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Target
G-protein coupled bile acid receptor 1
Ligand
BDBM50429131
Substrate
n/a
Meas. Tech.
ChEMBL_943575 (CHEMBL2343388)
EC50
>10000±n/a nM
Citation
 Londregan, AT; Piotrowski, DW; Futatsugi, K; Warmus, JS; Boehm, M; Carpino, PA; Chin, JE; Janssen, AM; Roush, NS; Buxton, J; Hinchey, T Discovery of 5-phenoxy-1,3-dimethyl-1H-pyrazole-4-carboxamides as potent agonists of TGR5 via sequential combinatorial libraries. Bioorg Med Chem Lett 23:1407-11 (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:
BDBM50429131
Synonyms:
CHEMBL2336229
Type:
Small organic molecule
Emp. Form.:
C19H16Cl2N4O2
Mol. Mass.:
403.262
SMILES:
Cc1nn(C)c(Oc2cccc(Cl)c2Cl)c1C(=O)N1Cc2cccnc2C1
Structure:
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