5-14a GKA: Part of a hepatoselective lead optimization effort (see reference) 2009 Benzo/Pyrido-thiazole,Sulfoxide/Sulfone derivatives 488.62 4.79 Novartis (USA) & Torrent research centre (India) C23H28N4O4S2 Bebernitz, G. R. et al. Investigation of functionally liver selective glucokinase activators for the treatment of type 2 diabetes. J. Med. Chem. (2009) 11540403 91
GKA5-14b GKA5-14b GKA: Part of a hepatoselective lead optimization effort (see reference) 2009 Benzo/Pyrido-thiazole,Sulfoxide/Sulfone derivatives 516.68 5.52 Novartis (USA) & Torrent research centre (India) C25H32N4O4S2 Bebernitz, G. R. et al. Investigation of functionally liver selective glucokinase activators for the treatment of type 2 diabetes. J. Med. Chem. (2009) 11613255 92
GKA5-14c GKA5-14c GKA: Part of a hepatoselective lead optimization effort (see reference) 2009 Benzo/Pyrido-thiazole,Sulfoxide/Sulfone derivatives 544.73 6.58 Novartis (USA) & Torrent research centre (India) C27H36N4O4S2 Bebernitz, G. R. et al. Investigation of functionally liver selective glucokinase activators for the treatment of type 2 diabetes. J. Med. Chem. (2009) 11555724 93
GKA5-14d GKA5-14d GKA: Part of a hepatoselective lead optimization effort (see reference) 2009 Benzo/Pyrido-thiazole,Sulfoxide/Sulfone derivatives 544.73 6.39 Novartis (USA) & Torrent research centre (India) C27H36N4O4S2 Bebernitz, G. R. et al. Investigation of functionally liver selective glucokinase activators for the treatment of type 2 diabetes. J. Med. Chem. (2009) 11599178 94
GKA5-14e GKA5-14e GKA: Part of a hepatoselective lead optimization effort (see reference) 2009 Benzo/Pyrido-thiazole,Sulfoxide/Sulfone derivatives 572.78 7.29 Novartis (USA) & Torrent research centre (India) C29H40N4O4S2 Bebernitz, G. R. et al. Investigation of functionally liver selective glucokinase activators for the treatment of type 2 diabetes. J. Med. Chem. (2009) 11642675 95
GKA51-4en GKA51-4en GKA: Systemic 2017 Pyridine,Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 520.6 1.81 Merck & Co. (USA) C27H28N4O5S Xu, J. et al. Novel, highly potent systemic glucokinase activators for the treatment of Type 2 Diabetes Mellitus. Bioorganic Med. Chem. Lett. (2017) 137632890 1302
GKA5-14f GKA5-14f GKA: Part of a hepatoselective lead optimization effort (see reference) 2009 Benzo/Pyrido-thiazole,Sulfoxide/Sulfone derivatives 536.67 6.16 Novartis (USA) & Torrent research centre (India) C27H28N4O4S2 Bebernitz, G. R. et al. Investigation of functionally liver selective glucokinase activators for the treatment of type 2 diabetes. J. Med. Chem. (2009) 11512165 96
GKA5-14g GKA5-14g GKA: Part of a hepatoselective lead optimization effort (see reference) 2009 Pyridine,Benzo/Pyrido-thiazole,Sulfoxide/Sulfone derivatives 537.65 5.09 Novartis (USA) & Torrent research centre (India) C26H27N5O4S2 Bebernitz, G. R. et al. Investigation of functionally liver selective glucokinase activators for the treatment of type 2 diabetes. J. Med. Chem. (2009) 11635201 97
GKA5-14h GKA5-14h GKA: Part of a hepatoselective lead optimization effort (see reference) 2009 Benzo/Pyrido-thiazole,Sulfoxide/Sulfone derivatives 542.71 6.42 Novartis (USA) & Torrent research centre (India) C27H34N4O4S2 Bebernitz, G. R. et al. Investigation of functionally liver selective glucokinase activators for the treatment of type 2 diabetes. J. Med. Chem. (2009) 11706571 98
GKA5-14i GKA5-14i GKA: Part of a hepatoselective lead optimization effort (see reference) 2009 Benzo/Pyrido-thiazole,Sulfoxide/Sulfone derivatives 544.69 5.01 Novartis (USA) & Torrent research centre (India) C26H32N4O5S2 Bebernitz, G. R. et al. Investigation of functionally liver selective glucokinase activators for the treatment of type 2 diabetes. J. Med. Chem. (2009) 44475562 99
GKA5-14j GKA5-14j GKA: Part of a hepatoselective lead optimization effort (see reference) 2009 Benzo/Pyrido-thiazole,Sulfoxide/Sulfone derivatives 500.63 5.16 Novartis (USA) & Torrent research centre (India) C24H28N4O4S2 Bebernitz, G. R. et al. Investigation of functionally liver selective glucokinase activators for the treatment of type 2 diabetes. J. Med. Chem. (2009) 11677751 100
GKA5-14k GKA5-14k GKA: Part of a hepatoselective lead optimization effort (see reference) 2009 Benzo/Pyrido-thiazole,Sulfoxide/Sulfone derivatives 550.69 6.1 Novartis (USA) & Torrent research centre (India) C28H30N4O4S2 Bebernitz, G. R. et al. Investigation of functionally liver selective glucokinase activators for the treatment of type 2 diabetes. J. Med. Chem. (2009) 11563014 101
GKA5-14l GKA5-14l GKA: Part of a hepatoselective lead optimization effort (see reference) 2009 Pyridine,Benzo/Pyrido-thiazole,Sulfoxide/Sulfone derivatives 551.68 5.03 Novartis (USA) & Torrent research centre (India) C27H29N5O4S2 Bebernitz, G. R. et al. Investigation of functionally liver selective glucokinase activators for the treatment of type 2 diabetes. J. Med. Chem. (2009) 11649700 102
GKA5-14m GKA5-14m GKA: Part of a hepatoselective lead optimization effort (see reference) 2009 Pyridine,Benzo/Pyrido-thiazole,Sulfoxide/Sulfone derivatives 551.68 5.03 Novartis (USA) & Torrent research centre (India) C27H29N5O4S2 Bebernitz, G. R. et al. Investigation of functionally liver selective glucokinase activators for the treatment of type 2 diabetes. J. Med. Chem. (2009) 11541271 103
GKA5-14n GKA5-14n GKA: Part of a hepatoselective lead optimization effort (see reference) 2009 Pyridine,Benzo/Pyrido-thiazole,Sulfoxide/Sulfone derivatives 551.68 5.07 Novartis (USA) & Torrent research centre (India) C27H29N5O4S2 Bebernitz, G. R. et al. Investigation of functionally liver selective glucokinase activators for the treatment of type 2 diabetes. J. Med. Chem. (2009) 11563024 104
GKA5-14o GKA5-14o GKA: Part of a hepatoselective lead optimization effort (see reference) 2009 Benzo/Pyrido-thiazole,Sulfoxide/Sulfone derivatives 540.65 5.2 Novartis (USA) & Torrent research centre (India) C26H28N4O5S2 Bebernitz, G. R. et al. Investigation of functionally liver selective glucokinase activators for the treatment of type 2 diabetes. J. Med. Chem. (2009) 11519518 105
GKA5-14p GKA5-14p GKA: Part of a hepatoselective lead optimization effort (see reference) 2009 Benzo/Pyrido-thiazole,Sulfoxide/Sulfone derivatives 556.72 5.82 Novartis (USA) & Torrent research centre (India) C26H28N4O4S3 Bebernitz, G. R. et al. Investigation of functionally liver selective glucokinase activators for the treatment of type 2 diabetes. J. Med. Chem. (2009) 11713787 106
GKA51-5 GKA51-5 GKA: Systemic 2017 Pyridine,Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 530.52 2.99 Merck & Co. (USA) C25H21F3N4O4S Xu, J. et al. Novel, highly potent systemic glucokinase activators for the treatment of Type 2 Diabetes Mellitus. Bioorganic Med. Chem. Lett. (2017) 137646747 1303
GKA5-15a GKA5-15a GKA: Part of a hepatoselective lead optimization effort (see reference) 2009 Benzo/Pyrido-thiazole,Sulfoxide/Sulfone derivatives 518.65 4.46 Novartis (USA) & Torrent research centre (India) C24H30N4O5S2 Bebernitz, G. R. et al. Investigation of functionally liver selective glucokinase activators for the treatment of type 2 diabetes. J. Med. Chem. (2009) 11692099 107
GKA5-15b GKA5-15b GKA: Part of a hepatoselective lead optimization effort (see reference) 2009 Benzo/Pyrido-thiazole,Sulfoxide/Sulfone derivatives 531.69 4.64 Novartis (USA) & Torrent research centre (India) C25H33N5O4S2 Bebernitz, G. R. et al. Investigation of functionally liver selective glucokinase activators for the treatment of type 2 diabetes. J. Med. Chem. (2009) 11591855 108
GKA5-15c GKA5-15c GKA: Part of a hepatoselective lead optimization effort (see reference) 2009 Benzo/Pyrido-thiazole,Sulfoxide/Sulfone derivatives 518.61 4.2 Novartis (USA) & Torrent research centre (India) C23H26N4O6S2 Bebernitz, G. R. et al. Investigation of functionally liver selective glucokinase activators for the treatment of type 2 diabetes. J. Med. Chem. (2009) 87782394 109
GKA5-15d GKA5-15d GKA: Part of a hepatoselective lead optimization effort (see reference) 2009 Benzo/Pyrido-thiazole,Sulfoxide/Sulfone derivatives 532.63 4.1 Novartis (USA) & Torrent research centre (India) C24H28N4O6S2 Bebernitz, G. R. et al. Investigation of functionally liver selective glucokinase activators for the treatment of type 2 diabetes. J. Med. Chem. (2009) 44475563 110
GKA51-5en GKA51-5en GKA: Systemic 2017 Pyridine,Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 530.52 2.99 Merck & Co. (USA) C25H21F3N4O4S Xu, J. et al. Novel, highly potent systemic glucokinase activators for the treatment of Type 2 Diabetes Mellitus. Bioorganic Med. Chem. Lett. (2017) 137646747 1304
GKA5-16a GKA5-16a GKA: Part of a hepatoselective lead optimization effort (see reference) 2009 Benzo/Pyrido-thiazole,Sulfoxide/Sulfone derivatives 564.72 6.28 Novartis (USA) & Torrent research centre (India) C29H32N4O4S2 Bebernitz, G. R. et al. Investigation of functionally liver selective glucokinase activators for the treatment of type 2 diabetes. J. Med. Chem. (2009) 11664117 111
GKA5-16b GKA5-16b GKA: Part of a hepatoselective lead optimization effort (see reference) 2009 Benzo/Pyrido-thiazole,Sulfoxide/Sulfone derivatives 554.68 5.38 Novartis (USA) & Torrent research centre (India) C27H30N4O5S2 Bebernitz, G. R. et al. Investigation of functionally liver selective glucokinase activators for the treatment of type 2 diabetes. J. Med. Chem. (2009) 44474003 112
GKA5-16c GKA5-16c GKA: Part of a hepatoselective lead optimization effort (see reference) 2009 Benzo/Pyrido-thiazole,Sulfoxide/Sulfone derivatives 518.65 4.11 Novartis (USA) & Torrent research centre (India) C24H30N4O5S2 Bebernitz, G. R. et al. Investigation of functionally liver selective glucokinase activators for the treatment of type 2 diabetes. J. Med. Chem. (2009) 11548098 113
GKA5-16d GKA5-16d GKA: Part of a hepatoselective lead optimization effort (see reference) 2009 Benzo/Pyrido-thiazole,Sulfoxide/Sulfone derivatives 568.71 4.41 Novartis (USA) & Torrent research centre (India) C27H32N6O4S2 Bebernitz, G. R. et al. Investigation of functionally liver selective glucokinase activators for the treatment of type 2 diabetes. J. Med. Chem. (2009) 44474164 114
GKA51-6rac GKA51-6rac GKA: Systemic 2017 Pyridine,Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 520.56 1.95 Merck & Co. (USA) C26H24N4O6S Xu, J. et al. Novel, highly potent systemic glucokinase activators for the treatment of Type 2 Diabetes Mellitus. Bioorganic Med. Chem. Lett. (2017) 90253114 1305
GKA51-7 GKA51-7 GKA: Systemic 2017 Pyridine,Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 543.56 4.09 Merck & Co. (USA) C27H24F3N3O4S Xu, J. et al. Novel, highly potent systemic glucokinase activators for the treatment of Type 2 Diabetes Mellitus. Bioorganic Med. Chem. Lett. (2017) 137642011 1306
GKA5-17a GKA5-17a GKA: Part of a hepatoselective lead optimization effort (see reference) 2009 Benzo/Pyrido-thiazole,Sulfoxide/Sulfone derivatives 528.69 5.63 Novartis (USA) & Torrent research centre (India) C26H32N4O4S2 Bebernitz, G. R. et al. Investigation of functionally liver selective glucokinase activators for the treatment of type 2 diabetes. J. Med. Chem. (2009) 11577339 115
GKA5-17b GKA5-17b GKA: Part of a hepatoselective lead optimization effort (see reference) 2009 Benzo/Pyrido-thiazole,Sulfoxide/Sulfone derivatives 530.66 4.42 Novartis (USA) & Torrent research centre (India) C25H30N4O5S2 Bebernitz, G. R. et al. Investigation of functionally liver selective glucokinase activators for the treatment of type 2 diabetes. J. Med. Chem. (2009) 11720695 116
GKA5-17c__-R_ GKA5-17c (R) GKA: Hepatoselective 2009 Benzo/Pyrido-thiazole,Sulfoxide/Sulfone derivatives 543.7 4.6 Novartis (USA) & Torrent research centre (India) C26H33N5O4S2 Bebernitz, G. R. et al. Investigation of functionally liver selective glucokinase activators for the treatment of type 2 diabetes. J. Med. Chem. (2009) 44224002 118
GKA5-17c GKA5-17c (racemic) GKA: Hepatoselective 2009 Benzo/Pyrido-thiazole,Sulfoxide/Sulfone derivatives 543.7 4.6 Novartis (USA) & Torrent research centre (India) C26H33N5O4S2 Bebernitz, G. R. et al. Investigation of functionally liver selective glucokinase activators for the treatment of type 2 diabetes. J. Med. Chem. (2009) 44224002 117
GKA5-17d GKA5-17d GKA: Part of a hepatoselective lead optimization effort (see reference) 2009 Benzo/Pyrido-thiazole,Sulfoxide/Sulfone derivatives 529.67 4.13 Novartis (USA) & Torrent research centre (India) C25H31N5O4S2 Bebernitz, G. R. et al. Investigation of functionally liver selective glucokinase activators for the treatment of type 2 diabetes. J. Med. Chem. (2009) 11519759 119
GKA51-8 GKA51-8 GKA: Systemic 2017 Pyridine,Indole/Benzimidazole/Indazole 523.5 4.7 Merck & Co. (USA) C28H24F3N3O4 Xu, J. et al. Novel, highly potent systemic glucokinase activators for the treatment of Type 2 Diabetes Mellitus. Bioorganic Med. Chem. Lett. (2017) 137632657 1307
GKA51-9 GKA51-9 GKA: Systemic 2017 Pyridine,Indole/Benzimidazole/Indazole 495.45 4.01 Merck & Co. (USA) C26H20F3N3O4 Xu, J. et al. Novel, highly potent systemic glucokinase activators for the treatment of Type 2 Diabetes Mellitus. Bioorganic Med. Chem. Lett. (2017) 137655205 1308
GKA52-1 GKA52-1 GKA: Systemic 2017 Pyridine,Phosphonate 473.48 5.11 Sri Venkateswara University (Tirupati, INDIA) C24H29FN3O4P Yellapu, N. K., Kilaru, R. B., Chamarthi, N., PVGK, S. & Matcha, B. Structure based design, synthesis and biological evaluation of amino phosphonate derivatives as human glucokinase activators. Comput. Biol. Chem. (2017) 1309
GKA52-10 GKA52-10 GKA: Systemic 2017 Phosphonate 432.47 0.88 Sri Venkateswara University (Tirupati, INDIA) C20H34FN2O5P Yellapu, N. K., Kilaru, R. B., Chamarthi, N., PVGK, S. & Matcha, B. Structure based design, synthesis and biological evaluation of amino phosphonate derivatives as human glucokinase activators. Comput. Biol. Chem. (2017) 1318
GKA52-11 GKA52-11 GKA: Systemic 2017 Thiazole/Thiadiazole,Phosphonate 561.63 4.81 Sri Venkateswara University (Tirupati, INDIA) C27H36N3O6PS Yellapu, N. K., Kilaru, R. B., Chamarthi, N., PVGK, S. & Matcha, B. Structure based design, synthesis and biological evaluation of amino phosphonate derivatives as human glucokinase activators. Comput. Biol. Chem. (2017) 1319
GKA52-12 GKA52-12 GKA: Systemic 2017 Thiazole/Thiadiazole,Phosphonate 612.66 4.14 Sri Venkateswara University (Tirupati, INDIA) C25H33N4O8PS2 Yellapu, N. K., Kilaru, R. B., Chamarthi, N., PVGK, S. & Matcha, B. Structure based design, synthesis and biological evaluation of amino phosphonate derivatives as human glucokinase activators. Comput. Biol. Chem. (2017) 1320
GKA52-13 GKA52-13 GKA: Systemic 2017 Thiazole/Thiadiazole,Phosphonate 695.77 5.46 Sri Venkateswara University (Tirupati, INDIA) C28H34N5O8PS3 Yellapu, N. K., Kilaru, R. B., Chamarthi, N., PVGK, S. & Matcha, B. Structure based design, synthesis and biological evaluation of amino phosphonate derivatives as human glucokinase activators. Comput. Biol. Chem. (2017) 1321
GKA52-14 GKA52-14 GKA: Systemic 2017 Thiazole/Thiadiazole,Urea,Pyridone/Pyrimidone/Pyrazinone,Phosphonate 683.67 1.44 Sri Venkateswara University (Tirupati, INDIA) C28H38N5O11PS Yellapu, N. K., Kilaru, R. B., Chamarthi, N., PVGK, S. & Matcha, B. Structure based design, synthesis and biological evaluation of amino phosphonate derivatives as human glucokinase activators. Comput. Biol. Chem. (2017) 1322
GKA52-15 GKA52-15 GKA: Systemic 2017 Thiazole/Thiadiazole,Phosphonate 513.59 4.24 Sri Venkateswara University (Tirupati, INDIA) C23H36N3O6PS Yellapu, N. K., Kilaru, R. B., Chamarthi, N., PVGK, S. & Matcha, B. Structure based design, synthesis and biological evaluation of amino phosphonate derivatives as human glucokinase activators. Comput. Biol. Chem. (2017) 1323
GKA52-16 GKA52-16 GKA: Systemic 2017 Pyridine,Phosphonate 411.41 3.98 Sri Venkateswara University (Tirupati, INDIA) C19H27FN3O4P Yellapu, N. K., Kilaru, R. B., Chamarthi, N., PVGK, S. & Matcha, B. Structure based design, synthesis and biological evaluation of amino phosphonate derivatives as human glucokinase activators. Comput. Biol. Chem. (2017) 1324
GKA52-17 GKA52-17 GKA: Systemic 2017 Pyridine,Phosphonate 471.49 4.65 Sri Venkateswara University (Tirupati, INDIA) C24H30N3O5P Yellapu, N. K., Kilaru, R. B., Chamarthi, N., PVGK, S. & Matcha, B. Structure based design, synthesis and biological evaluation of amino phosphonate derivatives as human glucokinase activators. Comput. Biol. Chem. (2017) 1325
GKA52-18 GKA52-18 GKA: Systemic 2017 Thiazole/Thiadiazole,Phosphonate 621.68 4.81 Sri Venkateswara University (Tirupati, INDIA) C29H40N3O8PS Yellapu, N. K., Kilaru, R. B., Chamarthi, N., PVGK, S. & Matcha, B. Structure based design, synthesis and biological evaluation of amino phosphonate derivatives as human glucokinase activators. Comput. Biol. Chem. (2017) 1326
GKA52-19 GKA52-19 GKA: Systemic 2017 Phosphonate 346.38 3.05 Sri Venkateswara University (Tirupati, INDIA) C16H28FN2O3P Yellapu, N. K., Kilaru, R. B., Chamarthi, N., PVGK, S. & Matcha, B. Structure based design, synthesis and biological evaluation of amino phosphonate derivatives as human glucokinase activators. Comput. Biol. Chem. (2017) 1327
GKA52-2 GKA52-2 GKA: Systemic 2017 Thiazole/Thiadiazole,Indole/Benzimidazole/Indazole,Phosphonate 602.68 4.77 Sri Venkateswara University (Tirupati, INDIA) C29H39N4O6PS Yellapu, N. K., Kilaru, R. B., Chamarthi, N., PVGK, S. & Matcha, B. Structure based design, synthesis and biological evaluation of amino phosphonate derivatives as human glucokinase activators. Comput. Biol. Chem. (2017) 1310
GKA52-3 GKA52-3 GKA: Systemic 2017 Thiazole/Thiadiazole,Pyridine,Phosphonate 640.69 6.3 Sri Venkateswara University (Tirupati, INDIA) C31H37N4O7PS Yellapu, N. K., Kilaru, R. B., Chamarthi, N., PVGK, S. & Matcha, B. Structure based design, synthesis and biological evaluation of amino phosphonate derivatives as human glucokinase activators. Comput. Biol. Chem. (2017) 1311
GKA52-4 GKA52-4 GKA: Systemic 2017 Thiazole/Thiadiazole,Urea,Pyridone/Pyrimidone/Pyrazinone,Phosphonate 687.7 3.18 Sri Venkateswara University (Tirupati, INDIA) C27H35FN5O9PS2 Yellapu, N. K., Kilaru, R. B., Chamarthi, N., PVGK, S. & Matcha, B. Structure based design, synthesis and biological evaluation of amino phosphonate derivatives as human glucokinase activators. Comput. Biol. Chem. (2017) 1312
GKA52-5 GKA52-5 GKA: Systemic 2017 Phosphonate 560.45 1.34 Sri Venkateswara University (Tirupati, INDIA) C21H31FN6O7P2 Yellapu, N. K., Kilaru, R. B., Chamarthi, N., PVGK, S. & Matcha, B. Structure based design, synthesis and biological evaluation of amino phosphonate derivatives as human glucokinase activators. Comput. Biol. Chem. (2017) 1313
GKA52-6 GKA52-6 GKA: Systemic 2017 Thiazole/Thiadiazole,Pyridine,Phosphonate 578.62 4.62 Sri Venkateswara University (Tirupati, INDIA) C26H35N4O7PS Yellapu, N. K., Kilaru, R. B., Chamarthi, N., PVGK, S. & Matcha, B. Structure based design, synthesis and biological evaluation of amino phosphonate derivatives as human glucokinase activators. Comput. Biol. Chem. (2017) 1314
GKA52-7 GKA52-7 GKA: Systemic 2017 Thiazole/Thiadiazole,Phosphonate 727.66 2.53 Sri Venkateswara University (Tirupati, INDIA) C28H39N7O10P2S Yellapu, N. K., Kilaru, R. B., Chamarthi, N., PVGK, S. & Matcha, B. Structure based design, synthesis and biological evaluation of amino phosphonate derivatives as human glucokinase activators. Comput. Biol. Chem. (2017) 1315
GKA52-8 GKA52-8 GKA: Systemic 2017 Thiazole/Thiadiazole,Phosphonate 623.7 6.1 Sri Venkateswara University (Tirupati, INDIA) C32H38N3O6PS Yellapu, N. K., Kilaru, R. B., Chamarthi, N., PVGK, S. & Matcha, B. Structure based design, synthesis and biological evaluation of amino phosphonate derivatives as human glucokinase activators. Comput. Biol. Chem. (2017) 1316
GKA52-9 GKA52-9 GKA: Systemic 2017 Phosphonate 483.5 4.64 Sri Venkateswara University (Tirupati, INDIA) C25H30N3O5P Yellapu, N. K., Kilaru, R. B., Chamarthi, N., PVGK, S. & Matcha, B. Structure based design, synthesis and biological evaluation of amino phosphonate derivatives as human glucokinase activators. Comput. Biol. Chem. (2017) 1317
GKA53-DPAA GKA53-DPAA GKA: Systemic 2018 Cadmium carboxylate 534.88 6.78 Riphah International University (Islamabad, PAKISTAN) C28H22CdO4 Bano, S. et al. Computational and pharmacological evaluation of ferrocene-based acyl ureas and homoleptic cadmium carboxylate derivatives for anti-diabetic potential. Front. Pharmacol. (2018) 1328
GKA53-DPC1 GKA53-DPC1 GKA: Systemic 2018 Urea,Benzamide,Ferrocene 458.72 5.91 Riphah International University (Islamabad, PAKISTAN) C24H19ClFeN2O2 Bano, S. et al. Computational and pharmacological evaluation of ferrocene-based acyl ureas and homoleptic cadmium carboxylate derivatives for anti-diabetic potential. Front. Pharmacol. (2018) 1329
GKA54-1 GKA54-1 GKA: Systemic 2018 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 359.42 2.64 JCDM College of Pharmacy (Sirsa, INDIA) C16H13N3O3S2 Charaya, N., Pandita, D., Grewal, A. S. & Lather, V. Design, synthesis and biological evaluation of novel thiazol-2-yl benzamide derivatives as glucokinase activators. Comput. Biol. Chem. (2018) 19257320 1330
GKA54-10 GKA54-10 GKA: Systemic 2018 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 415.53 4.01 JCDM College of Pharmacy (Sirsa, INDIA) C20H21N3O3S2 Charaya, N., Pandita, D., Grewal, A. S. & Lather, V. Design, synthesis and biological evaluation of novel thiazol-2-yl benzamide derivatives as glucokinase activators. Comput. Biol. Chem. (2018) 1339
GKA54-11 GKA54-11 GKA: Systemic 2018 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 479.57 4.64 JCDM College of Pharmacy (Sirsa, INDIA) C24H21N3O4S2 Charaya, N., Pandita, D., Grewal, A. S. & Lather, V. Design, synthesis and biological evaluation of novel thiazol-2-yl benzamide derivatives as glucokinase activators. Comput. Biol. Chem. (2018) 1340
GKA54-12 GKA54-12 GKA: Systemic 2018 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 524.57 5.02 JCDM College of Pharmacy (Sirsa, INDIA) C24H20N4O6S2 Charaya, N., Pandita, D., Grewal, A. S. & Lather, V. Design, synthesis and biological evaluation of novel thiazol-2-yl benzamide derivatives as glucokinase activators. Comput. Biol. Chem. (2018) 1341
GKA54-13 GKA54-13 GKA: Systemic 2018 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 514.02 5.27 JCDM College of Pharmacy (Sirsa, INDIA) C24H20ClN3O4S2 Charaya, N., Pandita, D., Grewal, A. S. & Lather, V. Design, synthesis and biological evaluation of novel thiazol-2-yl benzamide derivatives as glucokinase activators. Comput. Biol. Chem. (2018) 1342
GKA54-14 GKA54-14 GKA: Systemic 2018 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 431.53 3.45 JCDM College of Pharmacy (Sirsa, INDIA) C20H21N3O4S2 Charaya, N., Pandita, D., Grewal, A. S. & Lather, V. Design, synthesis and biological evaluation of novel thiazol-2-yl benzamide derivatives as glucokinase activators. Comput. Biol. Chem. (2018) 1343
