Target
G-protein coupled bile acid receptor 1
Ligand
BDBM50081124
Substrate
n/a
Meas. Tech.
ChEMBL_1475559 (CHEMBL3424620)
EC50
3800±n/a nM
Citation
 Duan, HNing, MZou, QYe, YFeng, YZhang, LLeng, YShen, J Discovery of Intestinal Targeted TGR5 Agonists for the Treatment of Type 2 Diabetes. J Med Chem 58:3315-28 (2015) [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:
BDBM50081124
Synonyms:
CHEMBL3421893
Type:
Small organic molecule
Emp. Form.:
C28H27Cl2N3O4
Mol. Mass.:
540.438
SMILES:
CCOC(=O)CCc1cc(Cl)c(Oc2ccncc2C(=O)N2CCN(C3CC3)c3ccccc23)cc1Cl
Structure:
Search PDB for entries with ligand similarity: