Target
G-protein coupled bile acid receptor 1
Ligand
BDBM50437877
Substrate
n/a
Meas. Tech.
ChEMBL_974032 (CHEMBL2410510)
EC50
4.0±n/a nM
Citation
 Dehmlow, HAlvarez Sánchez, RBachmann, SBissantz, CBliss, FConde-Knape, KGraf, MMartin, REObst Sander, URaab, SRichter, HGSewing, SSprecher, UUllmer, CMattei, P Discovery and optimisation of 1-hydroxyimino-3,3-diphenylpropanes, a new class of orally active GPBAR1 (TGR5) agonists. Bioorg Med Chem Lett 23:4627-32 (2013) [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:
BDBM50437877
Synonyms:
CHEMBL2407930
Type:
Small organic molecule
Emp. Form.:
C28H31N3O3
Mol. Mass.:
457.564
SMILES:
Cc1cc(ccn1)C(C[C@H](c1ccc(cc1)N1CCC(CC1)C(O)=O)c1ccccc1C)N=O |r|
Structure:
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