GKA54-15 GKA54-15 GKA: Systemic 2018 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 445.56 3.98 JCDM College of Pharmacy (Sirsa, INDIA) C21H23N3O4S2 Charaya, N., Pandita, D., Grewal, A. S. & Lather, V. Design, synthesis and biological evaluation of novel thiazol-2-yl benzamide derivatives as glucokinase activators. Comput. Biol. Chem. (2018) 1344
GKA54-16 GKA54-16 GKA: Systemic 2018 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 417.5 3.09 JCDM College of Pharmacy (Sirsa, INDIA) C19H19N3O4S2 Charaya, N., Pandita, D., Grewal, A. S. & Lather, V. Design, synthesis and biological evaluation of novel thiazol-2-yl benzamide derivatives as glucokinase activators. Comput. Biol. Chem. (2018) 1345
GKA54-2 GKA54-2 GKA: Systemic 2018 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 404.42 3.03 JCDM College of Pharmacy (Sirsa, INDIA) C16H12N4O5S2 Charaya, N., Pandita, D., Grewal, A. S. & Lather, V. Design, synthesis and biological evaluation of novel thiazol-2-yl benzamide derivatives as glucokinase activators. Comput. Biol. Chem. (2018) 1331
GKA54-3 GKA54-3 GKA: Systemic 2018 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 393.87 3.27 JCDM College of Pharmacy (Sirsa, INDIA) C16H12ClN3O3S2 Charaya, N., Pandita, D., Grewal, A. S. & Lather, V. Design, synthesis and biological evaluation of novel thiazol-2-yl benzamide derivatives as glucokinase activators. Comput. Biol. Chem. (2018) 18105280 1332
GKA54-4 GKA54-4 GKA: Systemic 2018 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 311.38 1.45 JCDM College of Pharmacy (Sirsa, INDIA) C12H13N3O3S2 Charaya, N., Pandita, D., Grewal, A. S. & Lather, V. Design, synthesis and biological evaluation of novel thiazol-2-yl benzamide derivatives as glucokinase activators. Comput. Biol. Chem. (2018) 133758445 1333
GKA54-5 GKA54-5 GKA: Systemic 2018 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 325.41 1.98 JCDM College of Pharmacy (Sirsa, INDIA) C13H15N3O3S2 Charaya, N., Pandita, D., Grewal, A. S. & Lather, V. Design, synthesis and biological evaluation of novel thiazol-2-yl benzamide derivatives as glucokinase activators. Comput. Biol. Chem. (2018) 1334
GKA54-6 GKA54-6 GKA: Systemic 2018 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 449.55 4.67 JCDM College of Pharmacy (Sirsa, INDIA) C23H19N3O3S2 Charaya, N., Pandita, D., Grewal, A. S. & Lather, V. Design, synthesis and biological evaluation of novel thiazol-2-yl benzamide derivatives as glucokinase activators. Comput. Biol. Chem. (2018) 1335
GKA54-7 GKA54-7 GKA: Systemic 2018 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 494.54 5.05 JCDM College of Pharmacy (Sirsa, INDIA) C23H18N4O5S2 Charaya, N., Pandita, D., Grewal, A. S. & Lather, V. Design, synthesis and biological evaluation of novel thiazol-2-yl benzamide derivatives as glucokinase activators. Comput. Biol. Chem. (2018) 1336
GKA54-8 GKA54-8 GKA: Systemic 2018 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 483.99 5.3 JCDM College of Pharmacy (Sirsa, INDIA) C23H18ClN3O3S2 Charaya, N., Pandita, D., Grewal, A. S. & Lather, V. Design, synthesis and biological evaluation of novel thiazol-2-yl benzamide derivatives as glucokinase activators. Comput. Biol. Chem. (2018) 1337
GKA54-9 GKA54-9 GKA: Systemic 2018 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 401.5 3.48 JCDM College of Pharmacy (Sirsa, INDIA) C19H19N3O3S2 Charaya, N., Pandita, D., Grewal, A. S. & Lather, V. Design, synthesis and biological evaluation of novel thiazol-2-yl benzamide derivatives as glucokinase activators. Comput. Biol. Chem. (2018) 78828000 1338
GKA55-16 GKA55-16 GKA: Part of a hepatoselective lead optimization effort (see reference) 2018 Thiazole/Thiadiazole,Benzamide 427.54 3.18 Sanwa Kagaku Kenkyusho Co., Ltd. (JAPAN) C21H21N3O3S2 Fujieda, H. et al. Discovery of a potent glucokinase activator with a favorable liver and pancreas distribution pattern for the treatment of type 2 diabetes mellitus. Eur. J. Med. Chem. (2018) 145987692 1346
GKA55-18 GKA55-18 GKA: Part of a hepatoselective lead optimization effort (see reference) 2018 Thiazole/Thiadiazole,Benzamide 454.61 3.9 Sanwa Kagaku Kenkyusho Co., Ltd. (JAPAN) C23H26N4O2S2 Fujieda, H. et al. Discovery of a potent glucokinase activator with a favorable liver and pancreas distribution pattern for the treatment of type 2 diabetes mellitus. Eur. J. Med. Chem. (2018) 145979079 1347
GKA55-20 GKA55-20 GKA: Part of a hepatoselective lead optimization effort (see reference) 2018 Thiazole/Thiadiazole,Benzamide 479.58 3.48 Sanwa Kagaku Kenkyusho Co., Ltd. (JAPAN) C22H21N7O2S2 Fujieda, H. et al. Discovery of a potent glucokinase activator with a favorable liver and pancreas distribution pattern for the treatment of type 2 diabetes mellitus. Eur. J. Med. Chem. (2018) 145987086 1348
GKA55-21 GKA55-21 GKA: Part of a hepatoselective lead optimization effort (see reference) 2018 Thiazole/Thiadiazole,Benzamide 454.57 2.71 Sanwa Kagaku Kenkyusho Co., Ltd. (JAPAN) C22H22N4O3S2 Fujieda, H. et al. Discovery of a potent glucokinase activator with a favorable liver and pancreas distribution pattern for the treatment of type 2 diabetes mellitus. Eur. J. Med. Chem. (2018) 145986718 1349
GKA55-26a GKA55-26a GKA: Part of a hepatoselective lead optimization effort (see reference) 2018 Thiazole/Thiadiazole 375.51 2.78 Sanwa Kagaku Kenkyusho Co., Ltd. (JAPAN) C18H21N3O2S2 Fujieda, H. et al. Discovery of a potent glucokinase activator with a favorable liver and pancreas distribution pattern for the treatment of type 2 diabetes mellitus. Eur. J. Med. Chem. (2018) 145979061 1350
GKA55-26b GKA55-26b GKA: Part of a hepatoselective lead optimization effort (see reference) 2018 Thiazole/Thiadiazole 389.53 3.14 Sanwa Kagaku Kenkyusho Co., Ltd. (JAPAN) C19H23N3O2S2 Fujieda, H. et al. Discovery of a potent glucokinase activator with a favorable liver and pancreas distribution pattern for the treatment of type 2 diabetes mellitus. Eur. J. Med. Chem. (2018) 145986562 1351
GKA55-29a GKA55-29a GKA: Part of a hepatoselective lead optimization effort (see reference) 2018 Thiazole/Thiadiazole 347.46 2.68 Sanwa Kagaku Kenkyusho Co., Ltd. (JAPAN) C16H17N3O2S2 Fujieda, H. et al. Discovery of a potent glucokinase activator with a favorable liver and pancreas distribution pattern for the treatment of type 2 diabetes mellitus. Eur. J. Med. Chem. (2018) 145979584 1352
GKA55-29b GKA55-29b GKA: Part of a hepatoselective lead optimization effort (see reference) 2018 Thiazole/Thiadiazole 361.48 3.04 Sanwa Kagaku Kenkyusho Co., Ltd. (JAPAN) C17H19N3O2S2 Fujieda, H. et al. Discovery of a potent glucokinase activator with a favorable liver and pancreas distribution pattern for the treatment of type 2 diabetes mellitus. Eur. J. Med. Chem. (2018) 145979684 1353
GKA55-33a GKA55-33a GKA: Part of a hepatoselective lead optimization effort (see reference) 2018 Thiazole/Thiadiazole 404.55 1.77 Sanwa Kagaku Kenkyusho Co., Ltd. (JAPAN) C19H24N4O2S2 Fujieda, H. et al. Discovery of a potent glucokinase activator with a favorable liver and pancreas distribution pattern for the treatment of type 2 diabetes mellitus. Eur. J. Med. Chem. (2018) 145990739 1354
GKA55-33b GKA55-33b GKA: Part of a hepatoselective lead optimization effort (see reference) 2018 Thiazole/Thiadiazole 364.49 1.05 Sanwa Kagaku Kenkyusho Co., Ltd. (JAPAN) C16H20N4O2S2 Fujieda, H. et al. Discovery of a potent glucokinase activator with a favorable liver and pancreas distribution pattern for the treatment of type 2 diabetes mellitus. Eur. J. Med. Chem. (2018) 145992519 1355
GKA55-33c GKA55-33c GKA: Part of a hepatoselective lead optimization effort (see reference) 2018 Thiazole/Thiadiazole 350.46 1.15 Sanwa Kagaku Kenkyusho Co., Ltd. (JAPAN) C15H18N4O2S2 Fujieda, H. et al. Discovery of a potent glucokinase activator with a favorable liver and pancreas distribution pattern for the treatment of type 2 diabetes mellitus. Eur. J. Med. Chem. (2018) 145981468 1356
GKA55-34d GKA55-34d GKA: Part of a hepatoselective lead optimization effort (see reference) 2018 Thiazole/Thiadiazole 378.51 2.12 Sanwa Kagaku Kenkyusho Co., Ltd. (JAPAN) C17H22N4O2S2 Fujieda, H. et al. Discovery of a potent glucokinase activator with a favorable liver and pancreas distribution pattern for the treatment of type 2 diabetes mellitus. Eur. J. Med. Chem. (2018) 145993047 1357
GKA55-34e GKA55-34e GKA: Part of a hepatoselective lead optimization effort (see reference) 2018 Thiazole/Thiadiazole 412.96 3.09 Sanwa Kagaku Kenkyusho Co., Ltd. (JAPAN) C17H21ClN4O2S2 Fujieda, H. et al. Discovery of a potent glucokinase activator with a favorable liver and pancreas distribution pattern for the treatment of type 2 diabetes mellitus. Eur. J. Med. Chem. (2018) 145946610 1358
GKA55-38 GKA55-38 GKA: Part of a hepatoselective lead optimization effort (see reference) 2018 Thiazole/Thiadiazole 412.96 3.09 Sanwa Kagaku Kenkyusho Co., Ltd. (JAPAN) C17H21ClN4O2S2 Fujieda, H. et al. Discovery of a potent glucokinase activator with a favorable liver and pancreas distribution pattern for the treatment of type 2 diabetes mellitus. Eur. J. Med. Chem. (2018) 145946610 1359
GKA55-42 GKA55-42 GKA: Part of a hepatoselective lead optimization effort (see reference) 2018 Thiazole/Thiadiazole 412.96 3.09 Sanwa Kagaku Kenkyusho Co., Ltd. (JAPAN) C17H21ClN4O2S2 Fujieda, H. et al. Discovery of a potent glucokinase activator with a favorable liver and pancreas distribution pattern for the treatment of type 2 diabetes mellitus. Eur. J. Med. Chem. (2018) 145946610 1360
GKA55-47a GKA55-47a GKA: Part of a hepatoselective lead optimization effort (see reference) 2018 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 462.99 2.15 Sanwa Kagaku Kenkyusho Co., Ltd. (JAPAN) C16H19ClN4O4S3 Fujieda, H. et al. Discovery of a potent glucokinase activator with a favorable liver and pancreas distribution pattern for the treatment of type 2 diabetes mellitus. Eur. J. Med. Chem. (2018) 145981137 1361
GKA55-47b GKA55-47b GKA: Part of a hepatoselective lead optimization effort (see reference) 2018 Thiazole/Thiadiazole 477.02 2.34 Sanwa Kagaku Kenkyusho Co., Ltd. (JAPAN) C17H21ClN4O4S3 Fujieda, H. et al. Discovery of a potent glucokinase activator with a favorable liver and pancreas distribution pattern for the treatment of type 2 diabetes mellitus. Eur. J. Med. Chem. (2018) 145990742 1362
GKA55-48a GKA55-48a GKA: Part of a hepatoselective lead optimization effort (see reference) 2018 Thiazole/Thiadiazole 426.94 2.36 Sanwa Kagaku Kenkyusho Co., Ltd. (JAPAN) C17H19ClN4O3S2 Fujieda, H. et al. Discovery of a potent glucokinase activator with a favorable liver and pancreas distribution pattern for the treatment of type 2 diabetes mellitus. Eur. J. Med. Chem. (2018) 145990121 1363
GKA55-48b GKA55-48b GKA: Part of a hepatoselective lead optimization effort (see reference) 2018 Thiazole/Thiadiazole 440.97 2.55 Sanwa Kagaku Kenkyusho Co., Ltd. (JAPAN) C18H21ClN4O3S2 Fujieda, H. et al. Discovery of a potent glucokinase activator with a favorable liver and pancreas distribution pattern for the treatment of type 2 diabetes mellitus. Eur. J. Med. Chem. (2018) 145993802 1364
GKA55-51 GKA55-51 GKA: Part of a hepatoselective lead optimization effort (see reference) 2018 Thiazole/Thiadiazole 442.94 -0.07 Sanwa Kagaku Kenkyusho Co., Ltd. (JAPAN) C17H19ClN4O4S2 Fujieda, H. et al. Discovery of a potent glucokinase activator with a favorable liver and pancreas distribution pattern for the treatment of type 2 diabetes mellitus. Eur. J. Med. Chem. (2018) 140187047 1365
GKA55-53a GKA55-53a GKA: Part of a hepatoselective lead optimization effort (see reference) 2018 Thiazole/Thiadiazole 456.97 0.4 Sanwa Kagaku Kenkyusho Co., Ltd. (JAPAN) C18H21ClN4O4S2 Fujieda, H. et al. Discovery of a potent glucokinase activator with a favorable liver and pancreas distribution pattern for the treatment of type 2 diabetes mellitus. Eur. J. Med. Chem. (2018) 145947854 1366
GKA55-53b GKA55-53b GKA: Part of a hepatoselective lead optimization effort (see reference) 2018 Thiazole/Thiadiazole 440.51 -0.13 Sanwa Kagaku Kenkyusho Co., Ltd. (JAPAN) C18H21FN4O4S2 Fujieda, H. et al. Discovery of a potent glucokinase activator with a favorable liver and pancreas distribution pattern for the treatment of type 2 diabetes mellitus. Eur. J. Med. Chem. (2018) 145947763 1367
GKA55-53c GKA55-53c GKA: Part of a hepatoselective lead optimization effort (see reference) 2018 Thiazole/Thiadiazole 454.54 -0.22 Sanwa Kagaku Kenkyusho Co., Ltd. (JAPAN) C19H23FN4O4S2 Fujieda, H. et al. Discovery of a potent glucokinase activator with a favorable liver and pancreas distribution pattern for the treatment of type 2 diabetes mellitus. Eur. J. Med. Chem. (2018) 145946414 1368
GKA55-53d GKA55-53d GKA: Part of a hepatoselective lead optimization effort (see reference) 2018 Thiazole/Thiadiazole 468.57 0.13 Sanwa Kagaku Kenkyusho Co., Ltd. (JAPAN) C20H25FN4O4S2 Fujieda, H. et al. Discovery of a potent glucokinase activator with a favorable liver and pancreas distribution pattern for the treatment of type 2 diabetes mellitus. Eur. J. Med. Chem. (2018) 145947614 1369
GKA55-53e GKA55-53e GKA: Part of a hepatoselective lead optimization effort (see reference) 2018 Thiazole/Thiadiazole 482.59 0.49 Sanwa Kagaku Kenkyusho Co., Ltd. (JAPAN) C21H27FN4O4S2 Fujieda, H. et al. Discovery of a potent glucokinase activator with a favorable liver and pancreas distribution pattern for the treatment of type 2 diabetes mellitus. Eur. J. Med. Chem. (2018) 86664459 1370
GKA55-58a GKA55-58a GKA: Part of a hepatoselective lead optimization effort (see reference) 2018 Thiazole/Thiadiazole 454.54 -0.22 Sanwa Kagaku Kenkyusho Co., Ltd. (JAPAN) C19H23FN4O4S2 Fujieda, H. et al. Discovery of a potent glucokinase activator with a favorable liver and pancreas distribution pattern for the treatment of type 2 diabetes mellitus. Eur. J. Med. Chem. (2018) 145946414 1371
GKA55-58b GKA55-58b GKA: Part of a hepatoselective lead optimization effort (see reference) 2018 Thiazole/Thiadiazole 454.54 0.27 Sanwa Kagaku Kenkyusho Co., Ltd. (JAPAN) C19H23FN4O4S2 Fujieda, H. et al. Discovery of a potent glucokinase activator with a favorable liver and pancreas distribution pattern for the treatment of type 2 diabetes mellitus. Eur. J. Med. Chem. (2018) 145947796 1372
GKA55-59 GKA55-59 GKA: Hepatoselective 2018 Thiazole/Thiadiazole 454.54 0.24 Sanwa Kagaku Kenkyusho Co., Ltd. (JAPAN) C19H23FN4O4S2 Fujieda, H. et al. Discovery of a potent glucokinase activator with a favorable liver and pancreas distribution pattern for the treatment of type 2 diabetes mellitus. Eur. J. Med. Chem. (2018) 138964067 1373
GKA56-Ia GKA56-Ia GKA: Systemic 2018 Urea,Pyridine 213.24 2 Ogarev Mordovia State University (Saransk, RUSSIA) C12H11N3O Semenov, A. V. et al. Glucokinase Activators Based on N-Aryl-N′-Pyridin-2-Ylurea Derivatives. Pharm. Chem. J. (2018) 221427 1374
GKA56-Ib GKA56-Ib GKA: Systemic 2018 Urea,Pyridine 258.23 1.58 Ogarev Mordovia State University (Saransk, RUSSIA) C12H10N4O3 Semenov, A. V. et al. Glucokinase Activators Based on N-Aryl-N′-Pyridin-2-Ylurea Derivatives. Pharm. Chem. J. (2018) 23804732 1375
GKA56-Ic GKA56-Ic GKA: Systemic 2018 Urea,Pyridine 258.23 1.83 Ogarev Mordovia State University (Saransk, RUSSIA) C12H10N4O3 Semenov, A. V. et al. Glucokinase Activators Based on N-Aryl-N′-Pyridin-2-Ylurea Derivatives. Pharm. Chem. J. (2018) 12099952 1376
GKA56-Ih GKA56-Ih GKA: Systemic 2018 Urea,Pyridine 243.26 1.72 Ogarev Mordovia State University (Saransk, RUSSIA) C13H13N3O2 Semenov, A. V. et al. Glucokinase Activators Based on N-Aryl-N′-Pyridin-2-Ylurea Derivatives. Pharm. Chem. J. (2018) 1377
GKA56-Ii GKA56-Ii GKA: Systemic 2018 Urea,Pyridine 288.26 1.55 Ogarev Mordovia State University (Saransk, RUSSIA) C13H12N4O4 Semenov, A. V. et al. Glucokinase Activators Based on N-Aryl-N′-Pyridin-2-Ylurea Derivatives. Pharm. Chem. J. (2018) 1378
GKA56-Ij GKA56-Ij GKA: Systemic 2018 Urea,Pyridine 288.26 1.55 Ogarev Mordovia State University (Saransk, RUSSIA) C13H12N4O4 Semenov, A. V. et al. Glucokinase Activators Based on N-Aryl-N′-Pyridin-2-Ylurea Derivatives. Pharm. Chem. J. (2018) 1379
GKA56-Ik GKA56-Ik GKA: Systemic 2018 Urea,Pyridine 257.29 2.09 Ogarev Mordovia State University (Saransk, RUSSIA) C14H15N3O2 Semenov, A. V. et al. Glucokinase Activators Based on N-Aryl-N′-Pyridin-2-Ylurea Derivatives. Pharm. Chem. J. (2018) 1380
GKA57-5a GKA57-5a GKA: Systemic 2019 Benzamide,Pyridine,Sulfoxide/Sulfone derivatives 398.39 2.04 Chitkara University & Amity Institute of Pharmacy (INDIA) C18H14N4O5S Grewal, A. S., Kharb, R., Prasad, D. N., Dua, J. S. & Lather, V. N-pyridin-2-yl benzamide analogues as allosteric activators of glucokinase: Design, synthesis, in vitro, in silico and in vivo evaluation. Chem. Biol. Drug Des. (2019) 1381
GKA57-5b GKA57-5b GKA: Systemic 2019 Benzamide,Pyridine,Sulfoxide/Sulfone derivatives 432.84 2.67 Chitkara University & Amity Institute of Pharmacy (INDIA) C18H13ClN4O5S Grewal, A. S., Kharb, R., Prasad, D. N., Dua, J. S. & Lather, V. N-pyridin-2-yl benzamide analogues as allosteric activators of glucokinase: Design, synthesis, in vitro, in silico and in vivo evaluation. Chem. Biol. Drug Des. (2019) 1382
GKA57-5c GKA57-5c GKA: Systemic 2019 Benzamide,Pyridine,Sulfoxide/Sulfone derivatives 432.84 2.67 Chitkara University & Amity Institute of Pharmacy (INDIA) C18H13ClN4O5S Grewal, A. S., Kharb, R., Prasad, D. N., Dua, J. S. & Lather, V. N-pyridin-2-yl benzamide analogues as allosteric activators of glucokinase: Design, synthesis, in vitro, in silico and in vivo evaluation. Chem. Biol. Drug Des. (2019) 1383
GKA57-5d GKA57-5d GKA: Systemic 2019 Benzamide,Pyridine,Sulfoxide/Sulfone derivatives 432.84 2.67 Chitkara University & Amity Institute of Pharmacy (INDIA) C18H13ClN4O5S Grewal, A. S., Kharb, R., Prasad, D. N., Dua, J. S. & Lather, V. N-pyridin-2-yl benzamide analogues as allosteric activators of glucokinase: Design, synthesis, in vitro, in silico and in vivo evaluation. Chem. Biol. Drug Des. (2019) 1384
GKA57-5e GKA57-5e GKA: Systemic 2019 Benzamide,Pyridine,Sulfoxide/Sulfone derivatives 443.39 1.87 Chitkara University & Amity Institute of Pharmacy (INDIA) C18H13N5O7S Grewal, A. S., Kharb, R., Prasad, D. N., Dua, J. S. & Lather, V. N-pyridin-2-yl benzamide analogues as allosteric activators of glucokinase: Design, synthesis, in vitro, in silico and in vivo evaluation. Chem. Biol. Drug Des. (2019) 1385
GKA57-5f GKA57-5f GKA: Systemic 2019 Benzamide,Pyridine,Sulfoxide/Sulfone derivatives 443.39 1.87 Chitkara University & Amity Institute of Pharmacy (INDIA) C18H13N5O7S Grewal, A. S., Kharb, R., Prasad, D. N., Dua, J. S. & Lather, V. N-pyridin-2-yl benzamide analogues as allosteric activators of glucokinase: Design, synthesis, in vitro, in silico and in vivo evaluation. Chem. Biol. Drug Des. (2019) 1386
GKA57-5g GKA57-5g GKA: Systemic 2019 Benzamide,Pyridine,Sulfoxide/Sulfone derivatives 443.39 1.87 Chitkara University & Amity Institute of Pharmacy (INDIA) C18H13N5O7S Grewal, A. S., Kharb, R., Prasad, D. N., Dua, J. S. & Lather, V. N-pyridin-2-yl benzamide analogues as allosteric activators of glucokinase: Design, synthesis, in vitro, in silico and in vivo evaluation. Chem. Biol. Drug Des. (2019) 1387
GKA57-5h GKA57-5h GKA: Systemic 2019 Benzamide,Pyridine,Sulfoxide/Sulfone derivatives 412.42 2.34 Chitkara University & Amity Institute of Pharmacy (INDIA) C19H16N4O5S Grewal, A. S., Kharb, R., Prasad, D. N., Dua, J. S. & Lather, V. N-pyridin-2-yl benzamide analogues as allosteric activators of glucokinase: Design, synthesis, in vitro, in silico and in vivo evaluation. Chem. Biol. Drug Des. (2019) 1388
GKA57-5i GKA57-5i GKA: Systemic 2019 Benzamide,Pyridine,Sulfoxide/Sulfone derivatives 350.35 1.21 Chitkara University & Amity Institute of Pharmacy (INDIA) C14H14N4O5S Grewal, A. S., Kharb, R., Prasad, D. N., Dua, J. S. & Lather, V. N-pyridin-2-yl benzamide analogues as allosteric activators of glucokinase: Design, synthesis, in vitro, in silico and in vivo evaluation. Chem. Biol. Drug Des. (2019) 1389
GKA57-6a GKA57-6a GKA: Systemic 2019 Benzamide,Pyridine,Sulfoxide/Sulfone derivatives 412.42 2.44 Chitkara University & Amity Institute of Pharmacy (INDIA) C19H16N4O5S Grewal, A. S., Kharb, R., Prasad, D. N., Dua, J. S. & Lather, V. N-pyridin-2-yl benzamide analogues as allosteric activators of glucokinase: Design, synthesis, in vitro, in silico and in vivo evaluation. Chem. Biol. Drug Des. (2019) 1390
GKA57-6b GKA57-6b GKA: Systemic 2019 Benzamide,Pyridine,Sulfoxide/Sulfone derivatives 446.86 3.07 Chitkara University & Amity Institute of Pharmacy (INDIA) C19H15ClN4O5S Grewal, A. S., Kharb, R., Prasad, D. N., Dua, J. S. & Lather, V. N-pyridin-2-yl benzamide analogues as allosteric activators of glucokinase: Design, synthesis, in vitro, in silico and in vivo evaluation. Chem. Biol. Drug Des. (2019) 1391
GKA57-6c GKA57-6c GKA: Systemic 2019 Benzamide,Pyridine,Sulfoxide/Sulfone derivatives 446.86 3.07 Chitkara University & Amity Institute of Pharmacy (INDIA) C19H15ClN4O5S Grewal, A. S., Kharb, R., Prasad, D. N., Dua, J. S. & Lather, V. N-pyridin-2-yl benzamide analogues as allosteric activators of glucokinase: Design, synthesis, in vitro, in silico and in vivo evaluation. Chem. Biol. Drug Des. (2019) 1392
GKA57-6d GKA57-6d GKA: Systemic 2019 Benzamide,Pyridine,Sulfoxide/Sulfone derivatives 446.86 3.07 Chitkara University & Amity Institute of Pharmacy (INDIA) C19H15ClN4O5S Grewal, A. S., Kharb, R., Prasad, D. N., Dua, J. S. & Lather, V. N-pyridin-2-yl benzamide analogues as allosteric activators of glucokinase: Design, synthesis, in vitro, in silico and in vivo evaluation. Chem. Biol. Drug Des. (2019) 1393
GKA57-6e GKA57-6e GKA: Systemic 2019 Benzamide,Pyridine,Sulfoxide/Sulfone derivatives 457.42 2.27 Chitkara University & Amity Institute of Pharmacy (INDIA) C19H15N5O7S Grewal, A. S., Kharb, R., Prasad, D. N., Dua, J. S. & Lather, V. N-pyridin-2-yl benzamide analogues as allosteric activators of glucokinase: Design, synthesis, in vitro, in silico and in vivo evaluation. Chem. Biol. Drug Des. (2019) 1394
GKA57-6f GKA57-6f GKA: Systemic 2019 Benzamide,Pyridine,Sulfoxide/Sulfone derivatives 457.42 2.27 Chitkara University & Amity Institute of Pharmacy (INDIA) C19H15N5O7S Grewal, A. S., Kharb, R., Prasad, D. N., Dua, J. S. & Lather, V. N-pyridin-2-yl benzamide analogues as allosteric activators of glucokinase: Design, synthesis, in vitro, in silico and in vivo evaluation. Chem. Biol. Drug Des. (2019) 1395
GKA57-6g GKA57-6g GKA: Systemic 2019 Benzamide,Pyridine,Sulfoxide/Sulfone derivatives 457.42 2.27 Chitkara University & Amity Institute of Pharmacy (INDIA) C19H15N5O7S Grewal, A. S., Kharb, R., Prasad, D. N., Dua, J. S. & Lather, V. N-pyridin-2-yl benzamide analogues as allosteric activators of glucokinase: Design, synthesis, in vitro, in silico and in vivo evaluation. Chem. Biol. Drug Des. (2019) 1396
