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Target
G-protein coupled bile acid receptor 1
Ligand
BDBM50300201
Substrate
n/a
Meas. Tech.
ChEMBL_592751 (CHEMBL1043242)
EC50
4790±n/a nM
Citation
 Pellicciari, R; Gioiello, A; Macchiarulo, A; Thomas, C; Rosatelli, E; Natalini, B; Sardella, R; Pruzanski, M; Roda, A; Pastorini, E; Schoonjans, K; Auwerx, J Discovery of 6alpha-ethyl-23(S)-methylcholic acid (S-EMCA, INT-777) as a potent and selective agonist for the TGR5 receptor, a novel target for diabesity. J Med Chem 52:7958-61 (2009) [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:
BDBM50300201
Synonyms:
3alpha,7alpha,12alpha-Trihydroxy-6alpha-ethyl-5beta-cholan-24-oic acid | CHEMBL567835
Type:
Small organic molecule
Emp. Form.:
C26H44O5
Mol. Mass.:
436.6246
SMILES:
CC[C@H]1[C@@H](O)[C@H]2[C@@H]3CC[C@H]([C@H](C)CCC(O)=O)[C@@]3(C)[C@@H](O)C[C@@H]2[C@@]2(C)CC[C@@H](O)C[C@@H]12 |r|
Structure:
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