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Target
Glucose-dependent insulinotropic receptor
Ligand
BDBM50343459
Substrate
n/a
Meas. Tech.
ChEMBL_746177 (CHEMBL1775791)
EC50
21±n/a nM
Citation
Semple, G; Ren, A; Fioravanti, B; Pereira, G; Calderon, I; Choi, K; Xiong, Y; Shin, YJ; Gharbaoui, T; Sage, CR; Morgan, M; Xing, C; Chu, ZL; Leonard, JN; Grottick, AJ; Al-Shamma, H; Liang, Y; Demarest, KT; Jones, RM Discovery of fused bicyclic agonists of the orphan G-protein coupled receptor GPR119 with in vivo activity in rodent models of glucose control. Bioorg Med Chem Lett 21:3134-41 (2011) [PubMed] Article
More Info.:
Target
Name:
Glucose-dependent insulinotropic receptor
Synonyms:
GP119_RAT | Gpr119
Type:
PROTEIN
Mol. Mass.:
51687.59
Organism:
Rattus norvegicus
Description:
ChEMBL_1506411
Residue:
468
Sequence:
MESSFSFGVILAVLTILIIAVNALVVVAMLLSIYKNDGVGLCFTLNLAVADTLIGVAISGLVTDQLSSSAQHTQKTLCSLRMAFVTSSAAASVLTVMLIAFDRYLAIKQPLRYFQIMNGLVAGGCIAGLWLISYLIGFLPLGVSIFQQTTYHGPCTFFAVFHPRFVLTLSCAGFFPAVLLFVFFYCDMLKIASVHSQHIRKMEHAGAMVGACRPPRPVNDFKAVRTVSVLIGSFTLSWSPFLITSIVQVACHKCCLYQVLEKYLWLLGVGNSLLNPLIYAYWQREVRQQLCHMALGLLADGSTQPQIETLKGKEERKKVGRKTLYTCDAQTLYTCDAQTLYTCDAQTLYTCDACDTQTLYTCDAQTLYTCDAQTLYTCDAQTLYTCDAQTLYTCDAQTLYTCDTQTLYTCDAQTLYTCDAQTLYTCDAQTLYTCDAQTLYTSSLVTGQTEQTPLKRANMSDPLRTCRG
Inhibitor
Name:
BDBM50343459
Synonyms:
CHEMBL1775174 | cyclopentyl 4-(1-(4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)piperidine-1-carboxylate
Type:
Small organic molecule
Emp. Form.:
C23H27N5O5S
Mol. Mass.:
485.556
SMILES:
CS(=O)(=O)c1ccc(cc1)-n1ncc2c(OC3CCN(CC3)C(=O)OC3CCCC3)ncnc12