GKA57-6h GKA57-6h GKA: Systemic 2019 Benzamide,Pyridine,Sulfoxide/Sulfone derivatives 426.45 2.74 Chitkara University & Amity Institute of Pharmacy (INDIA) C20H18N4O5S Grewal, A. S., Kharb, R., Prasad, D. N., Dua, J. S. & Lather, V. N-pyridin-2-yl benzamide analogues as allosteric activators of glucokinase: Design, synthesis, in vitro, in silico and in vivo evaluation. Chem. Biol. Drug Des. (2019) 1397
GKA57-6i GKA57-6i GKA: Systemic 2019 Benzamide,Pyridine,Sulfoxide/Sulfone derivatives 364.38 1.61 Chitkara University & Amity Institute of Pharmacy (INDIA) C15H16N4O5S Grewal, A. S., Kharb, R., Prasad, D. N., Dua, J. S. & Lather, V. N-pyridin-2-yl benzamide analogues as allosteric activators of glucokinase: Design, synthesis, in vitro, in silico and in vivo evaluation. Chem. Biol. Drug Des. (2019) 1398
GKA58-5a GKA58-5a GKA: Systemic 2019 Benzamide,Pyrimidine,Sulfoxide/Sulfone derivatives 399.38 1.72 Chitkara University & Amity Institute of Pharmacy (INDIA) C17H13N5O5S Grewal, A. S., Kharb, R., Prasad, D. N., Dua, J. S. & Lather, V. Design, synthesis and evaluation of novel 3,5-disubstituted benzamide derivatives as allosteric glucokinase activators. BMC Chem. (2019) 137321383 1399
GKA58-5b GKA58-5b GKA: Systemic 2019 Benzamide,Pyrimidine,Sulfoxide/Sulfone derivatives 433.83 2.35 Chitkara University & Amity Institute of Pharmacy (INDIA) C17H12ClN5O5S Grewal, A. S., Kharb, R., Prasad, D. N., Dua, J. S. & Lather, V. Design, synthesis and evaluation of novel 3,5-disubstituted benzamide derivatives as allosteric glucokinase activators. BMC Chem. (2019) 137321397 1400
GKA58-5c GKA58-5c GKA: Systemic 2019 Benzamide,Pyrimidine,Sulfoxide/Sulfone derivatives 433.83 2.35 Chitkara University & Amity Institute of Pharmacy (INDIA) C17H12ClN5O5S Grewal, A. S., Kharb, R., Prasad, D. N., Dua, J. S. & Lather, V. Design, synthesis and evaluation of novel 3,5-disubstituted benzamide derivatives as allosteric glucokinase activators. BMC Chem. (2019) 137321394 1401
GKA58-5d GKA58-5d GKA: Systemic 2019 Benzamide,Pyrimidine,Sulfoxide/Sulfone derivatives 433.83 2.35 Chitkara University & Amity Institute of Pharmacy (INDIA) C17H12ClN5O5S Grewal, A. S., Kharb, R., Prasad, D. N., Dua, J. S. & Lather, V. Design, synthesis and evaluation of novel 3,5-disubstituted benzamide derivatives as allosteric glucokinase activators. BMC Chem. (2019) 137321392 1402
GKA58-5e GKA58-5e GKA: Systemic 2019 Benzamide,Pyrimidine,Sulfoxide/Sulfone derivatives 444.38 2.1 Chitkara University & Amity Institute of Pharmacy (INDIA) C17H12N6O7S Grewal, A. S., Kharb, R., Prasad, D. N., Dua, J. S. & Lather, V. Design, synthesis and evaluation of novel 3,5-disubstituted benzamide derivatives as allosteric glucokinase activators. BMC Chem. (2019) 137321406 1403
GKA58-5f GKA58-5f GKA: Systemic 2019 Benzamide,Pyrimidine,Sulfoxide/Sulfone derivatives 444.38 1.55 Chitkara University & Amity Institute of Pharmacy (INDIA) C17H12N6O7S Grewal, A. S., Kharb, R., Prasad, D. N., Dua, J. S. & Lather, V. Design, synthesis and evaluation of novel 3,5-disubstituted benzamide derivatives as allosteric glucokinase activators. BMC Chem. (2019) 137321409 1404
GKA58-5g GKA58-5g GKA: Systemic 2019 Benzamide,Pyrimidine,Sulfoxide/Sulfone derivatives 444.38 1.55 Chitkara University & Amity Institute of Pharmacy (INDIA) C17H12N6O7S Grewal, A. S., Kharb, R., Prasad, D. N., Dua, J. S. & Lather, V. Design, synthesis and evaluation of novel 3,5-disubstituted benzamide derivatives as allosteric glucokinase activators. BMC Chem. (2019) 137321408 1405
GKA58-5h GKA58-5h GKA: Systemic 2019 Benzamide,Pyrimidine,Sulfoxide/Sulfone derivatives 413.41 1.66 Chitkara University & Amity Institute of Pharmacy (INDIA) C18H15N5O5S Grewal, A. S., Kharb, R., Prasad, D. N., Dua, J. S. & Lather, V. Design, synthesis and evaluation of novel 3,5-disubstituted benzamide derivatives as allosteric glucokinase activators. BMC Chem. (2019) 137321391 1406
GKA58-5i GKA58-5i GKA: Systemic 2019 Benzamide,Pyrimidine,Sulfoxide/Sulfone derivatives 351.34 0.53 Chitkara University & Amity Institute of Pharmacy (INDIA) C13H13N5O5S Grewal, A. S., Kharb, R., Prasad, D. N., Dua, J. S. & Lather, V. Design, synthesis and evaluation of novel 3,5-disubstituted benzamide derivatives as allosteric glucokinase activators. BMC Chem. (2019) 137321356 1407
GKA58-6a GKA58-6a GKA: Systemic 2019 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 404.42 2.47 Chitkara University & Amity Institute of Pharmacy (INDIA) C16H12N4O5S2 Grewal, A. S., Kharb, R., Prasad, D. N., Dua, J. S. & Lather, V. Design, synthesis and evaluation of novel 3,5-disubstituted benzamide derivatives as allosteric glucokinase activators. BMC Chem. (2019) 137321378 1408
GKA58-6b GKA58-6b GKA: Systemic 2019 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 438.87 3.1 Chitkara University & Amity Institute of Pharmacy (INDIA) C16H11ClN4O5S2 Grewal, A. S., Kharb, R., Prasad, D. N., Dua, J. S. & Lather, V. Design, synthesis and evaluation of novel 3,5-disubstituted benzamide derivatives as allosteric glucokinase activators. BMC Chem. (2019) 137321388 1409
GKA58-6c GKA58-6c GKA: Systemic 2019 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 438.87 3.1 Chitkara University & Amity Institute of Pharmacy (INDIA) C16H11ClN4O5S2 Grewal, A. S., Kharb, R., Prasad, D. N., Dua, J. S. & Lather, V. Design, synthesis and evaluation of novel 3,5-disubstituted benzamide derivatives as allosteric glucokinase activators. BMC Chem. (2019) 137321386 1410
GKA58-6d GKA58-6d GKA: Systemic 2019 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 438.87 3.1 Chitkara University & Amity Institute of Pharmacy (INDIA) C16H11ClN4O5S2 Grewal, A. S., Kharb, R., Prasad, D. N., Dua, J. S. & Lather, V. Design, synthesis and evaluation of novel 3,5-disubstituted benzamide derivatives as allosteric glucokinase activators. BMC Chem. (2019) 137321385 1411
GKA58-6e GKA58-6e GKA: Systemic 2019 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 449.42 2.85 Chitkara University & Amity Institute of Pharmacy (INDIA) C16H11N5O7S2 Grewal, A. S., Kharb, R., Prasad, D. N., Dua, J. S. & Lather, V. Design, synthesis and evaluation of novel 3,5-disubstituted benzamide derivatives as allosteric glucokinase activators. BMC Chem. (2019) 137321400 1412
GKA58-6f GKA58-6f GKA: Systemic 2019 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 449.42 2.3 Chitkara University & Amity Institute of Pharmacy (INDIA) C16H11N5O7S2 Grewal, A. S., Kharb, R., Prasad, D. N., Dua, J. S. & Lather, V. Design, synthesis and evaluation of novel 3,5-disubstituted benzamide derivatives as allosteric glucokinase activators. BMC Chem. (2019) 137321402 1413
GKA58-6g GKA58-6g GKA: Systemic 2019 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 449.42 2.3 Chitkara University & Amity Institute of Pharmacy (INDIA) C16H11N5O7S2 Grewal, A. S., Kharb, R., Prasad, D. N., Dua, J. S. & Lather, V. Design, synthesis and evaluation of novel 3,5-disubstituted benzamide derivatives as allosteric glucokinase activators. BMC Chem. (2019) 137321401 1414
GKA58-6h GKA58-6h GKA: Systemic 2019 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 418.45 2.41 Chitkara University & Amity Institute of Pharmacy (INDIA) C17H14N4O5S2 Grewal, A. S., Kharb, R., Prasad, D. N., Dua, J. S. & Lather, V. Design, synthesis and evaluation of novel 3,5-disubstituted benzamide derivatives as allosteric glucokinase activators. BMC Chem. (2019) 137321384 1415
GKA58-6i GKA58-6i GKA: Systemic 2019 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 356.38 1.28 Chitkara University & Amity Institute of Pharmacy (INDIA) C12H12N4O5S2 Grewal, A. S., Kharb, R., Prasad, D. N., Dua, J. S. & Lather, V. Design, synthesis and evaluation of novel 3,5-disubstituted benzamide derivatives as allosteric glucokinase activators. BMC Chem. (2019) 137321350 1416
GKA59-14 GKA59-14 GKA: Systemic 2020 Thiazole/Thiadiazole,Pyridine 362.24 4.71 Array BioPharma (USA) C15H12BrN3OS Hinklin, R. J. et al. Discovery and preclinical development of AR453588 as an anti-diabetic glucokinase activator. Bioorganic Med. Chem. (2020) 24765543 1419
GKA59-15 GKA59-15 GKA: Systemic 2020 Thiazole/Thiadiazole,Pyridine 283.35 4.02 Array BioPharma (USA) C15H13N3OS Hinklin, R. J. et al. Discovery and preclinical development of AR453588 as an anti-diabetic glucokinase activator. Bioorganic Med. Chem. (2020) 24765842 1420
GKA59-16 GKA59-16 GKA: Systemic 2020 Thiazole/Thiadiazole,Pyridine 405.54 6.03 Array BioPharma (USA) C22H19N3OS2 Hinklin, R. J. et al. Discovery and preclinical development of AR453588 as an anti-diabetic glucokinase activator. Bioorganic Med. Chem. (2020) 24765640 1421
GKA59-17 GKA59-17 GKA: Systemic 2020 Thiazole/Thiadiazole,Pyridine 391.51 6.09 Array BioPharma (USA) C21H17N3OS2 Hinklin, R. J. et al. Discovery and preclinical development of AR453588 as an anti-diabetic glucokinase activator. Bioorganic Med. Chem. (2020) 24765540 1422
GKA59-18 GKA59-18 GKA: Systemic 2020 Thiazole/Thiadiazole,Pyridine 392.5 5.35 Array BioPharma (USA) C20H16N4OS2 Hinklin, R. J. et al. Discovery and preclinical development of AR453588 as an anti-diabetic glucokinase activator. Bioorganic Med. Chem. (2020) 57742772 1423
GKA59-19 GKA59-19 GKA: Systemic 2020 Thiazole/Thiadiazole,Pyridine 392.5 5.02 Array BioPharma (USA) C20H16N4OS2 Hinklin, R. J. et al. Discovery and preclinical development of AR453588 as an anti-diabetic glucokinase activator. Bioorganic Med. Chem. (2020) 24765183 1424
GKA59-23 GKA59-23 GKA: Systemic 2020 Thiazole/Thiadiazole,Pyridine 406.52 5.45 Array BioPharma (USA) C21H18N4OS2 Hinklin, R. J. et al. Discovery and preclinical development of AR453588 as an anti-diabetic glucokinase activator. Bioorganic Med. Chem. (2020) 57742610 1425
GKA59-24 GKA59-24 GKA: Systemic 2020 Thiazole/Thiadiazole,Pyridine 446.47 5.54 Array BioPharma (USA) C20H13F3N4OS2 Hinklin, R. J. et al. Discovery and preclinical development of AR453588 as an anti-diabetic glucokinase activator. Bioorganic Med. Chem. (2020) 57742946 1426
GKA59-25 GKA59-25 GKA: Systemic 2020 Thiazole/Thiadiazole,Pyridine 418.53 5.2 Array BioPharma (USA) C22H18N4OS2 Hinklin, R. J. et al. Discovery and preclinical development of AR453588 as an anti-diabetic glucokinase activator. Bioorganic Med. Chem. (2020) 57742580 1427
GKA59-26 GKA59-26 GKA: Systemic 2020 Thiazole/Thiadiazole,Pyridine 420.55 5.78 Array BioPharma (USA) C22H20N4OS2 Hinklin, R. J. et al. Discovery and preclinical development of AR453588 as an anti-diabetic glucokinase activator. Bioorganic Med. Chem. (2020) 57742807 1428
GKA59-27 GKA59-27 GKA: Systemic 2020 Thiazole/Thiadiazole,Pyridine 434.58 6.25 Array BioPharma (USA) C23H22N4OS2 Hinklin, R. J. et al. Discovery and preclinical development of AR453588 as an anti-diabetic glucokinase activator. Bioorganic Med. Chem. (2020) 57742835 1429
GKA59-28 GKA59-28 GKA: Systemic 2020 Thiazole/Thiadiazole,Pyridine 460.61 6.82 Array BioPharma (USA) C25H24N4OS2 Hinklin, R. J. et al. Discovery and preclinical development of AR453588 as an anti-diabetic glucokinase activator. Bioorganic Med. Chem. (2020) 57742658 1430
GKA59-29 GKA59-29 GKA: Systemic 2020 Thiazole/Thiadiazole,Pyridine 482.62 6.87 Array BioPharma (USA) C27H22N4OS2 Hinklin, R. J. et al. Discovery and preclinical development of AR453588 as an anti-diabetic glucokinase activator. Bioorganic Med. Chem. (2020) 57742806 1431
GKA59-31 GKA59-31 GKA: Systemic 2020 Thiazole/Thiadiazole,Pyridine 450.53 4.41 Array BioPharma (USA) C22H18N4O3S2 Hinklin, R. J. et al. Discovery and preclinical development of AR453588 as an anti-diabetic glucokinase activator. Bioorganic Med. Chem. (2020) 57742686 1432
GKA59-37 GKA59-37 GKA: Systemic 2020 Thiazole/Thiadiazole,Pyridine 393.49 5.16 Array BioPharma (USA) C19H15N5OS2 Hinklin, R. J. et al. Discovery and preclinical development of AR453588 as an anti-diabetic glucokinase activator. Bioorganic Med. Chem. (2020) 24765289 1433
GKA59-38 GKA59-38 GKA: Systemic 2020 Thiazole/Thiadiazole,Pyridine 449.55 4.83 Array BioPharma (USA) C22H19N5O2S2 Hinklin, R. J. et al. Discovery and preclinical development of AR453588 as an anti-diabetic glucokinase activator. Bioorganic Med. Chem. (2020) 156020099 1434
GKA59-39 GKA59-39 GKA: Systemic 2020 Thiazole/Thiadiazole,Pyridine 449.55 4.96 Array BioPharma (USA) C22H19N5O2S2 Hinklin, R. J. et al. Discovery and preclinical development of AR453588 as an anti-diabetic glucokinase activator. Bioorganic Med. Chem. (2020) 66995270 1435
GKA59-42 GKA59-42 GKA: Systemic 2020 Thiazole/Thiadiazole,Pyridine 504.63 4.83 Array BioPharma (USA) C25H24N6O2S2 Hinklin, R. J. et al. Discovery and preclinical development of AR453588 as an anti-diabetic glucokinase activator. Bioorganic Med. Chem. (2020) 57742634 1436
GKA59-43 GKA59-43 GKA: Systemic 2020 Thiazole/Thiadiazole,Pyridine,Sulfoxide/Sulfone derivatives 540.68 4.62 Array BioPharma (USA) C24H24N6O3S3 Hinklin, R. J. et al. Discovery and preclinical development of AR453588 as an anti-diabetic glucokinase activator. Bioorganic Med. Chem. (2020) 66995165 1437
GKA59-44 GKA59-44 GKA: Systemic 2020 Thiazole/Thiadiazole,Urea,Pyridine 533.67 4.84 Array BioPharma (USA) C26H27N7O2S2 Hinklin, R. J. et al. Discovery and preclinical development of AR453588 as an anti-diabetic glucokinase activator. Bioorganic Med. Chem. (2020) 66994821 1438
GKA59-45 GKA59-45 GKA: Systemic 2020 Thiazole/Thiadiazole,Pyridine 532.68 5.87 Array BioPharma (USA) C27H28N6O2S2 Hinklin, R. J. et al. Discovery and preclinical development of AR453588 as an anti-diabetic glucokinase activator. Bioorganic Med. Chem. (2020) 66994526 1439
GKA59-46 GKA59-46 GKA: Systemic 2020 Thiazole/Thiadiazole,Pyridine 520.63 4.18 Array BioPharma (USA) C25H24N6O3S2 Hinklin, R. J. et al. Discovery and preclinical development of AR453588 as an anti-diabetic glucokinase activator. Bioorganic Med. Chem. (2020) 57742590 1440
GKA59-47 GKA59-47 GKA: Systemic 2020 Thiazole/Thiadiazole,Pyridine 547.69 4.9 Array BioPharma (USA) C27H29N7O2S2 Hinklin, R. J. et al. Discovery and preclinical development of AR453588 as an anti-diabetic glucokinase activator. Bioorganic Med. Chem. (2020) 66994540 1441
GKA59-48 GKA59-48 GKA: Systemic 2020 Thiazole/Thiadiazole,Pyridine 534.65 4.58 Array BioPharma (USA) C26H26N6O3S2 Hinklin, R. J. et al. Discovery and preclinical development of AR453588 as an anti-diabetic glucokinase activator. Bioorganic Med. Chem. (2020) 59291620 1442
GKA59-49 GKA59-49 GKA: Systemic 2020 Thiazole/Thiadiazole,Pyridine 534.65 4.58 Array BioPharma (USA) C26H26N6O3S2 Hinklin, R. J. et al. Discovery and preclinical development of AR453588 as an anti-diabetic glucokinase activator. Bioorganic Med. Chem. (2020) 25099728 1443
GKA59-6 GKA59-6 GKA: Systemic 2020 Thiazole/Thiadiazole,Pyridine 308.36 3.74 Array BioPharma (USA) C16H12N4OS Hinklin, R. J. et al. Discovery and preclinical development of AR453588 as an anti-diabetic glucokinase activator. Bioorganic Med. Chem. (2020) 16752714 1417
GKA59-7 GKA59-7 GKA: Systemic 2020 Thiazole/Thiadiazole,Pyridine 308.36 3.74 Array BioPharma (USA) C16H12N4OS Hinklin, R. J. et al. Discovery and preclinical development of AR453588 as an anti-diabetic glucokinase activator. Bioorganic Med. Chem. (2020) 24765455 1418
GKA59-71 GKA59-71 GKA: Systemic 2020 Thiazole/Thiadiazole,Pyridine 505.62 3.76 Array BioPharma (USA) C24H23N7O2S2 Hinklin, R. J. et al. Discovery and preclinical development of AR453588 as an anti-diabetic glucokinase activator. Bioorganic Med. Chem. (2020) 59291600 1444
GKA59-72 GKA59-72 GKA: Systemic 2020 Thiazole/Thiadiazole,Pyridine 519.64 4.16 Array BioPharma (USA) C25H25N7O2S2 Hinklin, R. J. et al. Discovery and preclinical development of AR453588 as an anti-diabetic glucokinase activator. Bioorganic Med. Chem. (2020) 59291641 1445
GKA59-73 GKA59-73 GKA: Systemic 2020 Thiazole/Thiadiazole,Pyridine,Sulfoxide/Sulfone derivatives 555.7 3.95 Array BioPharma (USA) C24H25N7O3S3 Hinklin, R. J. et al. Discovery and preclinical development of AR453588 as an anti-diabetic glucokinase activator. Bioorganic Med. Chem. (2020) 59291609 1446
GKA59-74 GKA59-74 GKA: Systemic 2020 Thiazole/Thiadiazole,Pyridine,Quinoline/Quinazoline 555.67 5.1 Array BioPharma (USA) C28H25N7O2S2 Hinklin, R. J. et al. Discovery and preclinical development of AR453588 as an anti-diabetic glucokinase activator. Bioorganic Med. Chem. (2020) 59291604 1447
GKA59-75 GKA59-75 GKA: Systemic 2020 Thiazole/Thiadiazole,Pyridine 508.62 3.14 Array BioPharma (USA) C23H24N8O2S2 Hinklin, R. J. et al. Discovery and preclinical development of AR453588 as an anti-diabetic glucokinase activator. Bioorganic Med. Chem. (2020) 59291753 1448
GKA60-12 GKA60-12 GKA: Systemic 2020 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 331.8 2.6 R.C. Patel Institute of Pharmaceutical Education and Research (Shirpur, INDIA) C11H10ClN3O3S2 Khadse, S. C. et al. Hetero-substituted sulfonamido-benzamide hybrids as glucokinase activators: Design, synthesis, molecular docking and in-silico ADME evaluation. J. Mol. Struct. (2020) 1449
GKA60-13 GKA60-13 GKA: Systemic 2020 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 383.44 1.83 R.C. Patel Institute of Pharmaceutical Education and Research (Shirpur, INDIA) C15H17N3O5S2 Khadse, S. C. et al. Hetero-substituted sulfonamido-benzamide hybrids as glucokinase activators: Design, synthesis, molecular docking and in-silico ADME evaluation. J. Mol. Struct. (2020) 1450
GKA60-14 GKA60-14 GKA: Systemic 2020 Benzamide,Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 329.37 2.4 R.C. Patel Institute of Pharmaceutical Education and Research (Shirpur, INDIA) C16H15N3O3S Khadse, S. C. et al. Hetero-substituted sulfonamido-benzamide hybrids as glucokinase activators: Design, synthesis, molecular docking and in-silico ADME evaluation. J. Mol. Struct. (2020) 1451
GKA60-15 GKA60-15 GKA: Systemic 2020 Benzamide,Benzo/Pyrido-thiazole,Sulfoxide/Sulfone derivatives 361.44 3.43 R.C. Patel Institute of Pharmaceutical Education and Research (Shirpur, INDIA) C16H15N3O3S2 Khadse, S. C. et al. Hetero-substituted sulfonamido-benzamide hybrids as glucokinase activators: Design, synthesis, molecular docking and in-silico ADME evaluation. J. Mol. Struct. (2020) 78793628 1452
GKA60-16 GKA60-16 GKA: Systemic 2020 Benzamide,Sulfoxide/Sulfone derivatives 294.33 0.92 R.C. Patel Institute of Pharmaceutical Education and Research (Shirpur, INDIA) C12H14N4O3S Khadse, S. C. et al. Hetero-substituted sulfonamido-benzamide hybrids as glucokinase activators: Design, synthesis, molecular docking and in-silico ADME evaluation. J. Mol. Struct. (2020) 47020087 1453
GKA60-17 GKA60-17 GKA: Systemic 2020 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 312.37 1.45 R.C. Patel Institute of Pharmaceutical Education and Research (Shirpur, INDIA) C11H12N4O3S2 Khadse, S. C. et al. Hetero-substituted sulfonamido-benzamide hybrids as glucokinase activators: Design, synthesis, molecular docking and in-silico ADME evaluation. J. Mol. Struct. (2020) 53525451 1454
GKA60-18 GKA60-18 GKA: Systemic 2020 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 370.4 1.6 R.C. Patel Institute of Pharmaceutical Education and Research (Shirpur, INDIA) C13H14N4O5S2 Khadse, S. C. et al. Hetero-substituted sulfonamido-benzamide hybrids as glucokinase activators: Design, synthesis, molecular docking and in-silico ADME evaluation. J. Mol. Struct. (2020) 1455
GKA60-19 GKA60-19 GKA: Systemic 2020 Benzamide,Pyrazine,Sulfoxide/Sulfone derivatives 292.31 0.47 R.C. Patel Institute of Pharmaceutical Education and Research (Shirpur, INDIA) C12H12N4O3S Khadse, S. C. et al. Hetero-substituted sulfonamido-benzamide hybrids as glucokinase activators: Design, synthesis, molecular docking and in-silico ADME evaluation. J. Mol. Struct. (2020) 1456
GKA60-20 GKA60-20 GKA: Systemic 2020 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 312.37 1.84 R.C. Patel Institute of Pharmaceutical Education and Research (Shirpur, INDIA) C11H12N4O3S2 Khadse, S. C. et al. Hetero-substituted sulfonamido-benzamide hybrids as glucokinase activators: Design, synthesis, molecular docking and in-silico ADME evaluation. J. Mol. Struct. (2020) 1457
GKA60-21 GKA60-21 GKA: Systemic 2020 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 407.89 4.52 R.C. Patel Institute of Pharmaceutical Education and Research (Shirpur, INDIA) C17H14ClN3O3S2 Khadse, S. C. et al. Hetero-substituted sulfonamido-benzamide hybrids as glucokinase activators: Design, synthesis, molecular docking and in-silico ADME evaluation. J. Mol. Struct. (2020) 1458
GKA60-22 GKA60-22 GKA: Systemic 2020 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 459.54 3.75 R.C. Patel Institute of Pharmaceutical Education and Research (Shirpur, INDIA) C21H21N3O5S2 Khadse, S. C. et al. Hetero-substituted sulfonamido-benzamide hybrids as glucokinase activators: Design, synthesis, molecular docking and in-silico ADME evaluation. J. Mol. Struct. (2020) 1459
GKA60-23 GKA60-23 GKA: Systemic 2020 Benzamide,Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 405.47 4.32 R.C. Patel Institute of Pharmaceutical Education and Research (Shirpur, INDIA) C22H19N3O3S Khadse, S. C. et al. Hetero-substituted sulfonamido-benzamide hybrids as glucokinase activators: Design, synthesis, molecular docking and in-silico ADME evaluation. J. Mol. Struct. (2020) 1460
GKA60-24 GKA60-24 GKA: Systemic 2020 Benzamide,Benzo/Pyrido-thiazole,Sulfoxide/Sulfone derivatives 437.53 5.35 R.C. Patel Institute of Pharmaceutical Education and Research (Shirpur, INDIA) C22H19N3O3S2 Khadse, S. C. et al. Hetero-substituted sulfonamido-benzamide hybrids as glucokinase activators: Design, synthesis, molecular docking and in-silico ADME evaluation. J. Mol. Struct. (2020) 5055191 1461
GKA60-25 GKA60-25 GKA: Systemic 2020 Benzamide,Sulfoxide/Sulfone derivatives 370.43 2.84 R.C. Patel Institute of Pharmaceutical Education and Research (Shirpur, INDIA) C18H18N4O3S Khadse, S. C. et al. Hetero-substituted sulfonamido-benzamide hybrids as glucokinase activators: Design, synthesis, molecular docking and in-silico ADME evaluation. J. Mol. Struct. (2020) 1462
GKA60-26 GKA60-26 GKA: Systemic 2020 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 388.46 3.37 R.C. Patel Institute of Pharmaceutical Education and Research (Shirpur, INDIA) C17H16N4O3S2 Khadse, S. C. et al. Hetero-substituted sulfonamido-benzamide hybrids as glucokinase activators: Design, synthesis, molecular docking and in-silico ADME evaluation. J. Mol. Struct. (2020) 1463
GKA60-27 GKA60-27 GKA: Systemic 2020 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 446.5 3.53 R.C. Patel Institute of Pharmaceutical Education and Research (Shirpur, INDIA) C19H18N4O5S2 Khadse, S. C. et al. Hetero-substituted sulfonamido-benzamide hybrids as glucokinase activators: Design, synthesis, molecular docking and in-silico ADME evaluation. J. Mol. Struct. (2020) 1464
