Target
G-protein coupled bile acid receptor 1
Ligand
BDBM50327542
Substrate
n/a
Meas. Tech.
ChEMBL_664648 (CHEMBL1260362)
IC50
>10000±n/a nM
Citation
 Herbert, MRSiegel, DLStaszewski, LCayanan, CBanerjee, UDhamija, SAnderson, JFan, AWang, LRix, PShiau, AKRao, TSNoble, SAHeyman, RABischoff, EGuha, MKabakibi, APinkerton, AB Synthesis and SAR of 2-aryl-3-aminomethylquinolines as agonists of the bile acid receptor TGR5. Bioorg Med Chem Lett 20:5718-21 (2010) [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:
BDBM50327542
Synonyms:
2-(4-bromophenyl)-N-((6,7-dimethoxy-2-(thiophen-3-yl)quinolin-3-yl)methyl)ethanamine | CHEMBL1257733
Type:
Small organic molecule
Emp. Form.:
C24H23BrN2O2S
Mol. Mass.:
483.421
SMILES:
COc1cc2cc(CNCCc3ccc(Br)cc3)c(nc2cc1OC)-c1ccsc1
Structure:
Search PDB for entries with ligand similarity: