Target
G-protein coupled bile acid receptor 1
Ligand
BDBM50428098
Substrate
n/a
Meas. Tech.
ChEMBL_943944 (CHEMBL2339911)
EC50
2430±n/a nM
Citation
 Piotrowski, DWFutatsugi, KWarmus, JSOrr, STFreeman-Cook, KDLondregan, ATWei, LJennings, SMHerr, MCoffey, SBJiao, WStorer, GHepworth, DWang, JLavergne, SYChin, JEHadcock, JRBrenner, MBWolford, ACJanssen, AMRoush, NSBuxton, JHinchey, TKalgutkar, ASSharma, RFlynn, DA Identification of Tetrahydropyrido[4,3-d]pyrimidine Amides as a New Class of Orally Bioavailable TGR5 Agonists. ACS Med Chem Lett 4:63-8 (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:
BDBM50428098
Synonyms:
CHEMBL2331647
Type:
Small organic molecule
Emp. Form.:
C20H25N5O3
Mol. Mass.:
383.4442
SMILES:
CCNc1nc2CCN(Cc2c(n1)C(N)=O)C(=O)CCc1ccc(OC)cc1
Structure:
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