GKA60-28 GKA60-28 GKA: Systemic 2020 Benzamide,Pyrazine,Sulfoxide/Sulfone derivatives 368.41 2.39 R.C. Patel Institute of Pharmaceutical Education and Research (Shirpur, INDIA) C18H16N4O3S Khadse, S. C. et al. Hetero-substituted sulfonamido-benzamide hybrids as glucokinase activators: Design, synthesis, molecular docking and in-silico ADME evaluation. J. Mol. Struct. (2020) 1465
GKA60-29 GKA60-29 GKA: Systemic 2020 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 388.46 3.76 R.C. Patel Institute of Pharmaceutical Education and Research (Shirpur, INDIA) C17H16N4O3S2 Khadse, S. C. et al. Hetero-substituted sulfonamido-benzamide hybrids as glucokinase activators: Design, synthesis, molecular docking and in-silico ADME evaluation. J. Mol. Struct. (2020) 1466
GKA6-10 GKA6-10 GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide 355.41 3.89 Banyu Tsukuba Research Institute (JAPAN) C18H17N3O3S Nishimura, T. et al. Identification of novel and potent 2-amino benzamide derivatives as allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 23067415 130
GKA6-11 GKA6-11 GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 403.48 3.16 Banyu Tsukuba Research Institute (JAPAN) C18H17N3O4S2 Nishimura, T. et al. Identification of novel and potent 2-amino benzamide derivatives as allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 10476292 131
GKA6-12 GKA6-12 GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide 293.41 3.27 Banyu Tsukuba Research Institute (JAPAN) C13H15N3OS2 Nishimura, T. et al. Identification of novel and potent 2-amino benzamide derivatives as allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 23067445 132
GKA6-13 GKA6-13 GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide 341.45 4.46 Banyu Tsukuba Research Institute (JAPAN) C17H15N3OS2 Nishimura, T. et al. Identification of novel and potent 2-amino benzamide derivatives as allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 44564986 133
GKA6-14 GKA6-14 GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Pyridine 342.44 3.72 Banyu Tsukuba Research Institute (JAPAN) C16H14N4OS2 Nishimura, T. et al. Identification of novel and potent 2-amino benzamide derivatives as allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 44564987 134
GKA61-4a GKA61-4a GKA: Systemic 2020 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 378.47 2.46 Mitsubishi Tanabe Pharma Corporation (Osaka, JAPAN) C16H18N4O3S2 Sugama, H. et al. Design, synthesis, and pharmacological evaluation of 2-(4-sulfonylphenyl)-2-[(E)-pyrrolidin-1-ylimino]-N-thiazoleacetamides as glucokinase activators. Bioorganic Med. Chem. Lett. (2020) 160495336 1467
GKA6-15 GKA6-15 GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide 331.42 2.93 Banyu Tsukuba Research Institute (JAPAN) C14H13N5OS2 Nishimura, T. et al. Identification of novel and potent 2-amino benzamide derivatives as allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 44564988 135
GKA61-5a GKA61-5a GKA: Systemic 2020 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 404.51 3.02 Mitsubishi Tanabe Pharma Corporation (Osaka, JAPAN) C18H20N4O3S2 Sugama, H. et al. Design, synthesis, and pharmacological evaluation of 2-(4-sulfonylphenyl)-2-[(E)-pyrrolidin-1-ylimino]-N-thiazoleacetamides as glucokinase activators. Bioorganic Med. Chem. Lett. (2020) 156018142 1468
GKA61-5b GKA61-5b GKA: Systemic 2020 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 438.95 3.98 Mitsubishi Tanabe Pharma Corporation (Osaka, JAPAN) C18H19ClN4O3S2 Sugama, H. et al. Design, synthesis, and pharmacological evaluation of 2-(4-sulfonylphenyl)-2-[(E)-pyrrolidin-1-ylimino]-N-thiazoleacetamides as glucokinase activators. Bioorganic Med. Chem. Lett. (2020) 156016426 1469
GKA61-5c GKA61-5c GKA: Systemic 2020 Pyridine,Sulfoxide/Sulfone derivatives 398.48 2.92 Mitsubishi Tanabe Pharma Corporation (Osaka, JAPAN) C20H22N4O3S Sugama, H. et al. Design, synthesis, and pharmacological evaluation of 2-(4-sulfonylphenyl)-2-[(E)-pyrrolidin-1-ylimino]-N-thiazoleacetamides as glucokinase activators. Bioorganic Med. Chem. Lett. (2020) 156012365 1470
GKA61-5d GKA61-5d GKA: Systemic 2020 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 405.49 2.82 Mitsubishi Tanabe Pharma Corporation (Osaka, JAPAN) C17H19N5O3S2 Sugama, H. et al. Design, synthesis, and pharmacological evaluation of 2-(4-sulfonylphenyl)-2-[(E)-pyrrolidin-1-ylimino]-N-thiazoleacetamides as glucokinase activators. Bioorganic Med. Chem. Lett. (2020) 152777390 1471
GKA61-5e GKA61-5e GKA: Systemic 2020 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 418.53 3.42 Mitsubishi Tanabe Pharma Corporation (Osaka, JAPAN) C19H22N4O3S2 Sugama, H. et al. Design, synthesis, and pharmacological evaluation of 2-(4-sulfonylphenyl)-2-[(E)-pyrrolidin-1-ylimino]-N-thiazoleacetamides as glucokinase activators. Bioorganic Med. Chem. Lett. (2020) 156010722 1472
GKA61-5f GKA61-5f GKA: Systemic 2020 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 419.52 2.83 Mitsubishi Tanabe Pharma Corporation (Osaka, JAPAN) C18H21N5O3S2 Sugama, H. et al. Design, synthesis, and pharmacological evaluation of 2-(4-sulfonylphenyl)-2-[(E)-pyrrolidin-1-ylimino]-N-thiazoleacetamides as glucokinase activators. Bioorganic Med. Chem. Lett. (2020) 156012575 1473
GKA61-5g GKA61-5g GKA: Systemic 2020 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 516.68 2.7 Mitsubishi Tanabe Pharma Corporation (Osaka, JAPAN) C24H32N6O3S2 Sugama, H. et al. Design, synthesis, and pharmacological evaluation of 2-(4-sulfonylphenyl)-2-[(E)-pyrrolidin-1-ylimino]-N-thiazoleacetamides as glucokinase activators. Bioorganic Med. Chem. Lett. (2020) 147486984 1474
GKA61-5h GKA61-5h GKA: Systemic 2020 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 544.69 2.16 Mitsubishi Tanabe Pharma Corporation (Osaka, JAPAN) C25H32N6O4S2 Sugama, H. et al. Design, synthesis, and pharmacological evaluation of 2-(4-sulfonylphenyl)-2-[(E)-pyrrolidin-1-ylimino]-N-thiazoleacetamides as glucokinase activators. Bioorganic Med. Chem. Lett. (2020) 156017587 1475
GKA6-16 GKA6-16 GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide 345.44 2.89 Banyu Tsukuba Research Institute (JAPAN) C15H15N5OS2 Nishimura, T. et al. Identification of novel and potent 2-amino benzamide derivatives as allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 44564989 136
GKA6-17 GKA6-17 GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide 332.4 2.35 Banyu Tsukuba Research Institute (JAPAN) C13H12N6OS2 Nishimura, T. et al. Identification of novel and potent 2-amino benzamide derivatives as allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 23067404 137
GKA6-18 GKA6-18 GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide 346.43 2.3 Banyu Tsukuba Research Institute (JAPAN) C14H14N6OS2 Nishimura, T. et al. Identification of novel and potent 2-amino benzamide derivatives as allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 9819610 138
GKA6-19 GKA6-19 GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide 333.39 1.7 Banyu Tsukuba Research Institute (JAPAN) C12H11N7OS2 Nishimura, T. et al. Identification of novel and potent 2-amino benzamide derivatives as allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 44565039 139
GKA6-1a GKA6-1a GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide 253.71 2.62 Banyu Tsukuba Research Institute (JAPAN) C10H8ClN3OS Nishimura, T. et al. Identification of novel and potent 2-amino benzamide derivatives as allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 16770707 120
GKA6-1b GKA6-1b GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide 267.73 3.02 Banyu Tsukuba Research Institute (JAPAN) C11H10ClN3OS Nishimura, T. et al. Identification of novel and potent 2-amino benzamide derivatives as allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 20119572 121
GKA6-2 GKA6-2 GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide 219.26 1.99 Banyu Tsukuba Research Institute (JAPAN) C10H9N3OS Nishimura, T. et al. Identification of novel and potent 2-amino benzamide derivatives as allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 847246 122
GKA6-20 GKA6-20 GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide 347.42 2.1 Banyu Tsukuba Research Institute (JAPAN) C13H13N7OS2 Nishimura, T. et al. Identification of novel and potent 2-amino benzamide derivatives as allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 44565040 140
GKA6-21 GKA6-21 GKA: Systemic 2009 Benzamide,Pyridine 326.38 1.8 Banyu Tsukuba Research Institute (JAPAN) C15H14N6OS Nishimura, T. et al. Identification of novel and potent 2-amino benzamide derivatives as allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 44565041 141
GKA6-22 GKA6-22 GKA: Systemic 2009 Benzamide,Pyridine 326.38 1.46 Banyu Tsukuba Research Institute (JAPAN) C15H14N6OS Nishimura, T. et al. Identification of novel and potent 2-amino benzamide derivatives as allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 44565042 142
GKA6-23 GKA6-23 GKA: Systemic 2009 Benzamide,Pyridine 326.38 1.46 Banyu Tsukuba Research Institute (JAPAN) C15H14N6OS Nishimura, T. et al. Identification of novel and potent 2-amino benzamide derivatives as allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 44565084 143
GKA6-24 GKA6-24 GKA: Systemic 2009 Benzamide 325.39 2.53 Banyu Tsukuba Research Institute (JAPAN) C16H15N5OS Nishimura, T. et al. Identification of novel and potent 2-amino benzamide derivatives as allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 44565085 144
GKA6-25 GKA6-25 GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide 332.4 1.9 Banyu Tsukuba Research Institute (JAPAN) C13H12N6OS2 Nishimura, T. et al. Identification of novel and potent 2-amino benzamide derivatives as allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 44565086 145
GKA6-26 GKA6-26 GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide 346.43 2.3 Banyu Tsukuba Research Institute (JAPAN) C14H14N6OS2 Nishimura, T. et al. Identification of novel and potent 2-amino benzamide derivatives as allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 44565087 146
GKA6-27 GKA6-27 GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide 404.47 2.45 Banyu Tsukuba Research Institute (JAPAN) C16H16N6O3S2 Nishimura, T. et al. Identification of novel and potent 2-amino benzamide derivatives as allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 44565088 147
GKA6-28 GKA6-28 GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide 362.43 1.05 Banyu Tsukuba Research Institute (JAPAN) C14H14N6O2S2 Nishimura, T. et al. Identification of novel and potent 2-amino benzamide derivatives as allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 44565089 148
GKA6-29 GKA6-29 GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide 400.4 2.82 Banyu Tsukuba Research Institute (JAPAN) C14H11F3N6OS2 Nishimura, T. et al. Identification of novel and potent 2-amino benzamide derivatives as allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 44565138 149
GKA6-3 GKA6-3 GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide 267.73 3.02 Banyu Tsukuba Research Institute (JAPAN) C11H10ClN3OS Nishimura, T. et al. Identification of novel and potent 2-amino benzamide derivatives as allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 20119064 123
GKA6-30 GKA6-30 GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide 331.42 2.43 Banyu Tsukuba Research Institute (JAPAN) C14H13N5OS2 Nishimura, T. et al. Identification of novel and potent 2-amino benzamide derivatives as allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 44593462 150
GKA6-31 GKA6-31 GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide 376.41 2.26 Banyu Tsukuba Research Institute (JAPAN) C14H12N6O3S2 Nishimura, T. et al. Identification of novel and potent 2-amino benzamide derivatives as allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 44565139 151
GKA6-32 GKA6-32 GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide 360.46 2.96 Banyu Tsukuba Research Institute (JAPAN) C15H16N6OS2 Nishimura, T. et al. Identification of novel and potent 2-amino benzamide derivatives as allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 25229552 152
GKA6-4 GKA6-4 GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide 252.72 3.15 Banyu Tsukuba Research Institute (JAPAN) C11H9ClN2OS Nishimura, T. et al. Identification of novel and potent 2-amino benzamide derivatives as allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 899301 124
GKA6-5 GKA6-5 GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide 277.34 2.73 Banyu Tsukuba Research Institute (JAPAN) C13H15N3O2S Nishimura, T. et al. Identification of novel and potent 2-amino benzamide derivatives as allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 44564889 125
GKA6-6 GKA6-6 GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide 325.38 3.92 Banyu Tsukuba Research Institute (JAPAN) C17H15N3O2S Nishimura, T. et al. Identification of novel and potent 2-amino benzamide derivatives as allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 23067400 126
GKA6-7 GKA6-7 GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide 343.38 4.02 Banyu Tsukuba Research Institute (JAPAN) C17H14FN3O2S Nishimura, T. et al. Identification of novel and potent 2-amino benzamide derivatives as allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 44564932 127
GKA6-8 GKA6-8 GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide 343.38 4.02 Banyu Tsukuba Research Institute (JAPAN) C17H14FN3O2S Nishimura, T. et al. Identification of novel and potent 2-amino benzamide derivatives as allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 44564933 128
GKA6-9 GKA6-9 GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide 343.38 4.02 Banyu Tsukuba Research Institute (JAPAN) C17H14FN3O2S Nishimura, T. et al. Identification of novel and potent 2-amino benzamide derivatives as allosteric glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 23067440 129
GKA7-16a GKA7-16a GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 480.56 4.82 Banyu Tsukuba Research Institute (JAPAN) C24H20N2O5S2 Iino, T. et al. Discovery of potent and orally active 3-alkoxy-5-phenoxy-N-thiazolyl benzamides as novel allosteric glucokinase activators. Bioorganic Med. Chem. (2009) 44572361 165
GKA7-16b GKA7-16b GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 480.56 4.82 Banyu Tsukuba Research Institute (JAPAN) C24H20N2O5S2 Iino, T. et al. Discovery of potent and orally active 3-alkoxy-5-phenoxy-N-thiazolyl benzamides as novel allosteric glucokinase activators. Bioorganic Med. Chem. (2009) 44572411 166
GKA7-16c GKA7-16c GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 480.56 4.82 Banyu Tsukuba Research Institute (JAPAN) C24H20N2O5S2 Iino, T. et al. Discovery of potent and orally active 3-alkoxy-5-phenoxy-N-thiazolyl benzamides as novel allosteric glucokinase activators. Bioorganic Med. Chem. (2009) 44572412 167
GKA7-20a GKA7-20a GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 446.54 4.06 Banyu Tsukuba Research Institute (JAPAN) C21H22N2O5S2 Iino, T. et al. Discovery of potent and orally active 3-alkoxy-5-phenoxy-N-thiazolyl benzamides as novel allosteric glucokinase activators. Bioorganic Med. Chem. (2009) 44572299 168
GKA7-20b GKA7-20b GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 480.56 4.82 Banyu Tsukuba Research Institute (JAPAN) C24H20N2O5S2 Iino, T. et al. Discovery of potent and orally active 3-alkoxy-5-phenoxy-N-thiazolyl benzamides as novel allosteric glucokinase activators. Bioorganic Med. Chem. (2009) 44572300 169
GKA7-27a GKA7-27a GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 418.49 3.26 Banyu Tsukuba Research Institute (JAPAN) C19H18N2O5S2 Iino, T. et al. Discovery of potent and orally active 3-alkoxy-5-phenoxy-N-thiazolyl benzamides as novel allosteric glucokinase activators. Bioorganic Med. Chem. (2009) 44572358 170
GKA7-27b GKA7-27b GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 432.51 3.63 Banyu Tsukuba Research Institute (JAPAN) C20H20N2O5S2 Iino, T. et al. Discovery of potent and orally active 3-alkoxy-5-phenoxy-N-thiazolyl benzamides as novel allosteric glucokinase activators. Bioorganic Med. Chem. (2009) 44572359 171
GKA7-27c GKA7-27c GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 446.54 4.06 Banyu Tsukuba Research Institute (JAPAN) C21H22N2O5S2 Iino, T. et al. Discovery of potent and orally active 3-alkoxy-5-phenoxy-N-thiazolyl benzamides as novel allosteric glucokinase activators. Bioorganic Med. Chem. (2009) 44572360 172
GKA7-27d GKA7-27d GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 446.54 4.06 Banyu Tsukuba Research Institute (JAPAN) C21H22N2O5S2 Iino, T. et al. Discovery of potent and orally active 3-alkoxy-5-phenoxy-N-thiazolyl benzamides as novel allosteric glucokinase activators. Bioorganic Med. Chem. (2009) 44572413 173
GKA7-27e GKA7-27e GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 446.54 4.06 Banyu Tsukuba Research Institute (JAPAN) C21H22N2O5S2 Iino, T. et al. Discovery of potent and orally active 3-alkoxy-5-phenoxy-N-thiazolyl benzamides as novel allosteric glucokinase activators. Bioorganic Med. Chem. (2009) 9868203 174
GKA7-7a GKA7-7a GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide 310.37 4.05 Banyu Tsukuba Research Institute (JAPAN) C17H14N2O2S Iino, T. et al. Discovery of potent and orally active 3-alkoxy-5-phenoxy-N-thiazolyl benzamides as novel allosteric glucokinase activators. Bioorganic Med. Chem. (2009) 2092675 153
GKA7-7b GKA7-7b GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide 328.36 4.15 Banyu Tsukuba Research Institute (JAPAN) C17H13FN2O2S Iino, T. et al. Discovery of potent and orally active 3-alkoxy-5-phenoxy-N-thiazolyl benzamides as novel allosteric glucokinase activators. Bioorganic Med. Chem. (2009) 44572162 154
GKA7-7c GKA7-7c GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide 328.36 4.15 Banyu Tsukuba Research Institute (JAPAN) C17H13FN2O2S Iino, T. et al. Discovery of potent and orally active 3-alkoxy-5-phenoxy-N-thiazolyl benzamides as novel allosteric glucokinase activators. Bioorganic Med. Chem. (2009) 44572202 155
GKA7-7d GKA7-7d GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide 328.36 4.15 Banyu Tsukuba Research Institute (JAPAN) C17H13FN2O2S Iino, T. et al. Discovery of potent and orally active 3-alkoxy-5-phenoxy-N-thiazolyl benzamides as novel allosteric glucokinase activators. Bioorganic Med. Chem. (2009) 44572245 156
GKA7-7e GKA7-7e GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide 324.4 4.42 Banyu Tsukuba Research Institute (JAPAN) C18H16N2O2S Iino, T. et al. Discovery of potent and orally active 3-alkoxy-5-phenoxy-N-thiazolyl benzamides as novel allosteric glucokinase activators. Bioorganic Med. Chem. (2009) 44572246 157
GKA7-7f GKA7-7f GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide 324.4 4.42 Banyu Tsukuba Research Institute (JAPAN) C18H16N2O2S Iino, T. et al. Discovery of potent and orally active 3-alkoxy-5-phenoxy-N-thiazolyl benzamides as novel allosteric glucokinase activators. Bioorganic Med. Chem. (2009) 44572247 158
GKA7-7g GKA7-7g GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide 324.4 4.42 Banyu Tsukuba Research Institute (JAPAN) C18H16N2O2S Iino, T. et al. Discovery of potent and orally active 3-alkoxy-5-phenoxy-N-thiazolyl benzamides as novel allosteric glucokinase activators. Bioorganic Med. Chem. (2009) 44572248 159
GKA7-7h GKA7-7h GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 388.46 3.29 Banyu Tsukuba Research Institute (JAPAN) C18H16N2O4S2 Iino, T. et al. Discovery of potent and orally active 3-alkoxy-5-phenoxy-N-thiazolyl benzamides as novel allosteric glucokinase activators. Bioorganic Med. Chem. (2009) 44572249 160
GKA7-7i GKA7-7i GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 388.46 3.29 Banyu Tsukuba Research Institute (JAPAN) C18H16N2O4S2 Iino, T. et al. Discovery of potent and orally active 3-alkoxy-5-phenoxy-N-thiazolyl benzamides as novel allosteric glucokinase activators. Bioorganic Med. Chem. (2009) 44572250 161
GKA7-7j GKA7-7j GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Sulfoxide/Sulfone derivatives 388.46 3.29 Banyu Tsukuba Research Institute (JAPAN) C18H16N2O4S2 Iino, T. et al. Discovery of potent and orally active 3-alkoxy-5-phenoxy-N-thiazolyl benzamides as novel allosteric glucokinase activators. Bioorganic Med. Chem. (2009) 44572296 162
GKA7-7k GKA7-7k GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide 340.4 4.02 Banyu Tsukuba Research Institute (JAPAN) C18H16N2O3S Iino, T. et al. Discovery of potent and orally active 3-alkoxy-5-phenoxy-N-thiazolyl benzamides as novel allosteric glucokinase activators. Bioorganic Med. Chem. (2009) 44572297 163
GKA7-7l GKA7-7l GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide 354.42 4.39 Banyu Tsukuba Research Institute (JAPAN) C19H18N2O3S Iino, T. et al. Discovery of potent and orally active 3-alkoxy-5-phenoxy-N-thiazolyl benzamides as novel allosteric glucokinase activators. Bioorganic Med. Chem. (2009) 44572298 164
GKA8-10 GKA8-10 GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Pyridine 412.51 3.74 Banyu Tsukuba Research Institute (JAPAN) C17H12N6OS3 Mitsuya, M. et al. Discovery of novel 3,6-disubstituted 2-pyridinecarboxamide derivatives as GK activators. Bioorganic Med. Chem. Lett. (2009) 10454363 182
GKA8-11 GKA8-11 GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Pyridine 442.54 3.71 Banyu Tsukuba Research Institute (JAPAN) C18H14N6O2S3 Mitsuya, M. et al. Discovery of novel 3,6-disubstituted 2-pyridinecarboxamide derivatives as GK activators. Bioorganic Med. Chem. Lett. (2009) 23092601 183
GKA8-12 GKA8-12 GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Pyridine 480.51 4.63 Banyu Tsukuba Research Institute (JAPAN) C18H11F3N6OS3 Mitsuya, M. et al. Discovery of novel 3,6-disubstituted 2-pyridinecarboxamide derivatives as GK activators. Bioorganic Med. Chem. Lett. (2009) 10412882 184
GKA8-13 GKA8-13 GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Pyridine 442.54 3.71 Banyu Tsukuba Research Institute (JAPAN) C18H14N6O2S3 Mitsuya, M. et al. Discovery of novel 3,6-disubstituted 2-pyridinecarboxamide derivatives as GK activators. Bioorganic Med. Chem. Lett. (2009) 45267160 185
GKA8-14 GKA8-14 GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Pyridine 426.54 4.11 Banyu Tsukuba Research Institute (JAPAN) C18H14N6OS3 Mitsuya, M. et al. Discovery of novel 3,6-disubstituted 2-pyridinecarboxamide derivatives as GK activators. Bioorganic Med. Chem. Lett. (2009) 45271402 186
GKA8-2 GKA8-2 GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide 360.46 2.96 Banyu Tsukuba Research Institute (JAPAN) C15H16N6OS2 Mitsuya, M. et al. Discovery of novel 3,6-disubstituted 2-pyridinecarboxamide derivatives as GK activators. Bioorganic Med. Chem. Lett. (2009) 25229552 175
GKA8-4 GKA8-4 GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Pyridine 458.56 4.2 Banyu Tsukuba Research Institute (JAPAN) C19H15FN6OS3 Mitsuya, M. et al. Discovery of novel 3,6-disubstituted 2-pyridinecarboxamide derivatives as GK activators. Bioorganic Med. Chem. Lett. (2009) 10411846 176
