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Target
G-protein coupled bile acid receptor 1
Ligand
BDBM50236240
Substrate
n/a
Meas. Tech.
ChEMBL_472949 (CHEMBL949256)
EC50
3200±n/a nM
Citation
 Sato, H; Macchiarulo, A; Thomas, C; Gioiello, A; Une, M; Hofmann, AF; Saladin, R; Schoonjans, K; Pellicciari, R; Auwerx, J Novel potent and selective bile acid derivatives as TGR5 agonists: biological screening, structure-activity relationships, and molecular modeling studies. J Med Chem 51:1831-41 (2008) [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:
BDBM50236240
Synonyms:
5alpha-androstan-3beta-OL-17-one | CHEMBL272195 | Epiandrosterone | epi-andosterone
Type:
Small organic molecule
Emp. Form.:
C19H30O2
Mol. Mass.:
290.4403
SMILES:
C[C@]12CC[C@H]3[C@@H](CC[C@H]4C[C@@H](O)CC[C@]34C)[C@@H]1CCC2=O |r|
Structure:
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