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Target
G-protein coupled bile acid receptor 1
Ligand
BDBM411181
Substrate
n/a
Meas. Tech.
cAMP Assay
EC50
36.0±n/a nM
Citation
 Bissantz, C; Dehmlow, H; Erickson, SD; Karnachi, PS; Kim, K; Martin, RE; Mattei, P; Sander, UO; Pietranico-Cole, SL; Richter, H; Ullmer, C 3-amino-pyridines as GPBAR1 agonists US Patent  US10385022 Publication Date 8/20/2019 
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:
BDBM411181
Synonyms:
N-Carbamoylmethyl-N-[4-(4-fluoro-2-methoxy-phenyl)-pyridin-3-yl]-2,6-bis-trifluoromethyl-isonicotinamide | US10385022, Example 177
Type:
Small organic molecule
Emp. Form.:
C22H15F7N4O3
Mol. Mass.:
516.3683
SMILES:
COc1cc(F)ccc1-c1ccncc1N(CC(N)=O)C(=O)c1cc(nc(c1)C(F)(F)F)C(F)(F)F
Structure:
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