GKA8-5 GKA8-5 GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide 457.57 4.6 Banyu Tsukuba Research Institute (JAPAN) C20H16FN5OS3 Mitsuya, M. et al. Discovery of novel 3,6-disubstituted 2-pyridinecarboxamide derivatives as GK activators. Bioorganic Med. Chem. Lett. (2009) 45270565 177
GKA8-6 GKA8-6 GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Pyridine 444.53 3.79 Banyu Tsukuba Research Institute (JAPAN) C18H13FN6OS3 Mitsuya, M. et al. Discovery of novel 3,6-disubstituted 2-pyridinecarboxamide derivatives as GK activators. Bioorganic Med. Chem. Lett. (2009) 45273147 178
GKA8-7 GKA8-7 GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Pyridine 430.5 3.84 Banyu Tsukuba Research Institute (JAPAN) C17H11FN6OS3 Mitsuya, M. et al. Discovery of novel 3,6-disubstituted 2-pyridinecarboxamide derivatives as GK activators. Bioorganic Med. Chem. Lett. (2009) 10342654 179
GKA8-8 GKA8-8 GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Pyridine 430.5 3.84 Banyu Tsukuba Research Institute (JAPAN) C17H11FN6OS3 Mitsuya, M. et al. Discovery of novel 3,6-disubstituted 2-pyridinecarboxamide derivatives as GK activators. Bioorganic Med. Chem. Lett. (2009) 10432843 180
GKA8-9 GKA8-9 GKA: Systemic 2009 Thiazole/Thiadiazole,Benzamide,Pyridine 430.5 3.84 Banyu Tsukuba Research Institute (JAPAN) C17H11FN6OS3 Mitsuya, M. et al. Discovery of novel 3,6-disubstituted 2-pyridinecarboxamide derivatives as GK activators. Bioorganic Med. Chem. Lett. (2009) 10455369 181
GKA9-14a GKA9-14a GKA: Systemic 2009 Pyridine,Indole/Benzimidazole/Indazole 374.41 3.64 Banyu Tsukuba Research Institute (JAPAN) C22H19FN4O Ishikawa, M. et al. Discovery of novel 2-(pyridine-2-yl)-1H-benzimidazole derivatives as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 23145575 191
GKA9-15a GKA9-15a GKA: Systemic 2009 Pyridine,Indole/Benzimidazole/Indazole 388.44 4.1 Banyu Tsukuba Research Institute (JAPAN) C23H21FN4O Ishikawa, M. et al. Discovery of novel 2-(pyridine-2-yl)-1H-benzimidazole derivatives as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 45271096 192
GKA9-15b GKA9-15b GKA: Systemic 2009 Pyridine,Indole/Benzimidazole/Indazole 402.46 4.47 Banyu Tsukuba Research Institute (JAPAN) C24H23FN4O Ishikawa, M. et al. Discovery of novel 2-(pyridine-2-yl)-1H-benzimidazole derivatives as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 45272809 193
GKA9-15c GKA9-15c GKA: Systemic 2009 Pyridine,Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 452.5 3.35 Banyu Tsukuba Research Institute (JAPAN) C23H21FN4O3S Ishikawa, M. et al. Discovery of novel 2-(pyridine-2-yl)-1H-benzimidazole derivatives as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 23145556 194
GKA9-15d GKA9-15d GKA: Systemic 2009 Pyridine,Indole/Benzimidazole/Indazole 445.49 3.76 Banyu Tsukuba Research Institute (JAPAN) C25H24FN5O2 Ishikawa, M. et al. Discovery of novel 2-(pyridine-2-yl)-1H-benzimidazole derivatives as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 45269441 195
GKA9-15e GKA9-15e GKA: Systemic 2009 Pyridine,Indole/Benzimidazole/Indazole 416.45 3.56 Banyu Tsukuba Research Institute (JAPAN) C24H21FN4O2 Ishikawa, M. et al. Discovery of novel 2-(pyridine-2-yl)-1H-benzimidazole derivatives as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 23145594 196
GKA9-15f GKA9-15f GKA: Systemic 2009 Pyridine,Indole/Benzimidazole/Indazole 430.47 4.03 Banyu Tsukuba Research Institute (JAPAN) C25H23FN4O2 Ishikawa, M. et al. Discovery of novel 2-(pyridine-2-yl)-1H-benzimidazole derivatives as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 23145280 197
GKA9-15g GKA9-15g GKA: Systemic 2009 Pyridine,Indole/Benzimidazole/Indazole 478.52 5.22 Banyu Tsukuba Research Institute (JAPAN) C29H23FN4O2 Ishikawa, M. et al. Discovery of novel 2-(pyridine-2-yl)-1H-benzimidazole derivatives as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 45272819 198
GKA9-16a GKA9-16a GKA: Systemic 2009 Pyridine,Indole/Benzimidazole/Indazole 398.46 3.46 Banyu Tsukuba Research Institute (JAPAN) C24H22N4O2 Ishikawa, M. et al. Discovery of novel 2-(pyridine-2-yl)-1H-benzimidazole derivatives as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 45271999 199
GKA9-16b GKA9-16b GKA: Systemic 2009 Pyridine,Indole/Benzimidazole/Indazole 416.45 3.56 Banyu Tsukuba Research Institute (JAPAN) C24H21FN4O2 Ishikawa, M. et al. Discovery of novel 2-(pyridine-2-yl)-1H-benzimidazole derivatives as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 45272000 200
GKA9-16c GKA9-16c GKA: Systemic 2009 Pyridine,Indole/Benzimidazole/Indazole 416.45 3.56 Banyu Tsukuba Research Institute (JAPAN) C24H21FN4O2 Ishikawa, M. et al. Discovery of novel 2-(pyridine-2-yl)-1H-benzimidazole derivatives as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 45267725 201
GKA9-16d GKA9-16d GKA: Systemic 2009 Pyridine,Indole/Benzimidazole/Indazole 428.48 3.43 Banyu Tsukuba Research Institute (JAPAN) C25H24N4O3 Ishikawa, M. et al. Discovery of novel 2-(pyridine-2-yl)-1H-benzimidazole derivatives as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 45272825 202
GKA9-16e GKA9-16e GKA: Systemic 2009 Pyridine,Indole/Benzimidazole/Indazole 428.48 3.43 Banyu Tsukuba Research Institute (JAPAN) C25H24N4O3 Ishikawa, M. et al. Discovery of novel 2-(pyridine-2-yl)-1H-benzimidazole derivatives as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 45271116 203
GKA9-16f GKA9-16f GKA: Systemic 2009 Pyridine,Indole/Benzimidazole/Indazole 428.48 3.43 Banyu Tsukuba Research Institute (JAPAN) C25H24N4O3 Ishikawa, M. et al. Discovery of novel 2-(pyridine-2-yl)-1H-benzimidazole derivatives as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 45271117 204
GKA9-16g GKA9-16g GKA: Systemic 2009 Pyridine,Indole/Benzimidazole/Indazole 423.47 3.18 Banyu Tsukuba Research Institute (JAPAN) C25H21N5O2 Ishikawa, M. et al. Discovery of novel 2-(pyridine-2-yl)-1H-benzimidazole derivatives as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 23145371 205
GKA9-16h GKA9-16h GKA: Systemic 2009 Pyridine,Indole/Benzimidazole/Indazole 423.47 3.18 Banyu Tsukuba Research Institute (JAPAN) C25H21N5O2 Ishikawa, M. et al. Discovery of novel 2-(pyridine-2-yl)-1H-benzimidazole derivatives as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 23145121 206
GKA9-16i GKA9-16i GKA: Systemic 2009 Pyridine,Indole/Benzimidazole/Indazole 423.47 3.18 Banyu Tsukuba Research Institute (JAPAN) C25H21N5O2 Ishikawa, M. et al. Discovery of novel 2-(pyridine-2-yl)-1H-benzimidazole derivatives as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 23145414 207
GKA9-16j GKA9-16j GKA: Systemic 2009 Pyridine,Indole/Benzimidazole/Indazole 474.55 5.09 Banyu Tsukuba Research Institute (JAPAN) C30H26N4O2 Ishikawa, M. et al. Discovery of novel 2-(pyridine-2-yl)-1H-benzimidazole derivatives as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 23145448 208
GKA9-16k GKA9-16k GKA: Systemic 2009 Pyridine,Indole/Benzimidazole/Indazole 474.55 5.09 Banyu Tsukuba Research Institute (JAPAN) C30H26N4O2 Ishikawa, M. et al. Discovery of novel 2-(pyridine-2-yl)-1H-benzimidazole derivatives as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 23145122 209
GKA9-16l GKA9-16l GKA: Systemic 2009 Pyridine,Indole/Benzimidazole/Indazole 441.48 2.34 Banyu Tsukuba Research Institute (JAPAN) C25H23N5O3 Ishikawa, M. et al. Discovery of novel 2-(pyridine-2-yl)-1H-benzimidazole derivatives as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 23145444 210
GKA9-16m GKA9-16m GKA: Systemic 2009 Pyridine,Indole/Benzimidazole/Indazole 470.52 3.68 Banyu Tsukuba Research Institute (JAPAN) C27H26N4O4 Ishikawa, M. et al. Discovery of novel 2-(pyridine-2-yl)-1H-benzimidazole derivatives as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 23145136 211
GKA9-16n GKA9-16n GKA: Systemic 2009 Pyridine,Indole/Benzimidazole/Indazole 443.45 3.29 Banyu Tsukuba Research Institute (JAPAN) C24H21N5O4 Ishikawa, M. et al. Discovery of novel 2-(pyridine-2-yl)-1H-benzimidazole derivatives as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 23145787 212
GKA9-16o GKA9-16o GKA: Systemic 2009 Pyridine,Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 476.55 2.7 Banyu Tsukuba Research Institute (JAPAN) C25H24N4O4S Ishikawa, M. et al. Discovery of novel 2-(pyridine-2-yl)-1H-benzimidazole derivatives as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 11179025 213
GKA9-16p__-R_ GKA9-16p (-R) GKA: Systemic 2009 Pyridine,Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 490.57 3.07 Banyu Tsukuba Research Institute (JAPAN) C26H26N4O4S Ishikawa, M. et al. Discovery of novel 2-(pyridine-2-yl)-1H-benzimidazole derivatives as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 44598465 215
GKA9-16p__racemic_ GKA9-16p (racemic) GKA: Systemic 2009 Pyridine,Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 490.57 3.07 Banyu Tsukuba Research Institute (JAPAN) C26H26N4O4S Ishikawa, M. et al. Discovery of novel 2-(pyridine-2-yl)-1H-benzimidazole derivatives as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 44598465 214
GKA9-16p__-S_ GKA9-16p (-S) GKA: Systemic 2009 Pyridine,Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 490.57 3.07 Banyu Tsukuba Research Institute (JAPAN) C26H26N4O4S Ishikawa, M. et al. Discovery of novel 2-(pyridine-2-yl)-1H-benzimidazole derivatives as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 45269468 216
GKA9-16q GKA9-16q GKA: Systemic 2009 Pyridine,Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 504.6 3.5 Banyu Tsukuba Research Institute (JAPAN) C27H28N4O4S Ishikawa, M. et al. Discovery of novel 2-(pyridine-2-yl)-1H-benzimidazole derivatives as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 45272843 217
GKA9-5a GKA9-5a GKA: Systemic 2009 Pyridine,Indole/Benzimidazole/Indazole 446.47 4.33 Banyu Tsukuba Research Institute (JAPAN) C25H23FN4O3 Ishikawa, M. et al. Discovery of novel 2-(pyridine-2-yl)-1H-benzimidazole derivatives as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 23145223 187
GKA9-5b GKA9-5b GKA: Systemic 2009 Pyridine,Indole/Benzimidazole/Indazole 446.47 4.3 Banyu Tsukuba Research Institute (JAPAN) C25H23FN4O3 Ishikawa, M. et al. Discovery of novel 2-(pyridine-2-yl)-1H-benzimidazole derivatives as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 45273766 188
GKA9-5c GKA9-5c GKA: Systemic 2009 Indole/Benzimidazole/Indazole 445.49 5.37 Banyu Tsukuba Research Institute (JAPAN) C26H24FN3O3 Ishikawa, M. et al. Discovery of novel 2-(pyridine-2-yl)-1H-benzimidazole derivatives as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 45271972 189
GKA9-5d GKA9-5d GKA: Systemic 2009 Pyridine,Indole/Benzimidazole/Indazole 460.5 4.25 Banyu Tsukuba Research Institute (JAPAN) C26H25FN4O3 Ishikawa, M. et al. Discovery of novel 2-(pyridine-2-yl)-1H-benzimidazole derivatives as potent glucokinase activators. Bioorganic Med. Chem. Lett. (2009) 45271973 190
GKI2-GLK1-001 GKI2-GLK1-001 TcGlcK (T.cruzi glucokinase) inhibitor 2019 Urea 301.12 1.7 University of South Carolina Beaufort (USA) C9H5BrN2O3S Mercaldi, G. F., D’Antonio, E. L., Aguessi, A., Rodriguez, A. & Cordeiro, A. T. Discovery of antichagasic inhibitors by high-throughput screening with Trypanosoma cruzi glucokinase. Bioorganic Med. Chem. Lett. (2019) 3121101 1680
GKI2-GLK1-002 GKI2-GLK1-002 TcGlcK (T.cruzi glucokinase) inhibitor 2019 Urea 248.19 0.25 University of South Carolina Beaufort (USA) C11H8N2O5 Mercaldi, G. F., D’Antonio, E. L., Aguessi, A., Rodriguez, A. & Cordeiro, A. T. Discovery of antichagasic inhibitors by high-throughput screening with Trypanosoma cruzi glucokinase. Bioorganic Med. Chem. Lett. (2019) 5337602 1681
GKI2-GLK1-003 GKI2-GLK1-003 TcGlcK (T.cruzi glucokinase) inhibitor 2019 Urea 260.2 1.68 University of South Carolina Beaufort (USA) C12H8N2O5 Mercaldi, G. F., D’Antonio, E. L., Aguessi, A., Rodriguez, A. & Cordeiro, A. T. Discovery of antichagasic inhibitors by high-throughput screening with Trypanosoma cruzi glucokinase. Bioorganic Med. Chem. Lett. (2019) 258209 1682
GKI2-GLK1-004 GKI2-GLK1-004 TcGlcK (T.cruzi glucokinase) inhibitor 2019 Urea 301.3 0.71 University of South Carolina Beaufort (USA) C15H15N3O4 Mercaldi, G. F., D’Antonio, E. L., Aguessi, A., Rodriguez, A. & Cordeiro, A. T. Discovery of antichagasic inhibitors by high-throughput screening with Trypanosoma cruzi glucokinase. Bioorganic Med. Chem. Lett. (2019) 2243878 1683
GKI2-GLK1-005 GKI2-GLK1-005 TcGlcK (T.cruzi glucokinase) inhibitor 2019 Urea 287.31 1.45 University of South Carolina Beaufort (USA) C15H17N3O3 Mercaldi, G. F., D’Antonio, E. L., Aguessi, A., Rodriguez, A. & Cordeiro, A. T. Discovery of antichagasic inhibitors by high-throughput screening with Trypanosoma cruzi glucokinase. Bioorganic Med. Chem. Lett. (2019) 93617 1684
GKI2-GLK1-006 GKI2-GLK1-006 TcGlcK (T.cruzi glucokinase) inhibitor 2019 Urea 433.3 3.85 University of South Carolina Beaufort (USA) C20H21BrN2O4 Mercaldi, G. F., D’Antonio, E. L., Aguessi, A., Rodriguez, A. & Cordeiro, A. T. Discovery of antichagasic inhibitors by high-throughput screening with Trypanosoma cruzi glucokinase. Bioorganic Med. Chem. Lett. (2019) 2919433 1685
GKI2-GLK1-007 GKI2-GLK1-007 TcGlcK (T.cruzi glucokinase) inhibitor 2019 Urea 358.35 3.54 University of South Carolina Beaufort (USA) C21H14N2O4 Mercaldi, G. F., D’Antonio, E. L., Aguessi, A., Rodriguez, A. & Cordeiro, A. T. Discovery of antichagasic inhibitors by high-throughput screening with Trypanosoma cruzi glucokinase. Bioorganic Med. Chem. Lett. (2019) 2288313 1686
GKI2-GLK2-001 GKI2-GLK2-001 TcGlcK (T.cruzi glucokinase) inhibitor 2019 313.3 3.44 University of South Carolina Beaufort (USA) C17H15NO5 Mercaldi, G. F., D’Antonio, E. L., Aguessi, A., Rodriguez, A. & Cordeiro, A. T. Discovery of antichagasic inhibitors by high-throughput screening with Trypanosoma cruzi glucokinase. Bioorganic Med. Chem. Lett. (2019) 729040 1687
GKI2-GLK2-002 GKI2-GLK2-002 TcGlcK (T.cruzi glucokinase) inhibitor 2019 341.36 4.17 University of South Carolina Beaufort (USA) C19H19NO5 Mercaldi, G. F., D’Antonio, E. L., Aguessi, A., Rodriguez, A. & Cordeiro, A. T. Discovery of antichagasic inhibitors by high-throughput screening with Trypanosoma cruzi glucokinase. Bioorganic Med. Chem. Lett. (2019) 705912 1688
GKI2-GLK2-003 GKI2-GLK2-003 TcGlcK (T.cruzi glucokinase) inhibitor 2019 406.23 4.5 University of South Carolina Beaufort (USA) C18H16BrNO5 Mercaldi, G. F., D’Antonio, E. L., Aguessi, A., Rodriguez, A. & Cordeiro, A. T. Discovery of antichagasic inhibitors by high-throughput screening with Trypanosoma cruzi glucokinase. Bioorganic Med. Chem. Lett. (2019) 1044490 1689
GKI2-GLK2-004 GKI2-GLK2-004 TcGlcK (T.cruzi glucokinase) inhibitor 2019 410.25 5.43 University of South Carolina Beaufort (USA) C19H17Cl2NO5 Mercaldi, G. F., D’Antonio, E. L., Aguessi, A., Rodriguez, A. & Cordeiro, A. T. Discovery of antichagasic inhibitors by high-throughput screening with Trypanosoma cruzi glucokinase. Bioorganic Med. Chem. Lett. (2019) 1826139 1690
GKI2-GLK2-005 GKI2-GLK2-005 TcGlcK (T.cruzi glucokinase) inhibitor 2019 347.32 4.56 University of South Carolina Beaufort (USA) C20H13NO5 Mercaldi, G. F., D’Antonio, E. L., Aguessi, A., Rodriguez, A. & Cordeiro, A. T. Discovery of antichagasic inhibitors by high-throughput screening with Trypanosoma cruzi glucokinase. Bioorganic Med. Chem. Lett. (2019) 706103 1691
GKI2-GLK3-001 GKI2-GLK3-001 TcGlcK (T.cruzi glucokinase) inhibitor 2019 437.29 4.66 University of South Carolina Beaufort (USA) C21H17BrN4O2 Mercaldi, G. F., D’Antonio, E. L., Aguessi, A., Rodriguez, A. & Cordeiro, A. T. Discovery of antichagasic inhibitors by high-throughput screening with Trypanosoma cruzi glucokinase. Bioorganic Med. Chem. Lett. (2019) 1035652 1692
GKI2-GLK3-002 GKI2-GLK3-002 TcGlcK (T.cruzi glucokinase) inhibitor 2019 346.36 4.1 University of South Carolina Beaufort (USA) C20H15FN4O Mercaldi, G. F., D’Antonio, E. L., Aguessi, A., Rodriguez, A. & Cordeiro, A. T. Discovery of antichagasic inhibitors by high-throughput screening with Trypanosoma cruzi glucokinase. Bioorganic Med. Chem. Lett. (2019) 690022 1693
GKI2-GLK3-003 GKI2-GLK3-003 TcGlcK (T.cruzi glucokinase) inhibitor 2019 332.36 3.43 University of South Carolina Beaufort (USA) C19H16N4O2 Mercaldi, G. F., D’Antonio, E. L., Aguessi, A., Rodriguez, A. & Cordeiro, A. T. Discovery of antichagasic inhibitors by high-throughput screening with Trypanosoma cruzi glucokinase. Bioorganic Med. Chem. Lett. (2019) 914511 1694
GKI2-GLK3-004 GKI2-GLK3-004 TcGlcK (T.cruzi glucokinase) inhibitor 2019 442.25 5.08 University of South Carolina Beaufort (USA) C20H13Cl2N5O3 Mercaldi, G. F., D’Antonio, E. L., Aguessi, A., Rodriguez, A. & Cordeiro, A. T. Discovery of antichagasic inhibitors by high-throughput screening with Trypanosoma cruzi glucokinase. Bioorganic Med. Chem. Lett. (2019) 1421359 1695
GKI2-GLK4-001 GKI2-GLK4-001 TcGlcK (T.cruzi glucokinase) inhibitor 2019 Sulfoxide/Sulfone derivatives 411.1 4.36 University of South Carolina Beaufort (USA) C13H10BrCl2NO3S Mercaldi, G. F., D’Antonio, E. L., Aguessi, A., Rodriguez, A. & Cordeiro, A. T. Discovery of antichagasic inhibitors by high-throughput screening with Trypanosoma cruzi glucokinase. Bioorganic Med. Chem. Lett. (2019) 17201016 1696
GKI2-GLK5-001 GKI2-GLK5-001 TcGlcK (T.cruzi glucokinase) inhibitor 2019 Sulfoxide/Sulfone derivatives 911.01 4.7 University of South Carolina Beaufort (USA) C44H46N8O10S2 Mercaldi, G. F., D’Antonio, E. L., Aguessi, A., Rodriguez, A. & Cordeiro, A. T. Discovery of antichagasic inhibitors by high-throughput screening with Trypanosoma cruzi glucokinase. Bioorganic Med. Chem. Lett. (2019) 135538499 1697
GKI2-GLK5-002 GKI2-GLK5-002 TcGlcK (T.cruzi glucokinase) inhibitor 2019 798.92 9.31 University of South Carolina Beaufort (USA) C50H46N4O6 Mercaldi, G. F., D’Antonio, E. L., Aguessi, A., Rodriguez, A. & Cordeiro, A. T. Discovery of antichagasic inhibitors by high-throughput screening with Trypanosoma cruzi glucokinase. Bioorganic Med. Chem. Lett. (2019) 24207239 1698
GKI2-GLK5-003 GKI2-GLK5-003 TcGlcK (T.cruzi glucokinase) inhibitor 2019 Sulfoxide/Sulfone derivatives 959 7.46 University of South Carolina Beaufort (USA) C50H42N2O14S2 Mercaldi, G. F., D’Antonio, E. L., Aguessi, A., Rodriguez, A. & Cordeiro, A. T. Discovery of antichagasic inhibitors by high-throughput screening with Trypanosoma cruzi glucokinase. Bioorganic Med. Chem. Lett. (2019) 24207241 1699
GKI2-GLK6-001 GKI2-GLK6-001 TcGlcK (T.cruzi glucokinase) inhibitor 2019 Pyridine,Subsituted ethynyl 312.45 2.48 University of South Carolina Beaufort (USA) C20H28N2O Mercaldi, G. F., D’Antonio, E. L., Aguessi, A., Rodriguez, A. & Cordeiro, A. T. Discovery of antichagasic inhibitors by high-throughput screening with Trypanosoma cruzi glucokinase. Bioorganic Med. Chem. Lett. (2019) 1509261 1700
GKI2-GLK6-002 GKI2-GLK6-002 TcGlcK (T.cruzi glucokinase) inhibitor 2019 Pyridine,Subsituted ethynyl 297.39 1.02 University of South Carolina Beaufort (USA) C18H23N3O Mercaldi, G. F., D’Antonio, E. L., Aguessi, A., Rodriguez, A. & Cordeiro, A. T. Discovery of antichagasic inhibitors by high-throughput screening with Trypanosoma cruzi glucokinase. Bioorganic Med. Chem. Lett. (2019) 1807539 1701
GKI2-GLK7-001 GKI2-GLK7-001 TcGlcK (T.cruzi glucokinase) inhibitor 2019 339.13 2.88 University of South Carolina Beaufort (USA) C13H10INO2 Mercaldi, G. F., D’Antonio, E. L., Aguessi, A., Rodriguez, A. & Cordeiro, A. T. Discovery of antichagasic inhibitors by high-throughput screening with Trypanosoma cruzi glucokinase. Bioorganic Med. Chem. Lett. (2019) 3439114 1702
GKI2-GLK8-001 GKI2-GLK8-001 TcGlcK (T.cruzi glucokinase) inhibitor 2019 Pyridine 376.39 4.17 University of South Carolina Beaufort (USA) C19H12N4O3S Mercaldi, G. F., D’Antonio, E. L., Aguessi, A., Rodriguez, A. & Cordeiro, A. T. Discovery of antichagasic inhibitors by high-throughput screening with Trypanosoma cruzi glucokinase. Bioorganic Med. Chem. Lett. (2019) 5117411 1703
GKI2-GLK9-001 GKI2-GLK9-001 TcGlcK (T.cruzi glucokinase) inhibitor 2019 Benzamide 374.45 3.91 University of South Carolina Beaufort (USA) C19H22N2O4S Mercaldi, G. F., D’Antonio, E. L., Aguessi, A., Rodriguez, A. & Cordeiro, A. T. Discovery of antichagasic inhibitors by high-throughput screening with Trypanosoma cruzi glucokinase. Bioorganic Med. Chem. Lett. (2019) 2171072 1704
GKI3-1 GKI3-1 TcGlcK (T.cruzi glucokinase) inhibitor 2021 Benzamide 283.28 0.5 University of South Carolina Beaufort (USA) C13H17NO6 Green, S. B. et al. Synthesis, biochemical, and biological evaluation of C2 linkage derivatives of amino sugars, inhibitors of glucokinase from Trypanosoma cruzi. Bioorganic Med. Chem. Lett. (2021) 21677942 1705
GKI3-10 GKI3-10 TcGlcK (T.cruzi glucokinase) inhibitor 2021 287.27 -1.13 University of South Carolina Beaufort (USA) C12H17NO7 Green, S. B. et al. Synthesis, biochemical, and biological evaluation of C2 linkage derivatives of amino sugars, inhibitors of glucokinase from Trypanosoma cruzi. Bioorganic Med. Chem. Lett. (2021) 155632152 1714
GKI3-11 GKI3-11 TcGlcK (T.cruzi glucokinase) inhibitor 2021 323.3 -0.19 University of South Carolina Beaufort (USA) C15H17NO7 Green, S. B. et al. Synthesis, biochemical, and biological evaluation of C2 linkage derivatives of amino sugars, inhibitors of glucokinase from Trypanosoma cruzi. Bioorganic Med. Chem. Lett. (2021) 155632150 1715
GKI3-12 GKI3-12 TcGlcK (T.cruzi glucokinase) inhibitor 2021 273.24 -1.87 University of South Carolina Beaufort (USA) C11H15NO7 Green, S. B. et al. Synthesis, biochemical, and biological evaluation of C2 linkage derivatives of amino sugars, inhibitors of glucokinase from Trypanosoma cruzi. Bioorganic Med. Chem. Lett. (2021) 155247289 1716
GKI3-13 GKI3-13 TcGlcK (T.cruzi glucokinase) inhibitor 2021 Benzamide 283.28 0.5 University of South Carolina Beaufort (USA) C13H17NO6 Green, S. B. et al. Synthesis, biochemical, and biological evaluation of C2 linkage derivatives of amino sugars, inhibitors of glucokinase from Trypanosoma cruzi. Bioorganic Med. Chem. Lett. (2021) 131700285 1717
GKI3-14 GKI3-14 TcGlcK (T.cruzi glucokinase) inhibitor 2021 Benzamide 362.17 -0.24 University of South Carolina Beaufort (USA) C13H16BrNO6 Green, S. B. et al. Synthesis, biochemical, and biological evaluation of C2 linkage derivatives of amino sugars, inhibitors of glucokinase from Trypanosoma cruzi. Bioorganic Med. Chem. Lett. (2021) 157635323 1718
GKI3-15 GKI3-15 TcGlcK (T.cruzi glucokinase) inhibitor 2021 Benzamide 331.75 0.89 University of South Carolina Beaufort (USA) C14H18ClNO6 Green, S. B. et al. Synthesis, biochemical, and biological evaluation of C2 linkage derivatives of amino sugars, inhibitors of glucokinase from Trypanosoma cruzi. Bioorganic Med. Chem. Lett. (2021) 155632151 1719
GKI3-16 GKI3-16 TcGlcK (T.cruzi glucokinase) inhibitor 2021 287.27 -1.13 University of South Carolina Beaufort (USA) C12H17NO7 Green, S. B. et al. Synthesis, biochemical, and biological evaluation of C2 linkage derivatives of amino sugars, inhibitors of glucokinase from Trypanosoma cruzi. Bioorganic Med. Chem. Lett. (2021) 155632152 1720
