Reaction Details Report a problem with these data
Target
G-protein coupled bile acid receptor 1
Ligand
BDBM50266580
Substrate
n/a
Meas. Tech.
ChEMBL_1700964 (CHEMBL4051946)
EC50
77±n/a nM
Citation
 Lasalle, M; Hoguet, V; Hennuyer, N; Leroux, F; Piveteau, C; Belloy, L; Lestavel, S; Vallez, E; Dorchies, E; Duplan, I; Sevin, E; Culot, M; Gosselet, F; Boulahjar, R; Herledan, A; Staels, B; Deprez, B; Tailleux, A; Charton, J Topical Intestinal Aminoimidazole Agonists of G-Protein-Coupled Bile Acid Receptor 1 Promote Glucagon Like Peptide-1 Secretion and Improve Glucose Tolerance. J Med Chem 60:4185-4211 (2017) [PubMed]  Article 
Target
Name:
G-protein coupled bile acid receptor 1
Synonyms:
BG37 | GPBAR1 | GPBAR_HUMAN | M-BAR | TGR5 | hBG37 | hGPCR19
Type:
G Protein-Coupled Receptor (GPCR)
Mol. Mass.:
35260.02
Organism:
Homo sapiens (Human)
Description:
CHO cells transiently transfected with hTGR5.
Residue:
330
Sequence:
MTPNSTGEVPSPIPKGALGLSLALASLIITANLLLALGIAWDRRLRSPPAGCFFLSLLLAGLLTGLALPTLPGLWNQSRRGYWSCLLVYLAPNFSFLSLLANLLLVHGERYMAVLRPLQPPGSIRLALLLTWAGPLLFASLPALGWNHWTPGANCSSQAIFPAPYLYLEVYGLLLPAVGAAAFLSVRVLATAHRQLQDICRLERAVCRDEPSALARALTWRQARAQAGAMLLFGLCWGPYVATLLLSVLAYEQRPPLGPGTLLSLLSLGSASAAAVPVAMGLGDQRYTAPWRAAAQRCLQGLWGRASRDSPGPSIAYHPSSQSSVDLDLN
  
Inhibitor
Name:
BDBM50266580
Synonyms:
CHEMBL4087611
Type:
Small organic molecule
Emp. Form.:
C32H43F3N6O9S3
Mol. Mass.:
808.909
SMILES:
N.N.COc1ccc(cc1OC)N(C)c1cnc(SCc2c(F)cc(OCCCN(CCS(O)(=O)=O)CCS(O)(=O)=O)cc2F)n1-c1ccc(F)cc1
Structure:
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