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Target
Glucose-dependent insulinotropic receptor
Ligand
BDBM50026192
Substrate
n/a
Meas. Tech.
ChEMBL_1438933 (CHEMBL3382444)
EC50
3500±n/a nM
Citation
 Wacker, DA; Wang, Y; Broekema, M; Rossi, K; O'Connor, S; Hong, Z; Wu, G; Malmstrom, SE; Hung, CP; LaMarre, L; Chimalakonda, A; Zhang, L; Xin, L; Cai, H; Chu, C; Boehm, S; Zalaznick, J; Ponticiello, R; Sereda, L; Han, SP; Zebo, R; Zinker, B; Luk, CE; Wong, R; Everlof, G; Li, YX; Wu, CK; Lee, M; Griffen, S; Miller, KJ; Krupinski, J; Robl, JA Discovery of 5-chloro-4-((1-(5-chloropyrimidin-2-yl)piperidin-4-yl)oxy)-1-(2-fluoro-4-(methylsulfonyl)phenyl)pyridin-2(1H)-one (BMS-903452), an antidiabetic clinical candidate targeting GPR119. J Med Chem 57:7499-508 (2014) [PubMed]  Article 
Target
Name:
Glucose-dependent insulinotropic receptor
Synonyms:
G-protein coupled receptor 119 (GPR119) | GP119_HUMAN | GPR119 | Glucose-dependent insulinotropic receptor
Type:
Protein
Mol. Mass.:
36901.49
Organism:
Homo sapiens (Human)
Description:
Q8TDV5
Residue:
335
Sequence:
MESSFSFGVILAVLASLIIATNTLVAVAVLLLIHKNDGVSLCFTLNLAVADTLIGVAISGLLTDQLSSPSRPTQKTLCSLRMAFVTSSAAASVLTVMLITFDRYLAIKQPFRYLKIMSGFVAGACIAGLWLVSYLIGFLPLGIPMFQQTAYKGQCSFFAVFHPHFVLTLSCVGFFPAMLLFVFFYCDMLKIASMHSQQIRKMEHAGAMAGGYRSPRTPSDFKALRTVSVLIGSFALSWTPFLITGIVQVACQECHLYLVLERYLWLLGVGNSLLNPLIYAYWQKEVRLQLYHMALGVKKVLTSFLLFLSARNCGPERPRESSCHIVTISSSEFDG
  
Inhibitor
Name:
BDBM50026192
Synonyms:
CHEMBL3338166
Type:
Small organic molecule
Emp. Form.:
C23H28N2O6S
Mol. Mass.:
460.543
SMILES:
[H][C@@]12CC[C@]([H])(CC(C1)Oc1ccn(-c3ccc(cc3)S(C)(=O)=O)c(=O)c1)N2C(=O)OC(C)C |r,@@:7,THB:9:7:27:2.3|
Structure:
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