GKI3-17 GKI3-17 TcGlcK (T.cruzi glucokinase) inhibitor 2021 323.3 -0.19 University of South Carolina Beaufort (USA) C15H17NO7 Green, S. B. et al. Synthesis, biochemical, and biological evaluation of C2 linkage derivatives of amino sugars, inhibitors of glucokinase from Trypanosoma cruzi. Bioorganic Med. Chem. Lett. (2021) 155632150 1721
GKI3-18 GKI3-18 TcGlcK (T.cruzi glucokinase) inhibitor 2021 273.24 -1.87 University of South Carolina Beaufort (USA) C11H15NO7 Green, S. B. et al. Synthesis, biochemical, and biological evaluation of C2 linkage derivatives of amino sugars, inhibitors of glucokinase from Trypanosoma cruzi. Bioorganic Med. Chem. Lett. (2021) 155247289 1722
GKI3-2 GKI3-2 TcGlcK (T.cruzi glucokinase) inhibitor 2021 Benzamide 362.17 -0.24 University of South Carolina Beaufort (USA) C13H16BrNO6 Green, S. B. et al. Synthesis, biochemical, and biological evaluation of C2 linkage derivatives of amino sugars, inhibitors of glucokinase from Trypanosoma cruzi. Bioorganic Med. Chem. Lett. (2021) 134147054 1706
GKI3-3 GKI3-3 TcGlcK (T.cruzi glucokinase) inhibitor 2021 Benzamide 331.75 0.89 University of South Carolina Beaufort (USA) C14H18ClNO6 Green, S. B. et al. Synthesis, biochemical, and biological evaluation of C2 linkage derivatives of amino sugars, inhibitors of glucokinase from Trypanosoma cruzi. Bioorganic Med. Chem. Lett. (2021) 155632151 1707
GKI3-4 GKI3-4 TcGlcK (T.cruzi glucokinase) inhibitor 2021 287.27 -1.13 University of South Carolina Beaufort (USA) C12H17NO7 Green, S. B. et al. Synthesis, biochemical, and biological evaluation of C2 linkage derivatives of amino sugars, inhibitors of glucokinase from Trypanosoma cruzi. Bioorganic Med. Chem. Lett. (2021) 155632152 1708
GKI3-5 GKI3-5 TcGlcK (T.cruzi glucokinase) inhibitor 2021 323.3 -0.19 University of South Carolina Beaufort (USA) C15H17NO7 Green, S. B. et al. Synthesis, biochemical, and biological evaluation of C2 linkage derivatives of amino sugars, inhibitors of glucokinase from Trypanosoma cruzi. Bioorganic Med. Chem. Lett. (2021) 155632150 1709
GKI3-6 GKI3-6 TcGlcK (T.cruzi glucokinase) inhibitor 2021 273.24 -1.87 University of South Carolina Beaufort (USA) C11H15NO7 Green, S. B. et al. Synthesis, biochemical, and biological evaluation of C2 linkage derivatives of amino sugars, inhibitors of glucokinase from Trypanosoma cruzi. Bioorganic Med. Chem. Lett. (2021) 155247289 1710
GKI3-7 GKI3-7 TcGlcK (T.cruzi glucokinase) inhibitor 2021 Benzamide 283.28 0.5 University of South Carolina Beaufort (USA) C13H17NO6 Green, S. B. et al. Synthesis, biochemical, and biological evaluation of C2 linkage derivatives of amino sugars, inhibitors of glucokinase from Trypanosoma cruzi. Bioorganic Med. Chem. Lett. (2021) 27506903 1711
GKI3-8 GKI3-8 TcGlcK (T.cruzi glucokinase) inhibitor 2021 Benzamide 362.17 -0.24 University of South Carolina Beaufort (USA) C13H16BrNO6 Green, S. B. et al. Synthesis, biochemical, and biological evaluation of C2 linkage derivatives of amino sugars, inhibitors of glucokinase from Trypanosoma cruzi. Bioorganic Med. Chem. Lett. (2021) 157635323 1712
GKI3-9 GKI3-9 TcGlcK (T.cruzi glucokinase) inhibitor 2021 Benzamide 331.75 0.89 University of South Carolina Beaufort (USA) C14H18ClNO6 Green, S. B. et al. Synthesis, biochemical, and biological evaluation of C2 linkage derivatives of amino sugars, inhibitors of glucokinase from Trypanosoma cruzi. Bioorganic Med. Chem. Lett. (2021) 155632151 1713
GKI-BENZ-GlcN GKI-BENZ-GlcN TcGlcK (T.cruzi glucokinase) inhibitor 2015 Benzamide 283.28 0.5 University of South Carolina Beaufort (USA) C13H17NO6 D’Antonio, E. L. et al. Structure-based approach to the identification of a novel group of selective glucosamine analogue inhibitors of Trypanosoma cruzi glucokinase. Mol. Biochem. Parasitol. (2015) 21677942 1676
GKI-CBZ-GlcN GKI-CBZ-GlcN TcGlcK (T.cruzi glucokinase) inhibitor 2015 313.3 -0.69 University of South Carolina Beaufort (USA) C14H19NO7 D’Antonio, E. L. et al. Structure-based approach to the identification of a novel group of selective glucosamine analogue inhibitors of Trypanosoma cruzi glucokinase. Mol. Biochem. Parasitol. (2015) 13474484 1677
GKI-DBT-GlcN GKI-DBT-GlcN TcGlcK (T.cruzi glucokinase) inhibitor 2015 Sulfoxide/Sulfone derivatives 401.39 -1.31 University of South Carolina Beaufort (USA) C16H19NO9S D’Antonio, E. L. et al. Structure-based approach to the identification of a novel group of selective glucosamine analogue inhibitors of Trypanosoma cruzi glucokinase. Mol. Biochem. Parasitol. (2015) 137348290 1679
GKI-HPOP-GLcN GKI-HPOP-GlcN TcGlcK (T.cruzi glucokinase) inhibitor 2015 327.33 -1.06 University of South Carolina Beaufort (USA) C15H21NO7 D’Antonio, E. L. et al. Structure-based approach to the identification of a novel group of selective glucosamine analogue inhibitors of Trypanosoma cruzi glucokinase. Mol. Biochem. Parasitol. (2015) 91801173 1678
GKRP1-1 GKRP1-1 GK-GKRP disruptor 2014 Sulfoxide/Sulfone derivatives 474.44 3.87 Amgen Inc. (USA) C17H16F6N2O3S2 Ashton, K. S. et al. Small molecule disruptors of the Glucokinase-Glucokinase regulatory protein interaction: 1. Discovery of a novel tool compound for in vivo proof-of-concept. J. Med. Chem. (2014) 56832521 1478
GKRP1-10 GKRP1-10 GK-GKRP disruptor 2014 Sulfoxide/Sulfone derivatives 580.56 5.54 Amgen Inc. (USA) C24H22F6N2O4S2 Ashton, K. S. et al. Small molecule disruptors of the Glucokinase-Glucokinase regulatory protein interaction: 1. Discovery of a novel tool compound for in vivo proof-of-concept. J. Med. Chem. (2014) 87058744 1487
GKRP1-11 GKRP1-11 GK-GKRP disruptor 2014 Sulfoxide/Sulfone derivatives 580.56 5.54 Amgen Inc. (USA) C24H22F6N2O4S2 Ashton, K. S. et al. Small molecule disruptors of the Glucokinase-Glucokinase regulatory protein interaction: 1. Discovery of a novel tool compound for in vivo proof-of-concept. J. Med. Chem. (2014) 87058490 1488
GKRP1-12 GKRP1-12 GK-GKRP disruptor 2014 Sulfoxide/Sulfone derivatives 580.56 5.54 Amgen Inc. (USA) C24H22F6N2O4S2 Ashton, K. S. et al. Small molecule disruptors of the Glucokinase-Glucokinase regulatory protein interaction: 1. Discovery of a novel tool compound for in vivo proof-of-concept. J. Med. Chem. (2014) 87058762 1489
GKRP1-13 GKRP1-13 GK-GKRP disruptor 2014 Sulfoxide/Sulfone derivatives 578.59 6.26 Amgen Inc. (USA) C25H24F6N2O3S2 Ashton, K. S. et al. Small molecule disruptors of the Glucokinase-Glucokinase regulatory protein interaction: 1. Discovery of a novel tool compound for in vivo proof-of-concept. J. Med. Chem. (2014) 76314688 1490
GKRP1-14 GKRP1-14 GK-GKRP disruptor 2014 Sulfoxide/Sulfone derivatives 578.59 6.26 Amgen Inc. (USA) C25H24F6N2O3S2 Ashton, K. S. et al. Small molecule disruptors of the Glucokinase-Glucokinase regulatory protein interaction: 1. Discovery of a novel tool compound for in vivo proof-of-concept. J. Med. Chem. (2014) 86670317 1491
GKRP1-15 GKRP1-15 GK-GKRP disruptor 2014 Sulfoxide/Sulfone derivatives 578.59 6.26 Amgen Inc. (USA) C25H24F6N2O3S2 Ashton, K. S. et al. Small molecule disruptors of the Glucokinase-Glucokinase regulatory protein interaction: 1. Discovery of a novel tool compound for in vivo proof-of-concept. J. Med. Chem. (2014) 86670323 1492
GKRP1-16 GKRP1-16 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives 565.55 4.83 Amgen Inc. (USA) C23H21F6N3O3S2 Ashton, K. S. et al. Small molecule disruptors of the Glucokinase-Glucokinase regulatory protein interaction: 1. Discovery of a novel tool compound for in vivo proof-of-concept. J. Med. Chem. (2014) 76318259 1493
GKRP1-17 GKRP1-17 GK-GKRP disruptor 2014 Sulfoxide/Sulfone derivatives 570.61 7.04 Amgen Inc. (USA) C24H28F6N2O3S2 Ashton, K. S. et al. Small molecule disruptors of the Glucokinase-Glucokinase regulatory protein interaction: 1. Discovery of a novel tool compound for in vivo proof-of-concept. J. Med. Chem. (2014) 76336428 1494
GKRP1-18 GKRP1-18 GK-GKRP disruptor 2014 Sulfoxide/Sulfone derivatives 572.58 4.89 Amgen Inc. (USA) C23H26F6N2O4S2 Ashton, K. S. et al. Small molecule disruptors of the Glucokinase-Glucokinase regulatory protein interaction: 1. Discovery of a novel tool compound for in vivo proof-of-concept. J. Med. Chem. (2014) 86670315 1495
GKRP1-19 GKRP1-19 GK-GKRP disruptor 2014 Sulfoxide/Sulfone derivatives 573.57 3.6 Amgen Inc. (USA) C22H25F6N3O4S2 Ashton, K. S. et al. Small molecule disruptors of the Glucokinase-Glucokinase regulatory protein interaction: 1. Discovery of a novel tool compound for in vivo proof-of-concept. J. Med. Chem. (2014) 56932571 1496
GKRP1-2 GKRP1-2 GK-GKRP disruptor 2014 Sulfoxide/Sulfone derivatives 488.47 4.31 Amgen Inc. (USA) C18H18F6N2O3S2 Ashton, K. S. et al. Small molecule disruptors of the Glucokinase-Glucokinase regulatory protein interaction: 1. Discovery of a novel tool compound for in vivo proof-of-concept. J. Med. Chem. (2014) 76332807 1479
GKRP1-20 GKRP1-20 GK-GKRP disruptor 2014 Sulfoxide/Sulfone derivatives 587.6 4.04 Amgen Inc. (USA) C23H27F6N3O4S2 Ashton, K. S. et al. Small molecule disruptors of the Glucokinase-Glucokinase regulatory protein interaction: 1. Discovery of a novel tool compound for in vivo proof-of-concept. J. Med. Chem. (2014) 56932571 1497
GKRP1-23 GKRP1-23 GK-GKRP disruptor 2014 Sulfoxide/Sulfone derivatives 518.61 4.15 Amgen Inc. (USA) C23H29F3N2O4S2 Ashton, K. S. et al. Small molecule disruptors of the Glucokinase-Glucokinase regulatory protein interaction: 1. Discovery of a novel tool compound for in vivo proof-of-concept. J. Med. Chem. (2014) 70655359 1498
GKRP1-24 GKRP1-24 GK-GKRP disruptor 2014 Sulfoxide/Sulfone derivatives 518.61 4.15 Amgen Inc. (USA) C23H29F3N2O4S2 Ashton, K. S. et al. Small molecule disruptors of the Glucokinase-Glucokinase regulatory protein interaction: 1. Discovery of a novel tool compound for in vivo proof-of-concept. J. Med. Chem. (2014) 70655359 1499
GKRP1-26 GKRP1-26 GK-GKRP disruptor 2014 Sulfoxide/Sulfone derivatives 533.63 3.29 Amgen Inc. (USA) C23H30F3N3O4S2 Ashton, K. S. et al. Small molecule disruptors of the Glucokinase-Glucokinase regulatory protein interaction: 1. Discovery of a novel tool compound for in vivo proof-of-concept. J. Med. Chem. (2014) 66582747 1500
GKRP1-3 GKRP1-3 GK-GKRP disruptor 2014 Sulfoxide/Sulfone derivatives 488.47 4.31 Amgen Inc. (USA) C18H18F6N2O3S2 Ashton, K. S. et al. Small molecule disruptors of the Glucokinase-Glucokinase regulatory protein interaction: 1. Discovery of a novel tool compound for in vivo proof-of-concept. J. Med. Chem. (2014) 76318260 1480
GKRP1-4 GKRP1-4 GK-GKRP disruptor 2014 Sulfoxide/Sulfone derivatives 488.47 4.31 Amgen Inc. (USA) C18H18F6N2O3S2 Ashton, K. S. et al. Small molecule disruptors of the Glucokinase-Glucokinase regulatory protein interaction: 1. Discovery of a novel tool compound for in vivo proof-of-concept. J. Med. Chem. (2014) 76311064 1481
GKRP1-5 GKRP1-5 GK-GKRP disruptor 2014 Sulfoxide/Sulfone derivatives 488.47 4.31 Amgen Inc. (USA) C18H18F6N2O3S2 Ashton, K. S. et al. Small molecule disruptors of the Glucokinase-Glucokinase regulatory protein interaction: 1. Discovery of a novel tool compound for in vivo proof-of-concept. J. Med. Chem. (2014) 76336429 1482
GKRP1-6 GKRP1-6 GK-GKRP disruptor 2014 Sulfoxide/Sulfone derivatives 502.49 4.83 Amgen Inc. (USA) C19H20F6N2O3S2 Ashton, K. S. et al. Small molecule disruptors of the Glucokinase-Glucokinase regulatory protein interaction: 1. Discovery of a novel tool compound for in vivo proof-of-concept. J. Med. Chem. (2014) 76314690 1483
GKRP1-7 GKRP1-7 GK-GKRP disruptor 2014 Sulfoxide/Sulfone derivatives 516.52 5.27 Amgen Inc. (USA) C20H22F6N2O3S2 Ashton, K. S. et al. Small molecule disruptors of the Glucokinase-Glucokinase regulatory protein interaction: 1. Discovery of a novel tool compound for in vivo proof-of-concept. J. Med. Chem. (2014) 76311065 1484
GKRP1-8 GKRP1-8 GK-GKRP disruptor 2014 Sulfoxide/Sulfone derivatives 550.54 5.4 Amgen Inc. (USA) C23H20F6N2O3S2 Ashton, K. S. et al. Small molecule disruptors of the Glucokinase-Glucokinase regulatory protein interaction: 1. Discovery of a novel tool compound for in vivo proof-of-concept. J. Med. Chem. (2014) 76314691 1485
GKRP1-9 GKRP1-9 GK-GKRP disruptor 2014 Sulfoxide/Sulfone derivatives 564.56 5.9 Amgen Inc. (USA) C24H22F6N2O3S2 Ashton, K. S. et al. Small molecule disruptors of the Glucokinase-Glucokinase regulatory protein interaction: 1. Discovery of a novel tool compound for in vivo proof-of-concept. J. Med. Chem. (2014) 56932319 1486
GKRP2-10 GKRP2-10 GK-GKRP disruptor 2014 Sulfoxide/Sulfone derivatives 561.64 2.5 Amgen Inc. (USA) C24H30F3N3O5S2 St. Jean, D. J. et al. Small molecule disruptors of the Glucokinase-Glucokinase regulatory protein interaction: 2. Leveraging structure-based drug design to identify analogues with improved pharmacokinetic profiles. J. Med. Chem. (2014) 70655743 1507
GKRP2-11 GKRP2-11 GK-GKRP disruptor 2014 Sulfoxide/Sulfone derivatives 561.64 2.5 Amgen Inc. (USA) C24H30F3N3O5S2 St. Jean, D. J. et al. Small molecule disruptors of the Glucokinase-Glucokinase regulatory protein interaction: 2. Leveraging structure-based drug design to identify analogues with improved pharmacokinetic profiles. J. Med. Chem. (2014) 70655743 1508
GKRP2-12 GKRP2-12 GK-GKRP disruptor 2014 Sulfoxide/Sulfone derivatives 561.64 2.5 Amgen Inc. (USA) C24H30F3N3O5S2 St. Jean, D. J. et al. Small molecule disruptors of the Glucokinase-Glucokinase regulatory protein interaction: 2. Leveraging structure-based drug design to identify analogues with improved pharmacokinetic profiles. J. Med. Chem. (2014) 70655077 1509
GKRP2-13 GKRP2-13 GK-GKRP disruptor 2014 Sulfoxide/Sulfone derivatives 561.64 2.5 Amgen Inc. (USA) C24H30F3N3O5S2 St. Jean, D. J. et al. Small molecule disruptors of the Glucokinase-Glucokinase regulatory protein interaction: 2. Leveraging structure-based drug design to identify analogues with improved pharmacokinetic profiles. J. Med. Chem. (2014) 70655491 1510
GKRP2-14 GKRP2-14 GK-GKRP disruptor 2014 Sulfoxide/Sulfone derivatives 561.64 2.5 Amgen Inc. (USA) C24H30F3N3O5S2 St. Jean, D. J. et al. Small molecule disruptors of the Glucokinase-Glucokinase regulatory protein interaction: 2. Leveraging structure-based drug design to identify analogues with improved pharmacokinetic profiles. J. Med. Chem. (2014) 70655526 1511
GKRP2-16 GKRP2-16 GK-GKRP disruptor 2014 Sulfoxide/Sulfone derivatives 468.41 3.86 Amgen Inc. (USA) C19H18F6N2O3S St. Jean, D. J. et al. Small molecule disruptors of the Glucokinase-Glucokinase regulatory protein interaction: 2. Leveraging structure-based drug design to identify analogues with improved pharmacokinetic profiles. J. Med. Chem. (2014) 76310480 1512
GKRP2-17 GKRP2-17 GK-GKRP disruptor 2014 Sulfoxide/Sulfone derivatives 489.46 3.53 Amgen Inc. (USA) C17H17F6N3O3S2 St. Jean, D. J. et al. Small molecule disruptors of the Glucokinase-Glucokinase regulatory protein interaction: 2. Leveraging structure-based drug design to identify analogues with improved pharmacokinetic profiles. J. Med. Chem. (2014) 76317707 1513
GKRP2-18 GKRP2-18 GK-GKRP disruptor 2014 Sulfoxide/Sulfone derivatives 489.46 3.19 Amgen Inc. (USA) C17H17F6N3O3S2 St. Jean, D. J. et al. Small molecule disruptors of the Glucokinase-Glucokinase regulatory protein interaction: 2. Leveraging structure-based drug design to identify analogues with improved pharmacokinetic profiles. J. Med. Chem. (2014) 76314133 1514
GKRP2-19 GKRP2-19 GK-GKRP disruptor 2014 Sulfoxide/Sulfone derivatives 483.43 3.73 Amgen Inc. (USA) C19H19F6N3O3S St. Jean, D. J. et al. Small molecule disruptors of the Glucokinase-Glucokinase regulatory protein interaction: 2. Leveraging structure-based drug design to identify analogues with improved pharmacokinetic profiles. J. Med. Chem. (2014) 76325010 1515
GKRP2-20 GKRP2-20 GK-GKRP disruptor 2014 Sulfoxide/Sulfone derivatives 483.43 3.18 Amgen Inc. (USA) C19H19F6N3O3S St. Jean, D. J. et al. Small molecule disruptors of the Glucokinase-Glucokinase regulatory protein interaction: 2. Leveraging structure-based drug design to identify analogues with improved pharmacokinetic profiles. J. Med. Chem. (2014) 76321415 1516
GKRP2-21 GKRP2-21 GK-GKRP disruptor 2014 Sulfoxide/Sulfone derivatives 483.43 3.18 Amgen Inc. (USA) C19H19F6N3O3S St. Jean, D. J. et al. Small molecule disruptors of the Glucokinase-Glucokinase regulatory protein interaction: 2. Leveraging structure-based drug design to identify analogues with improved pharmacokinetic profiles. J. Med. Chem. (2014) 76335899 1517
GKRP2-22 GKRP2-22 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives 484.42 2.44 Amgen Inc. (USA) C18H18F6N4O3S St. Jean, D. J. et al. Small molecule disruptors of the Glucokinase-Glucokinase regulatory protein interaction: 2. Leveraging structure-based drug design to identify analogues with improved pharmacokinetic profiles. J. Med. Chem. (2014) 76332259 1518
GKRP2-23 GKRP2-23 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives 484.42 2.44 Amgen Inc. (USA) C18H18F6N4O3S St. Jean, D. J. et al. Small molecule disruptors of the Glucokinase-Glucokinase regulatory protein interaction: 2. Leveraging structure-based drug design to identify analogues with improved pharmacokinetic profiles. J. Med. Chem. (2014) 73659150 1519
GKRP2-24 GKRP2-24 GK-GKRP disruptor 2014 Pyrimidine,Sulfoxide/Sulfone derivatives 485.4 1.79 Amgen Inc. (USA) C17H17F6N5O3S St. Jean, D. J. et al. Small molecule disruptors of the Glucokinase-Glucokinase regulatory protein interaction: 2. Leveraging structure-based drug design to identify analogues with improved pharmacokinetic profiles. J. Med. Chem. (2014) 76328584 1520
GKRP2-25 GKRP2-25 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 522.46 3.1 Amgen Inc. (USA) C21H20F6N4O3S St. Jean, D. J. et al. Small molecule disruptors of the Glucokinase-Glucokinase regulatory protein interaction: 2. Leveraging structure-based drug design to identify analogues with improved pharmacokinetic profiles. J. Med. Chem. (2014) 76321432 1521
GKRP2-26 GKRP2-26 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 522.46 3.1 Amgen Inc. (USA) C21H20F6N4O3S St. Jean, D. J. et al. Small molecule disruptors of the Glucokinase-Glucokinase regulatory protein interaction: 2. Leveraging structure-based drug design to identify analogues with improved pharmacokinetic profiles. J. Med. Chem. (2014) 76321432 1522
GKRP2-28 GKRP2-28 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 468.49 2.36 Amgen Inc. (USA) C21H23F3N4O3S St. Jean, D. J. et al. Small molecule disruptors of the Glucokinase-Glucokinase regulatory protein interaction: 2. Leveraging structure-based drug design to identify analogues with improved pharmacokinetic profiles. J. Med. Chem. (2014) 66582550 1523
GKRP2-29 GKRP2-29 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 468.49 2.36 Amgen Inc. (USA) C21H23F3N4O3S St. Jean, D. J. et al. Small molecule disruptors of the Glucokinase-Glucokinase regulatory protein interaction: 2. Leveraging structure-based drug design to identify analogues with improved pharmacokinetic profiles. J. Med. Chem. (2014) 66582448 1524
GKRP2-30 GKRP2-30 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 536.49 3.54 Amgen Inc. (USA) C22H22F6N4O3S St. Jean, D. J. et al. Small molecule disruptors of the Glucokinase-Glucokinase regulatory protein interaction: 2. Leveraging structure-based drug design to identify analogues with improved pharmacokinetic profiles. J. Med. Chem. (2014) 89761117 1525
GKRP2-31 GKRP2-31 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 548.5 3.65 Amgen Inc. (USA) C23H22F6N4O3S St. Jean, D. J. et al. Small molecule disruptors of the Glucokinase-Glucokinase regulatory protein interaction: 2. Leveraging structure-based drug design to identify analogues with improved pharmacokinetic profiles. J. Med. Chem. (2014) 76328603 1526
GKRP2-32 GKRP2-32 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 564.54 4.41 Amgen Inc. (USA) C24H26F6N4O3S St. Jean, D. J. et al. Small molecule disruptors of the Glucokinase-Glucokinase regulatory protein interaction: 2. Leveraging structure-based drug design to identify analogues with improved pharmacokinetic profiles. J. Med. Chem. (2014) 89762043 1527
GKRP2-4 GKRP2-4 GK-GKRP disruptor 2014 Sulfoxide/Sulfone derivatives 553.61 4.39 Amgen Inc. (USA) C23H28F5N3O3S2 St. Jean, D. J. et al. Small molecule disruptors of the Glucokinase-Glucokinase regulatory protein interaction: 2. Leveraging structure-based drug design to identify analogues with improved pharmacokinetic profiles. J. Med. Chem. (2014) 66582461 1501
GKRP2-5 GKRP2-5 GK-GKRP disruptor 2014 Sulfoxide/Sulfone derivatives 567.67 2.38 Amgen Inc. (USA) C22H28F3N3O5S3 St. Jean, D. J. et al. Small molecule disruptors of the Glucokinase-Glucokinase regulatory protein interaction: 2. Leveraging structure-based drug design to identify analogues with improved pharmacokinetic profiles. J. Med. Chem. (2014) 56932374 1502
GKRP2-6 GKRP2-6 GK-GKRP disruptor 2014 Sulfoxide/Sulfone derivatives 581.69 2.81 Amgen Inc. (USA) C23H30F3N3O5S3 St. Jean, D. J. et al. Small molecule disruptors of the Glucokinase-Glucokinase regulatory protein interaction: 2. Leveraging structure-based drug design to identify analogues with improved pharmacokinetic profiles. J. Med. Chem. (2014) 66586173 1503
GKRP2-7 GKRP2-7 GK-GKRP disruptor 2014 Sulfoxide/Sulfone derivatives 531.61 2.75 Amgen Inc. (USA) C23H28F3N3O4S2 St. Jean, D. J. et al. Small molecule disruptors of the Glucokinase-Glucokinase regulatory protein interaction: 2. Leveraging structure-based drug design to identify analogues with improved pharmacokinetic profiles. J. Med. Chem. (2014) 66582839 1504
GKRP2-8 GKRP2-8 GK-GKRP disruptor 2014 Sulfoxide/Sulfone derivatives 545.64 3.48 Amgen Inc. (USA) C24H30F3N3O4S2 St. Jean, D. J. et al. Small molecule disruptors of the Glucokinase-Glucokinase regulatory protein interaction: 2. Leveraging structure-based drug design to identify analogues with improved pharmacokinetic profiles. J. Med. Chem. (2014) 76317706 1505
GKRP2-9 GKRP2-9 GK-GKRP disruptor 2014 Sulfoxide/Sulfone derivatives 561.64 2.5 Amgen Inc. (USA) C24H30F3N3O5S2 St. Jean, D. J. et al. Small molecule disruptors of the Glucokinase-Glucokinase regulatory protein interaction: 2. Leveraging structure-based drug design to identify analogues with improved pharmacokinetic profiles. J. Med. Chem. (2014) 70655587 1506
GKRP3-10 GKRP3-10 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 356.44 1.91 Amgen Inc. (USA) C18H20N4O2S Nishimura, N. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N′-arylpiperazine series. J. Med. Chem. (2014) 90655466 1528
GKRP3-11 GKRP3-11 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 452.49 3.61 Amgen Inc. (USA) C21H23F3N4O2S Nishimura, N. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N′-arylpiperazine series. J. Med. Chem. (2014) 90045463 1529
GKRP3-12 GKRP3-12 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 398.48 1.59 Amgen Inc. (USA) C20H22N4O3S Nishimura, N. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N′-arylpiperazine series. J. Med. Chem. (2014) 73332125 1530
GKRP3-13 GKRP3-13 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 413.49 1.18 Amgen Inc. (USA) C20H23N5O3S Nishimura, N. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N′-arylpiperazine series. J. Med. Chem. (2014) 90655465 1531
GKRP3-14 GKRP3-14 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 418.53 1.03 Amgen Inc. (USA) C19H22N4O3S2 Nishimura, N. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N′-arylpiperazine series. J. Med. Chem. (2014) 90655467 1532
GKRP3-15 GKRP3-15 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 449.55 0.87 Amgen Inc. (USA) C19H23N5O4S2 Nishimura, N. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N′-arylpiperazine series. J. Med. Chem. (2014) 73332274 1533
GKRP3-16 GKRP3-16 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 475.58 1.43 Amgen Inc. (USA) C21H25N5O4S2 Nishimura, N. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N′-arylpiperazine series. J. Med. Chem. (2014) 73332120 1534
GKRP3-17 GKRP3-17 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 489.61 1.62 Amgen Inc. (USA) C22H27N5O4S2 Nishimura, N. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N′-arylpiperazine series. J. Med. Chem. (2014) 73332123 1535
GKRP3-18 GKRP3-18 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 511.62 2.43 Amgen Inc. (USA) C24H25N5O4S2 Nishimura, N. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N′-arylpiperazine series. J. Med. Chem. (2014) 90655468 1536
GKRP3-19 GKRP3-19 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 501.55 3.1 Amgen Inc. (USA) C20H22F3N5O3S2 Nishimura, N. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N′-arylpiperazine series. J. Med. Chem. (2014) 90065380 1537
GKRP3-20 GKRP3-20 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 434.53 1.14 Amgen Inc. (USA) C19H22N4O4S2 Nishimura, N. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N′-arylpiperazine series. J. Med. Chem. (2014) 90655469 1538
GKRP3-21 GKRP3-21 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 477.6 1.67 Amgen Inc. (USA) C21H27N5O4S2 Nishimura, N. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N′-arylpiperazine series. J. Med. Chem. (2014) 90043783 1539
GKRP3-22 GKRP3-22 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 487.52 3.64 Amgen Inc. (USA) C19H20F3N5O3S2 Nishimura, N. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N′-arylpiperazine series. J. Med. Chem. (2014) 90065460 1540
GKRP3-23 GKRP3-23 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 487.52 3.64 Amgen Inc. (USA) C19H20F3N5O3S2 Nishimura, N. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N′-arylpiperazine series. J. Med. Chem. (2014) 90065461 1541
GKRP3-24 GKRP3-24 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 487.52 3.64 Amgen Inc. (USA) C19H20F3N5O3S2 Nishimura, N. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N′-arylpiperazine series. J. Med. Chem. (2014) 90065460 1542
GKRP3-25 GKRP3-25 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 469.48 1.32 Amgen Inc. (USA) C20H22F3N5O3S Nishimura, N. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N′-arylpiperazine series. J. Med. Chem. (2014) 90655470 1543
GKRP3-26 GKRP3-26 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 523.45 2.37 Amgen Inc. (USA) C20H19F6N5O3S Nishimura, N. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N′-arylpiperazine series. J. Med. Chem. (2014) 71715584 1544
GKRP3-27 GKRP3-27 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 450.54 0.14 Amgen Inc. (USA) C18H22N6O4S2 Nishimura, N. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N′-arylpiperazine series. J. Med. Chem. (2014) 73332275 1545
GKRP3-28 GKRP3-28 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 469.48 1.62 Amgen Inc. (USA) C20H22F3N5O3S Nishimura, N. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N′-arylpiperazine series. J. Med. Chem. (2014) 89760985 1546
GKRP3-29 GKRP3-29 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 469.48 1.62 Amgen Inc. (USA) C20H22F3N5O3S Nishimura, N. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N′-arylpiperazine series. J. Med. Chem. (2014) 89760985 1547
GKRP3-30 GKRP3-30 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 469.48 1.62 Amgen Inc. (USA) C20H22F3N5O3S Nishimura, N. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N′-arylpiperazine series. J. Med. Chem. (2014) 89761168 1548
GKRP3-47 GKRP3-47 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 459.58 2.98 Amgen Inc. (USA) C21H25N5O3S2 Nishimura, N. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N′-arylpiperazine series. J. Med. Chem. (2014) 73332122 1549
GKRP3-48 GKRP3-48 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 433.55 2.43 Amgen Inc. (USA) C19H23N5O3S2 Nishimura, N. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N′-arylpiperazine series. J. Med. Chem. (2014) 90065524 1550
GKRP3-49 GKRP3-49 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 435.52 0.47 Amgen Inc. (USA) C18H21N5O4S2 Nishimura, N. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N′-arylpiperazine series. J. Med. Chem. (2014) 73331966 1551
GKRP3-51 GKRP3-51 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 484.49 1.31 Amgen Inc. (USA) C21H23F3N4O4S Nishimura, N. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N′-arylpiperazine series. J. Med. Chem. (2014) 76871909 1552
GKRP3-52 GKRP3-52 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 484.49 1.31 Amgen Inc. (USA) C21H23F3N4O4S Nishimura, N. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N′-arylpiperazine series. J. Med. Chem. (2014) 89761004 1553
GKRP3-53 GKRP3-53 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 485.48 0.57 Amgen Inc. (USA) C20H22F3N5O4S Nishimura, N. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N′-arylpiperazine series. J. Med. Chem. (2014) 89762388 1554
GKRP3-54 GKRP3-54 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 485.48 0.57 Amgen Inc. (USA) C20H22F3N5O4S Nishimura, N. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N′-arylpiperazine series. J. Med. Chem. (2014) 89761475 1555
GKRP3-55 GKRP3-55 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 485.48 0.57 Amgen Inc. (USA) C20H22F3N5O4S Nishimura, N. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N′-arylpiperazine series. J. Med. Chem. (2014) 89762388 1556
GKRP3-62 GKRP3-62 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 493.5 1.68 Amgen Inc. (USA) C22H22F3N5O3S Nishimura, N. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N′-arylpiperazine series. J. Med. Chem. (2014) 90044911 1557
GKRP3-63 GKRP3-63 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 498.52 1.84 Amgen Inc. (USA) C22H25F3N4O4S Nishimura, N. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N′-arylpiperazine series. J. Med. Chem. (2014) 90043802 1558
GKRP3-64 GKRP3-64 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 492.51 2.57 Amgen Inc. (USA) C23H23F3N4O3S Nishimura, N. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N′-arylpiperazine series. J. Med. Chem. (2014) 90044769 1559
GKRP3-65 GKRP3-65 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 506.54 3.08 Amgen Inc. (USA) C24H25F3N4O3S Nishimura, N. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N′-arylpiperazine series. J. Med. Chem. (2014) 78350451 1560
GKRP3-67 GKRP3-67 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 483.51 1.05 Amgen Inc. (USA) C21H24F3N5O3S Nishimura, N. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N′-arylpiperazine series. J. Med. Chem. (2014) 90045230 1561
GKRP3-68 GKRP3-68 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 483.51 1.05 Amgen Inc. (USA) C21H24F3N5O3S Nishimura, N. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N′-arylpiperazine series. J. Med. Chem. (2014) 90044906 1562
GKRP3-74 GKRP3-74 GK-GKRP disruptor 2014 Thiazole/Thiadiazole,Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 529.48 2.5 Amgen Inc. (USA) C18H17F6N5O3S2 Nishimura, N. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N′-arylpiperazine series. J. Med. Chem. (2014) 90655471 1563
GKRP3-80 GKRP3-80 GK-GKRP disruptor 2014 Thiazole/Thiadiazole,Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 475.51 1.76 Amgen Inc. (USA) C18H20F3N5O3S2 Nishimura, N. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N′-arylpiperazine series. J. Med. Chem. (2014) 90655472 1564
GKRP3-88 GKRP3-88 GK-GKRP disruptor 2014 Pyridine,Pyrimidine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 524.44 1.72 Amgen Inc. (USA) C19H18F6N6O3S Nishimura, N. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N′-arylpiperazine series. J. Med. Chem. (2014) 87058555 1565
GKRP4-23 GKRP4-23 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives 519.85 2.33 Amgen Inc. (USA) C17H16ClF6N5O3S Hong, F. T. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket. J. Med. Chem. (2014) 118709613 1567
GKRP4-24 GKRP4-24 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives 564.3 2.4 Amgen Inc. (USA) C17H16BrF6N5O3S Hong, F. T. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket. J. Med. Chem. (2014) 118709614 1568
GKRP4-25 GKRP4-25 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives 515.43 1.68 Amgen Inc. (USA) C18H19F6N5O4S Hong, F. T. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket. J. Med. Chem. (2014) 118709615 1569
GKRP4-26 GKRP4-26 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives 485.4 1.71 Amgen Inc. (USA) C17H17F6N5O3S Hong, F. T. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket. J. Med. Chem. (2014) 118709612 1570
GKRP4-27 GKRP4-27 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives 525.47 2.62 Amgen Inc. (USA) C20H21F6N5O3S Hong, F. T. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket. J. Med. Chem. (2014) 118709616 1571
GKRP4-28 GKRP4-28 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 549.49 3.01 Amgen Inc. (USA) C22H21F6N5O3S Hong, F. T. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket. J. Med. Chem. (2014) 118709617 1572
GKRP4-29 GKRP4-29 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 539.45 1.21 Amgen Inc. (USA) C20H19F6N5O4S Hong, F. T. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket. J. Med. Chem. (2014) 118709618 1573
GKRP4-3 GKRP4-3 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 561.5 3.13 Amgen Inc. (USA) C23H21F6N5O3S Hong, F. T. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket. J. Med. Chem. (2014) 1566
GKRP4-30 GKRP4-30 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 553.48 1.75 Amgen Inc. (USA) C21H21F6N5O4S Hong, F. T. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket. J. Med. Chem. (2014) 118709619 1574
GKRP4-31 GKRP4-31 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 567.5 1.81 Amgen Inc. (USA) C22H23F6N5O4S Hong, F. T. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket. J. Med. Chem. (2014) 118709620 1575
GKRP4-32 GKRP4-32 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 553.48 1.68 Amgen Inc. (USA) C21H21F6N5O4S Hong, F. T. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket. J. Med. Chem. (2014) 118709621 1576
GKRP4-33 GKRP4-33 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 551.47 1.66 Amgen Inc. (USA) C20H19F6N7O3S Hong, F. T. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket. J. Med. Chem. (2014) 118709622 1577
GKRP4-34 GKRP4-34 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives 565.49 1.64 Amgen Inc. (USA) C21H21F6N7O3S Hong, F. T. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket. J. Med. Chem. (2014) 118709623 1578
GKRP4-35 GKRP4-35 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives 579.52 1.94 Amgen Inc. (USA) C22H23F6N7O3S Hong, F. T. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket. J. Med. Chem. (2014) 118709624 1579
GKRP4-36 GKRP4-36 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives 593.55 2.35 Amgen Inc. (USA) C23H25F6N7O3S Hong, F. T. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket. J. Med. Chem. (2014) 118709625 1580
GKRP4-37 GKRP4-37 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives 607.57 2.53 Amgen Inc. (USA) C24H27F6N7O3S Hong, F. T. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket. J. Med. Chem. (2014) 118709626 1581
GKRP4-38 GKRP4-38 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives 579.52 2.04 Amgen Inc. (USA) C22H23F6N7O3S Hong, F. T. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket. J. Med. Chem. (2014) 118709627 1582
GKRP4-39 GKRP4-39 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives 633.49 2.56 Amgen Inc. (USA) C22H20F9N7O3S Hong, F. T. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket. J. Med. Chem. (2014) 118709628 1583
GKRP4-40 GKRP4-40 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives 551.46 2.4 Amgen Inc. (USA) C21H19F6N5O4S Hong, F. T. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket. J. Med. Chem. (2014) 118709629 1584
GKRP4-41 GKRP4-41 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives 581.55 3.41 Amgen Inc. (USA) C22H21F6N5O3S2 Hong, F. T. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket. J. Med. Chem. (2014) 118709630 1585
GKRP4-42 GKRP4-42 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives 561.5 3.33 Amgen Inc. (USA) C23H21F6N5O3S Hong, F. T. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket. J. Med. Chem. (2014) 118709631 1586
GKRP4-43 GKRP4-43 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives 579.49 3.43 Amgen Inc. (USA) C23H20F7N5O3S Hong, F. T. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket. J. Med. Chem. (2014) 118709632 1587
GKRP4-44 GKRP4-44 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives 579.49 3.43 Amgen Inc. (USA) C23H20F7N5O3S Hong, F. T. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket. J. Med. Chem. (2014) 118709633 1588
GKRP4-45 GKRP4-45 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives 579.49 3.43 Amgen Inc. (USA) C23H20F7N5O3S Hong, F. T. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket. J. Med. Chem. (2014) 118709634 1589
GKRP4-46 GKRP4-46 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives 577.5 2.98 Amgen Inc. (USA) C23H21F6N5O4S Hong, F. T. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket. J. Med. Chem. (2014) 118709635 1590
GKRP4-47 GKRP4-47 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives 654.6 2.3 Amgen Inc. (USA) C24H24F6N6O5S2 Hong, F. T. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket. J. Med. Chem. (2014) 118709636 1591
GKRP4-48 GKRP4-48 GK-GKRP disruptor 2014 Benzamide,Pyridine,Sulfoxide/Sulfone derivatives 604.52 2.21 Amgen Inc. (USA) C24H22F6N6O4S Hong, F. T. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket. J. Med. Chem. (2014) 118709637 1592
GKRP4-49 GKRP4-49 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives 639.59 2.57 Amgen Inc. (USA) C24H23F6N5O5S2 Hong, F. T. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket. J. Med. Chem. (2014) 118709638 1593
GKRP4-50 GKRP4-50 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives 562.49 2.26 Amgen Inc. (USA) C22H20F6N6O3S Hong, F. T. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket. J. Med. Chem. (2014) 118709639 1594
GKRP4-51 GKRP4-51 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives 562.49 2.26 Amgen Inc. (USA) C22H20F6N6O3S Hong, F. T. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket. J. Med. Chem. (2014) 73332001 1595
GKRP4-52 GKRP4-52 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives 580.48 2.36 Amgen Inc. (USA) C22H19F7N6O3S Hong, F. T. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket. J. Med. Chem. (2014) 118709640 1596
GKRP4-53 GKRP4-53 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives 580.48 2.36 Amgen Inc. (USA) C22H19F7N6O3S Hong, F. T. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket. J. Med. Chem. (2014) 118709641 1597
GKRP4-54 GKRP4-54 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives 576.51 2.63 Amgen Inc. (USA) C23H22F6N6O3S Hong, F. T. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket. J. Med. Chem. (2014) 118709642 1598
GKRP4-55 GKRP4-55 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives 576.51 2.66 Amgen Inc. (USA) C23H22F6N6O3S Hong, F. T. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket. J. Med. Chem. (2014) 118709643 1599
GKRP4-56 GKRP4-56 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives 592.51 2.57 Amgen Inc. (USA) C23H22F6N6O4S Hong, F. T. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket. J. Med. Chem. (2014) 118709644 1600
GKRP4-57 GKRP4-57 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives 592.51 2.23 Amgen Inc. (USA) C23H22F6N6O4S Hong, F. T. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket. J. Med. Chem. (2014) 118709645 1601
GKRP4-58 GKRP4-58 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives 617.59 4.35 Amgen Inc. (USA) C25H21F6N5O3S2 Hong, F. T. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket. J. Med. Chem. (2014) 118709646 1602
GKRP4-59 GKRP4-59 GK-GKRP disruptor 2014 Pyridine,Benzo/Pyrido-thiazole,Sulfoxide/Sulfone derivatives 618.57 3.79 Amgen Inc. (USA) C24H20F6N6O3S2 Hong, F. T. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket. J. Med. Chem. (2014) 118709647 1603
GKRP4-60 GKRP4-60 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives 602.51 3.17 Amgen Inc. (USA) C24H20F6N6O4S Hong, F. T. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket. J. Med. Chem. (2014) 118709648 1604
GKRP4-61 GKRP4-61 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives 616.54 3.57 Amgen Inc. (USA) C25H22F6N6O4S Hong, F. T. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket. J. Med. Chem. (2014) 118709649 1605
GKRP4-62 GKRP4-62 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives 630.56 2.36 Amgen Inc. (USA) C26H24F6N6O4S Hong, F. T. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket. J. Med. Chem. (2014) 118709650 1606
GKRP4-63 GKRP4-63 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives 616.54 2.18 Amgen Inc. (USA) C25H22F6N6O4S Hong, F. T. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket. J. Med. Chem. (2014) 118709651 1607
GKRP4-64 GKRP4-64 GK-GKRP disruptor 2014 Pyridine,Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 601.52 2.96 Amgen Inc. (USA) C24H21F6N7O3S Hong, F. T. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket. J. Med. Chem. (2014) 118709652 1608
GKRP4-65 GKRP4-65 GK-GKRP disruptor 2014 Pyridine,Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 601.52 2.96 Amgen Inc. (USA) C24H21F6N7O3S Hong, F. T. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket. J. Med. Chem. (2014) 118709653 1609
GKRP4-66 GKRP4-66 GK-GKRP disruptor 2014 Pyridine,Indole/Benzimidazole/Indazole,Sulfoxide/Sulfone derivatives 600.54 3.49 Amgen Inc. (USA) C25H22F6N6O3S Hong, F. T. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket. J. Med. Chem. (2014) 118709654 1610
GKRP4-67 GKRP4-67 GK-GKRP disruptor 2014 Pyridine,Sulfoxide/Sulfone derivatives 617.59 4.39 Amgen Inc. (USA) C25H21F6N5O3S2 Hong, F. T. et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket. J. Med. Chem. (2014) 118709655 1611
GKRP5-105 GKRP5-105 GK-GKRP disruptor 2015 Pyridine,Sulfoxide/Sulfone derivatives 480.38 2.58 Amgen Inc. (USA) C18H14F6N4O3S Tamayo, N. A. et al. Small Molecule Disruptors of the Glucokinase-Glucokinase Regulatory Protein Interaction: 5. A Novel Aryl Sulfone Series, Optimization Through Conformational Analysis. J. Med. Chem. (2015) 122178257 1649
GKRP5-110 GKRP5-110 GK-GKRP disruptor 2015 Pyridine,Sulfoxide/Sulfone derivatives 426.41 1.84 Amgen Inc. (USA) C18H17F3N4O3S Tamayo, N. A. et al. Small Molecule Disruptors of the Glucokinase-Glucokinase Regulatory Protein Interaction: 5. A Novel Aryl Sulfone Series, Optimization Through Conformational Analysis. J. Med. Chem. (2015) 122178258 1650
GKRP5-12 GKRP5-12 GK-GKRP disruptor 2015 Pyridine,Sulfoxide/Sulfone derivatives 477.38 3.09 Amgen Inc. (USA) C19H13F6N3O3S Tamayo, N. A. et al. Small Molecule Disruptors of the Glucokinase-Glucokinase Regulatory Protein Interaction: 5. A Novel Aryl Sulfone Series, Optimization Through Conformational Analysis. J. Med. Chem. (2015) 56933051 1613
GKRP5-13 GKRP5-13 GK-GKRP disruptor 2015 Pyridine,Pyrimidine,Sulfoxide/Sulfone derivatives 478.37 2.44 Amgen Inc. (USA) C18H12F6N4O3S Tamayo, N. A. et al. Small Molecule Disruptors of the Glucokinase-Glucokinase Regulatory Protein Interaction: 5. A Novel Aryl Sulfone Series, Optimization Through Conformational Analysis. J. Med. Chem. (2015) 86670436 1614
GKRP5-17 GKRP5-17 GK-GKRP disruptor 2015 Pyridine,Sulfoxide/Sulfone derivatives 424.4 1.31 Amgen Inc. (USA) C18H15F3N4O3S Tamayo, N. A. et al. Small Molecule Disruptors of the Glucokinase-Glucokinase Regulatory Protein Interaction: 5. A Novel Aryl Sulfone Series, Optimization Through Conformational Analysis. J. Med. Chem. (2015) 89762389 1615
GKRP5-20 GKRP5-20 GK-GKRP disruptor 2015 Pyridine,Sulfoxide/Sulfone derivatives 511.83 3.72 Amgen Inc. (USA) C19H12ClF6N3O3S Tamayo, N. A. et al. Small Molecule Disruptors of the Glucokinase-Glucokinase Regulatory Protein Interaction: 5. A Novel Aryl Sulfone Series, Optimization Through Conformational Analysis. J. Med. Chem. (2015) 71715076 1616
GKRP5-21 GKRP5-21 GK-GKRP disruptor 2015 Pyridine,Sulfoxide/Sulfone derivatives 507.41 3.06 Amgen Inc. (USA) C20H15F6N3O4S Tamayo, N. A. et al. Small Molecule Disruptors of the Glucokinase-Glucokinase Regulatory Protein Interaction: 5. A Novel Aryl Sulfone Series, Optimization Through Conformational Analysis. J. Med. Chem. (2015) 122178238 1617
GKRP5-22 GKRP5-22 GK-GKRP disruptor 2015 Pyridine,Sulfoxide/Sulfone derivatives 502.39 2.81 Amgen Inc. (USA) C20H12F6N4O3S Tamayo, N. A. et al. Small Molecule Disruptors of the Glucokinase-Glucokinase Regulatory Protein Interaction: 5. A Novel Aryl Sulfone Series, Optimization Through Conformational Analysis. J. Med. Chem. (2015) 122178239 1618
GKRP5-23 GKRP5-23 GK-GKRP disruptor 2015 Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 515.43 3.85 Amgen Inc. (USA) C22H15F6N3O3S Tamayo, N. A. et al. Small Molecule Disruptors of the Glucokinase-Glucokinase Regulatory Protein Interaction: 5. A Novel Aryl Sulfone Series, Optimization Through Conformational Analysis. J. Med. Chem. (2015) 71715077 1619
GKRP5-24 GKRP5-24 GK-GKRP disruptor 2015 Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 531.43 2.6 Amgen Inc. (USA) C22H15F6N3O4S Tamayo, N. A. et al. Small Molecule Disruptors of the Glucokinase-Glucokinase Regulatory Protein Interaction: 5. A Novel Aryl Sulfone Series, Optimization Through Conformational Analysis. J. Med. Chem. (2015) 71715135 1620
GKRP5-25 GKRP5-25 GK-GKRP disruptor 2015 Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 545.45 3.13 Amgen Inc. (USA) C23H17F6N3O4S Tamayo, N. A. et al. Small Molecule Disruptors of the Glucokinase-Glucokinase Regulatory Protein Interaction: 5. A Novel Aryl Sulfone Series, Optimization Through Conformational Analysis. J. Med. Chem. (2015) 71715133 1621
GKRP5-26 GKRP5-26 GK-GKRP disruptor 2015 Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 545.45 3 Amgen Inc. (USA) C23H17F6N3O4S Tamayo, N. A. et al. Small Molecule Disruptors of the Glucokinase-Glucokinase Regulatory Protein Interaction: 5. A Novel Aryl Sulfone Series, Optimization Through Conformational Analysis. J. Med. Chem. (2015) 122178240 1622
GKRP5-27 GKRP5-27 GK-GKRP disruptor 2015 Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 559.48 3.19 Amgen Inc. (USA) C24H19F6N3O4S Tamayo, N. A. et al. Small Molecule Disruptors of the Glucokinase-Glucokinase Regulatory Protein Interaction: 5. A Novel Aryl Sulfone Series, Optimization Through Conformational Analysis. J. Med. Chem. (2015) 122178241 1623
GKRP5-34 GKRP5-34 GK-GKRP disruptor 2015 Pyridine,Sulfoxide/Sulfone derivatives 453.44 1.92 Amgen Inc. (USA) C19H18F3N5O3S Tamayo, N. A. et al. Small Molecule Disruptors of the Glucokinase-Glucokinase Regulatory Protein Interaction: 5. A Novel Aryl Sulfone Series, Optimization Through Conformational Analysis. J. Med. Chem. (2015) 122178242 1624
GKRP5-35 GKRP5-35 GK-GKRP disruptor 2015 Pyridine,Sulfoxide/Sulfone derivatives 467.46 2.29 Amgen Inc. (USA) C20H20F3N5O3S Tamayo, N. A. et al. Small Molecule Disruptors of the Glucokinase-Glucokinase Regulatory Protein Interaction: 5. A Novel Aryl Sulfone Series, Optimization Through Conformational Analysis. J. Med. Chem. (2015) 122178243 1625
GKRP5-36 GKRP5-36 GK-GKRP disruptor 2015 Pyridine,Sulfoxide/Sulfone derivatives 481.49 2.72 Amgen Inc. (USA) C21H22F3N5O3S Tamayo, N. A. et al. Small Molecule Disruptors of the Glucokinase-Glucokinase Regulatory Protein Interaction: 5. A Novel Aryl Sulfone Series, Optimization Through Conformational Analysis. J. Med. Chem. (2015) 122178244 1626
GKRP5-37 GKRP5-37 GK-GKRP disruptor 2015 Pyridine,Sulfoxide/Sulfone derivatives 479.48 2.48 Amgen Inc. (USA) C21H20F3N5O3S Tamayo, N. A. et al. Small Molecule Disruptors of the Glucokinase-Glucokinase Regulatory Protein Interaction: 5. A Novel Aryl Sulfone Series, Optimization Through Conformational Analysis. J. Med. Chem. (2015) 122178245 1627
GKRP5-38 GKRP5-38 GK-GKRP disruptor 2015 Pyridine,Sulfoxide/Sulfone derivatives 521.56 3.73 Amgen Inc. (USA) C24H26F3N5O3S Tamayo, N. A. et al. Small Molecule Disruptors of the Glucokinase-Glucokinase Regulatory Protein Interaction: 5. A Novel Aryl Sulfone Series, Optimization Through Conformational Analysis. J. Med. Chem. (2015) 122178246 1628
GKRP5-39 GKRP5-39 GK-GKRP disruptor 2015 Pyridine,Sulfoxide/Sulfone derivatives 515.51 3.48 Amgen Inc. (USA) C24H20F3N5O3S Tamayo, N. A. et al. Small Molecule Disruptors of the Glucokinase-Glucokinase Regulatory Protein Interaction: 5. A Novel Aryl Sulfone Series, Optimization Through Conformational Analysis. J. Med. Chem. (2015) 122178247 1629
GKRP5-4 GKRP5-4 GK-GKRP disruptor 2015 Pyridine,Sulfoxide/Sulfone derivatives 422.42 3.38 Amgen Inc. (USA) C20H17F3N2O3S Tamayo, N. A. et al. Small Molecule Disruptors of the Glucokinase-Glucokinase Regulatory Protein Interaction: 5. A Novel Aryl Sulfone Series, Optimization Through Conformational Analysis. J. Med. Chem. (2015) 89528850 1612
GKRP5-40 GKRP5-40 GK-GKRP disruptor 2015 Pyridine,Sulfoxide/Sulfone derivatives 529.53 3.42 Amgen Inc. (USA) C25H22F3N5O3S Tamayo, N. A. et al. Small Molecule Disruptors of the Glucokinase-Glucokinase Regulatory Protein Interaction: 5. A Novel Aryl Sulfone Series, Optimization Through Conformational Analysis. J. Med. Chem. (2015) 122178248 1630
GKRP5-45 GKRP5-45 GK-GKRP disruptor 2015 Pyridine,Sulfoxide/Sulfone derivatives 516.49 3.47 Amgen Inc. (USA) C24H19F3N4O4S Tamayo, N. A. et al. Small Molecule Disruptors of the Glucokinase-Glucokinase Regulatory Protein Interaction: 5. A Novel Aryl Sulfone Series, Optimization Through Conformational Analysis. J. Med. Chem. (2015) 122178249 1631
GKRP5-46 GKRP5-46 GK-GKRP disruptor 2015 Pyridine,Sulfoxide/Sulfone derivatives 516.5 2.41 Amgen Inc. (USA) C23H19F3N6O3S Tamayo, N. A. et al. Small Molecule Disruptors of the Glucokinase-Glucokinase Regulatory Protein Interaction: 5. A Novel Aryl Sulfone Series, Optimization Through Conformational Analysis. J. Med. Chem. (2015) 122178250 1632
GKRP5-47 GKRP5-47 GK-GKRP disruptor 2015 Pyridine,Sulfoxide/Sulfone derivatives 516.5 2.41 Amgen Inc. (USA) C23H19F3N6O3S Tamayo, N. A. et al. Small Molecule Disruptors of the Glucokinase-Glucokinase Regulatory Protein Interaction: 5. A Novel Aryl Sulfone Series, Optimization Through Conformational Analysis. J. Med. Chem. (2015) 122178251 1633
GKRP5-48 GKRP5-48 GK-GKRP disruptor 2015 Pyridine,Sulfoxide/Sulfone derivatives 516.5 2.75 Amgen Inc. (USA) C23H19F3N6O3S Tamayo, N. A. et al. Small Molecule Disruptors of the Glucokinase-Glucokinase Regulatory Protein Interaction: 5. A Novel Aryl Sulfone Series, Optimization Through Conformational Analysis. J. Med. Chem. (2015) 122178252 1634
GKRP5-58 GKRP5-58 GK-GKRP disruptor 2015 Pyridine,Pyrimidine,Sulfoxide/Sulfone derivatives 430.42 1.74 Amgen Inc. (USA) C16H13F3N4O3S2 Tamayo, N. A. et al. Small Molecule Disruptors of the Glucokinase-Glucokinase Regulatory Protein Interaction: 5. A Novel Aryl Sulfone Series, Optimization Through Conformational Analysis. J. Med. Chem. (2015) 122178253 1635
GKRP5-59 GKRP5-59 GK-GKRP disruptor 2015 Pyridine,Sulfoxide/Sulfone derivatives 463.88 3.02 Amgen Inc. (USA) C17H13ClF3N3O3S2 Tamayo, N. A. et al. Small Molecule Disruptors of the Glucokinase-Glucokinase Regulatory Protein Interaction: 5. A Novel Aryl Sulfone Series, Optimization Through Conformational Analysis. J. Med. Chem. (2015) 122178259 1636
GKRP5-60 GKRP5-60 GK-GKRP disruptor 2015 Pyridine,Sulfoxide/Sulfone derivatives,Subsituted ethynyl 467.48 3.15 Amgen Inc. (USA) C20H16F3N3O3S2 Tamayo, N. A. et al. Small Molecule Disruptors of the Glucokinase-Glucokinase Regulatory Protein Interaction: 5. A Novel Aryl Sulfone Series, Optimization Through Conformational Analysis. J. Med. Chem. (2015) 122178260 1637
GKRP5-65 GKRP5-65 GK-GKRP disruptor 2015 Pyridine,Sulfoxide/Sulfone derivatives 428.45 3.43 Amgen Inc. (USA) C18H15F3N2O3S2 Tamayo, N. A. et al. Small Molecule Disruptors of the Glucokinase-Glucokinase Regulatory Protein Interaction: 5. A Novel Aryl Sulfone Series, Optimization Through Conformational Analysis. J. Med. Chem. (2015) 122178254 1638
GKRP5-86 GKRP5-86 GK-GKRP disruptor 2015 Thiazole/Thiadiazole,Pyridine,Sulfoxide/Sulfone derivatives 483.41 3.52 Amgen Inc. (USA) C17H11F6N3O3S2 Tamayo, N. A. et al. Small Molecule Disruptors of the Glucokinase-Glucokinase Regulatory Protein Interaction: 5. A Novel Aryl Sulfone Series, Optimization Through Conformational Analysis. J. Med. Chem. (2015) 122178255 1639
GKRP5-87 GKRP5-87 GK-GKRP disruptor 2015 Thiazole/Thiadiazole,Pyridine,Sulfoxide/Sulfone derivatives 463.88 3.41 Amgen Inc. (USA) C17H13ClF3N3O3S2 Tamayo, N. A. et al. Small Molecule Disruptors of the Glucokinase-Glucokinase Regulatory Protein Interaction: 5. A Novel Aryl Sulfone Series, Optimization Through Conformational Analysis. J. Med. Chem. (2015) 122178262 1640
GKRP5-88 GKRP5-88 GK-GKRP disruptor 2015 Thiazole/Thiadiazole,Pyridine,Sulfoxide/Sulfone derivatives 463.88 3.41 Amgen Inc. (USA) C17H13ClF3N3O3S2 Tamayo, N. A. et al. Small Molecule Disruptors of the Glucokinase-Glucokinase Regulatory Protein Interaction: 5. A Novel Aryl Sulfone Series, Optimization Through Conformational Analysis. J. Med. Chem. (2015) 122178262 1641
GKRP5-89 GKRP5-89 GK-GKRP disruptor 2015 Thiazole/Thiadiazole,Pyridine,Sulfoxide/Sulfone derivatives 463.88 3.41 Amgen Inc. (USA) C17H13ClF3N3O3S2 Tamayo, N. A. et al. Small Molecule Disruptors of the Glucokinase-Glucokinase Regulatory Protein Interaction: 5. A Novel Aryl Sulfone Series, Optimization Through Conformational Analysis. J. Med. Chem. (2015) 122178263 1642
GKRP5-90 GKRP5-90 GK-GKRP disruptor 2015 Thiazole/Thiadiazole,Pyridine,Sulfoxide/Sulfone derivatives 409.91 2.66 Amgen Inc. (USA) C17H16ClN3O3S2 Tamayo, N. A. et al. Small Molecule Disruptors of the Glucokinase-Glucokinase Regulatory Protein Interaction: 5. A Novel Aryl Sulfone Series, Optimization Through Conformational Analysis. J. Med. Chem. (2015) 122178264 1643
GKRP5-91 GKRP5-91 GK-GKRP disruptor 2015 Thiazole/Thiadiazole,Pyridine,Sulfoxide/Sulfone derivatives 430.91 1.52 Amgen Inc. (USA) C14H11ClN4O4S3 Tamayo, N. A. et al. Small Molecule Disruptors of the Glucokinase-Glucokinase Regulatory Protein Interaction: 5. A Novel Aryl Sulfone Series, Optimization Through Conformational Analysis. J. Med. Chem. (2015) 122178265 1644
GKRP5-92 GKRP5-92 GK-GKRP disruptor 2015 Thiazole/Thiadiazole,Pyridine,Sulfoxide/Sulfone derivatives 425.91 1.61 Amgen Inc. (USA) C17H16ClN3O4S2 Tamayo, N. A. et al. Small Molecule Disruptors of the Glucokinase-Glucokinase Regulatory Protein Interaction: 5. A Novel Aryl Sulfone Series, Optimization Through Conformational Analysis. J. Med. Chem. (2015) 122178267 1645
GKRP5-93 GKRP5-93 GK-GKRP disruptor 2015 Thiazole/Thiadiazole,Pyridine,Sulfoxide/Sulfone derivatives 425.91 1.61 Amgen Inc. (USA) C17H16ClN3O4S2 Tamayo, N. A. et al. Small Molecule Disruptors of the Glucokinase-Glucokinase Regulatory Protein Interaction: 5. A Novel Aryl Sulfone Series, Optimization Through Conformational Analysis. J. Med. Chem. (2015) 122178268 1646
GKRP5-94 GKRP5-94 GK-GKRP disruptor 2015 Thiazole/Thiadiazole,Pyridine,Sulfoxide/Sulfone derivatives 425.91 1.61 Amgen Inc. (USA) C17H16ClN3O4S2 Tamayo, N. A. et al. Small Molecule Disruptors of the Glucokinase-Glucokinase Regulatory Protein Interaction: 5. A Novel Aryl Sulfone Series, Optimization Through Conformational Analysis. J. Med. Chem. (2015) 122178267 1647
GKRP5-99 GKRP5-99 GK-GKRP disruptor 2015 Thiazole/Thiadiazole,Pyridine,Sulfoxide/Sulfone derivatives 483.41 3.52 Amgen Inc. (USA) C17H11F6N3O3S2 Tamayo, N. A. et al. Small Molecule Disruptors of the Glucokinase-Glucokinase Regulatory Protein Interaction: 5. A Novel Aryl Sulfone Series, Optimization Through Conformational Analysis. J. Med. Chem. (2015) 122178256 1648
GKRP6-11 GKRP6-11 GK-GKRP disruptor 2015 Sulfoxide/Sulfone derivatives 469.94 5.22 Amgen Inc. (USA) C24H20ClNO5S Pennington, L. D. et al. Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase-Glucokinase Regulatory Protein (GK-GKRP) Binding: Strategic Use of a N → S (nN → σ∗ S-X) Interaction for Conformational Constraint. J. Med. Chem. (2015) 66556625 1654
GKRP6-12 GKRP6-12 GK-GKRP disruptor 2015 Sulfoxide/Sulfone derivatives 486 5.83 Amgen Inc. (USA) C24H20ClNO4S2 Pennington, L. D. et al. Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase-Glucokinase Regulatory Protein (GK-GKRP) Binding: Strategic Use of a N → S (nN → σ∗ S-X) Interaction for Conformational Constraint. J. Med. Chem. (2015) 70818806 1655
GKRP6-13 GKRP6-13 GK-GKRP disruptor 2015 Sulfoxide/Sulfone derivatives 502 4.86 Amgen Inc. (USA) C24H20ClNO5S2 Pennington, L. D. et al. Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase-Glucokinase Regulatory Protein (GK-GKRP) Binding: Strategic Use of a N → S (nN → σ∗ S-X) Interaction for Conformational Constraint. J. Med. Chem. (2015) 90195507 1656
GKRP6-14 GKRP6-14 GK-GKRP disruptor 2015 Sulfoxide/Sulfone derivatives 503.99 5.89 Amgen Inc. (USA) C24H19ClFNO4S2 Pennington, L. D. et al. Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase-Glucokinase Regulatory Protein (GK-GKRP) Binding: Strategic Use of a N → S (nN → σ∗ S-X) Interaction for Conformational Constraint. J. Med. Chem. (2015) 90195515 1657
GKRP6-15 GKRP6-15 GK-GKRP disruptor 2015 Sulfoxide/Sulfone derivatives 521.98 6.15 Amgen Inc. (USA) C24H18ClF2NO4S2 Pennington, L. D. et al. Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase-Glucokinase Regulatory Protein (GK-GKRP) Binding: Strategic Use of a N → S (nN → σ∗ S-X) Interaction for Conformational Constraint. J. Med. Chem. (2015) 66557138 1658
GKRP6-16 GKRP6-16 GK-GKRP disruptor 2015 Sulfoxide/Sulfone derivatives 487.98 4.53 Amgen Inc. (USA) C22H18ClN3O4S2 Pennington, L. D. et al. Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase-Glucokinase Regulatory Protein (GK-GKRP) Binding: Strategic Use of a N → S (nN → σ∗ S-X) Interaction for Conformational Constraint. J. Med. Chem. (2015) 70819298 1659
GKRP6-17 GKRP6-17 GK-GKRP disruptor 2015 Sulfoxide/Sulfone derivatives 471.98 5.48 Amgen Inc. (USA) C23H18ClNO4S2 Pennington, L. D. et al. Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase-Glucokinase Regulatory Protein (GK-GKRP) Binding: Strategic Use of a N → S (nN → σ∗ S-X) Interaction for Conformational Constraint. J. Med. Chem. (2015) 127038966 1660
GKRP6-18 GKRP6-18 GK-GKRP disruptor 2015 Sulfoxide/Sulfone derivatives 457.95 5.57 Amgen Inc. (USA) C22H16ClNO4S2 Pennington, L. D. et al. Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase-Glucokinase Regulatory Protein (GK-GKRP) Binding: Strategic Use of a N → S (nN → σ∗ S-X) Interaction for Conformational Constraint. J. Med. Chem. (2015) 127038967 1661
GKRP6-19 GKRP6-19 GK-GKRP disruptor 2015 Sulfoxide/Sulfone derivatives 443.97 5.73 Amgen Inc. (USA) C22H18ClNO3S2 Pennington, L. D. et al. Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase-Glucokinase Regulatory Protein (GK-GKRP) Binding: Strategic Use of a N → S (nN → σ∗ S-X) Interaction for Conformational Constraint. J. Med. Chem. (2015) 127039284 1662
GKRP6-20 GKRP6-20 GK-GKRP disruptor 2015 Sulfoxide/Sulfone derivatives 413.94 5.76 Amgen Inc. (USA) C21H16ClNO2S2 Pennington, L. D. et al. Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase-Glucokinase Regulatory Protein (GK-GKRP) Binding: Strategic Use of a N → S (nN → σ∗ S-X) Interaction for Conformational Constraint. J. Med. Chem. (2015) 127039285 1663
GKRP6-21 GKRP6-21 GK-GKRP disruptor 2015 Sulfoxide/Sulfone derivatives 377.91 4.76 Amgen Inc. (USA) C18H16ClNO2S2 Pennington, L. D. et al. Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase-Glucokinase Regulatory Protein (GK-GKRP) Binding: Strategic Use of a N → S (nN → σ∗ S-X) Interaction for Conformational Constraint. J. Med. Chem. (2015) 127039286 1664
GKRP6-22 GKRP6-22 GK-GKRP disruptor 2015 Sulfoxide/Sulfone derivatives 566.05 6.83 Amgen Inc. (USA) C27H23ClF3NO3S2 Pennington, L. D. et al. Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase-Glucokinase Regulatory Protein (GK-GKRP) Binding: Strategic Use of a N → S (nN → σ∗ S-X) Interaction for Conformational Constraint. J. Med. Chem. (2015) 127040636 1665
GKRP6-23 GKRP6-23 GK-GKRP disruptor 2015 Sulfoxide/Sulfone derivatives 566.05 6.83 Amgen Inc. (USA) C27H23ClF3NO3S2 Pennington, L. D. et al. Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase-Glucokinase Regulatory Protein (GK-GKRP) Binding: Strategic Use of a N → S (nN → σ∗ S-X) Interaction for Conformational Constraint. J. Med. Chem. (2015) 127040949 1666
GKRP6-24 GKRP6-24 GK-GKRP disruptor 2015 Pyridine,Sulfoxide/Sulfone derivatives 567.04 5.8 Amgen Inc. (USA) C26H22ClF3N2O3S2 Pennington, L. D. et al. Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase-Glucokinase Regulatory Protein (GK-GKRP) Binding: Strategic Use of a N → S (nN → σ∗ S-X) Interaction for Conformational Constraint. J. Med. Chem. (2015) 72549535 1667
GKRP6-25 GKRP6-25 GK-GKRP disruptor 2015 Pyridine,Sulfoxide/Sulfone derivatives 567.04 5.8 Amgen Inc. (USA) C26H22ClF3N2O3S2 Pennington, L. D. et al. Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase-Glucokinase Regulatory Protein (GK-GKRP) Binding: Strategic Use of a N → S (nN → σ∗ S-X) Interaction for Conformational Constraint. J. Med. Chem. (2015) 72550209 1668
GKRP6-26 GKRP6-26 GK-GKRP disruptor 2015 Pyridine,Sulfoxide/Sulfone derivatives 513.07 5.05 Amgen Inc. (USA) C26H25ClN2O3S2 Pennington, L. D. et al. Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase-Glucokinase Regulatory Protein (GK-GKRP) Binding: Strategic Use of a N → S (nN → σ∗ S-X) Interaction for Conformational Constraint. J. Med. Chem. (2015) 72548598 1669
GKRP6-27 GKRP6-27 GK-GKRP disruptor 2015 Pyridine,Sulfoxide/Sulfone derivatives 531.06 5.15 Amgen Inc. (USA) C26H24ClFN2O3S2 Pennington, L. D. et al. Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase-Glucokinase Regulatory Protein (GK-GKRP) Binding: Strategic Use of a N → S (nN → σ∗ S-X) Interaction for Conformational Constraint. J. Med. Chem. (2015) 89905482 1670
GKRP6-28 GKRP6-28 GK-GKRP disruptor 2015 Pyridine,Sulfoxide/Sulfone derivatives 529.07 3.67 Amgen Inc. (USA) C25H25ClN4O3S2 Pennington, L. D. et al. Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase-Glucokinase Regulatory Protein (GK-GKRP) Binding: Strategic Use of a N → S (nN → σ∗ S-X) Interaction for Conformational Constraint. J. Med. Chem. (2015) 72548601 1671
GKRP6-29 GKRP6-29 GK-GKRP disruptor 2015 Pyridine,Sulfoxide/Sulfone derivatives 547.06 3.77 Amgen Inc. (USA) C25H24ClFN4O3S2 Pennington, L. D. et al. Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase-Glucokinase Regulatory Protein (GK-GKRP) Binding: Strategic Use of a N → S (nN → σ∗ S-X) Interaction for Conformational Constraint. J. Med. Chem. (2015) 89905917 1672
GKRP6-30 GKRP6-30 GK-GKRP disruptor 2015 Pyridine,Sulfoxide/Sulfone derivatives 529.07 3.63 Amgen Inc. (USA) C25H25ClN4O3S2 Pennington, L. D. et al. Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase-Glucokinase Regulatory Protein (GK-GKRP) Binding: Strategic Use of a N → S (nN → σ∗ S-X) Interaction for Conformational Constraint. J. Med. Chem. (2015) 127042206 1673
GKRP6-31 GKRP6-31 GK-GKRP disruptor 2015 Pyridine,Pyrimidine,Sulfoxide/Sulfone derivatives 530.06 3.02 Amgen Inc. (USA) C24H24ClN5O3S2 Pennington, L. D. et al. Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase-Glucokinase Regulatory Protein (GK-GKRP) Binding: Strategic Use of a N → S (nN → σ∗ S-X) Interaction for Conformational Constraint. J. Med. Chem. (2015) 76903476 1674
GKRP6-32 GKRP6-32 GK-GKRP disruptor 2015 Pyridine,Sulfoxide/Sulfone derivatives 547.06 3.74 Amgen Inc. (USA) C25H24ClFN4O3S2 Pennington, L. D. et al. Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase-Glucokinase Regulatory Protein (GK-GKRP) Binding: Strategic Use of a N → S (nN → σ∗ S-X) Interaction for Conformational Constraint. J. Med. Chem. (2015) 89905551 1675
GKRP6-6 GKRP6-6 GK-GKRP disruptor 2015 Sulfoxide/Sulfone derivatives 435.49 4.59 Amgen Inc. (USA) C24H21NO5S Pennington, L. D. et al. Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase-Glucokinase Regulatory Protein (GK-GKRP) Binding: Strategic Use of a N → S (nN → σ∗ S-X) Interaction for Conformational Constraint. J. Med. Chem. (2015) 25956468 1651
GKRP6-7 GKRP6-7 GK-GKRP disruptor 2015 Sulfoxide/Sulfone derivatives 435.49 4.59 Amgen Inc. (USA) C24H21NO5S Pennington, L. D. et al. Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase-Glucokinase Regulatory Protein (GK-GKRP) Binding: Strategic Use of a N → S (nN → σ∗ S-X) Interaction for Conformational Constraint. J. Med. Chem. (2015) 25956468 1652
GKRP6-7__S-_ GKRP6-7 (S-) GK-GKRP disruptor 2015 Sulfoxide/Sulfone derivatives 435.49 4.59 Amgen Inc. (USA) C24H21NO5S Pennington, L. D. et al. Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase-Glucokinase Regulatory Protein (GK-GKRP) Binding: Strategic Use of a N → S (nN → σ∗ S-X) Interaction for Conformational Constraint. J. Med. Chem. (2015) 25956467 1653
Globalagliatin Globalagliatin/AMG-1694 GKA: Systemic 2020 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 533.63 3.29 Yabao Pharmaceutical Group (CHINA) C23H30F3N3O4S2 Zheng, S. et al. Safety, Pharmacokinetics, and Pharmacodynamics of Globalagliatin, a Glucokinase Activator, in Chinese Patients with Type 2 Diabetes Mellitus: A Randomized, Phase Ib, 28-day Ascending Dose Study. Clin. Drug Investig. (2020) 66582747 15
LY2121260 LY2121260 GKA: Systemic 2005 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 404.55 4.28 Lilly Research Laboratories (Germany) C20H24N2O3S2 Efanov, A. M. et al. A novel glucokinase activator modulates pancreatic islet and hepatocyte function. Endocrinology (2005) 10341191 2
MK-0941 MK-0941 GKA: Systemic 2011 Benzamide,Pyridine,Sulfoxide/Sulfone derivatives 460.5 1.52 Banyu Tsukuba Research Institute (JAPAN) & Merck (USA) C21H24N4O6S Eiki, J. I. et al. Pharmacokinetic and pharmacodynamic properties of the glucokinase activator MK-0941 in rodent models of type 2 diabetes and healthy dogs. Mol. Pharmacol. (2011) 25235801 7
PF-04991532 PF-04991532 GKA: Hepatoselective 2014 Pyridine 396.36 3.32 Pfizer Global Research & Development (USA) C18H19F3N4O3 Erion, D. M. et al. The hepatoselective glucokinase activator PF-04991532 ameliorates hyperglycemia without causing hepatic steatosis in diabetic rats. PLoS One (2014) 46181428 9
Piragliatin Piragliatin (RO4389620) GKA: Systemic 0 Pyrazine,Sulfoxide/Sulfone derivatives 421.9 1.21 Hoffmann-La Roche Inc. (USA) C19H20ClN3O4S Bonadonna, R. C. et al. Piragliatin (RO4389620), a Novel Glucokinase Activator, Lowers Plasma Glucose Both in the Postabsorptive State and after a Glucose Challenge in Patients with Type 2 Diabetes Mellitus: A Mechanistic Study. J. Clin. Endocrinol. Metab. 95, 5028–5036 (2010) & Sarabu, R. et al. Discovery of piragliatin-first glucokinase activator studied in type 2 diabetic patients. J. Med. Chem. (2012) 10432339 5
PSN-GK1 PSN-GK1 GKA: Systemic 2008 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 438.54 3.27 OSI Pharmaceuticals (USA); Prosidion Limited (UK) C20H23FN2O4S2 Bertram, L. S. et al. SAR, pharmacokinetics, safety, and efficacy of glucokinase activating 2-(4-sulfonylphenyl)-N-thiazol-2-ylacetamides: Discovery of PSN-GK1. J. Med. Chem. (2008) 11743862 6
RO-28-1675 RO-28-1675 GKA: Systemic 2003 Thiazole/Thiadiazole,Sulfoxide/Sulfone derivatives 378.51 3.88 Hoffmann-La Roche Inc. (USA) C18H22N2O3S2 Grimsby, J. et al. Allosteric activators of glucokinase: Potential role in diabetes therapy. Science. (2003) 9886086 0
SHP289-03 SHP289-03 GKA: Systemic 2015 Benzamide,Pyridine 424.42 3.98 Chinese Academy of Medical Sciences (Beijing, CHINA) C23H21FN2O5 Lei, L. et al. Antidiabetic potential of a novel dual-target activator of glucokinase and peroxisome proliferator activated receptor-γ. Metabolism. (2015) 71556708 10
SHP289-04 SHP289-04 GKA: Systemic 2018 Benzamide,Pyridine 410.4 3.45 Chinese Academy of Medical Sciences (Beijing, CHINA) C22H19FN2O5 Lei, L. et al. The potential role of glucokinase activator SHP289-04 in anti-diabetes and hepatic protection. Eur. J. Pharmacol. (2018) 71556513 13
TTP-399 TTP-399 GKA: Hepatoselective 2019 Thiazole/Thiadiazole,Urea 455.63 4.8 vTv Therapeutics (USA) C21H33N3O4S2 Vella, A. et al. Targeting hepatic glucokinase to treat diabetes with TTP399, a hepatoselective glucokinase activator. Sci. Transl. Med. (2019) 54673176 14
YH-GKA YH-GKA GKA: Systemic 2012 Benzamide,Pyridine 470.47 4.22 Yuhan Research Institute (SOUTH KOREA) C25H24F2N2O5 Park, K. Identification of YH-GKA, a novel benzamide glucokinase activator as therapeutic candidate for type 2 diabetes mellitus. Arch. Pharm. Res. (2012) 71533605 8