Ki Summary BindingDB logo
myBDB logout
Reaction Details
Report a problem with these data
TargetG-protein coupled bile acid receptor 1
LigandBDBM50429128
Substrate/Competitorn/a
Meas. Tech.ChEMBL_943575 (CHEMBL2343388)
EC50 0.300000±n/a nM
Citation Londregan, ATPiotrowski, DWFutatsugi, KWarmus, JSBoehm, MCarpino, PAChin, JEJanssen, AMRoush, NSBuxton, JHinchey, T Discovery of 5-phenoxy-1,3-dimethyl-1H-pyrazole-4-carboxamides as potent agonists of TGR5 via sequential combinatorial libraries. Bioorg Med Chem Lett23:1407-11 (2013) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
G-protein coupled bile acid receptor 1
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:
MTPNSTGEVPSPIPKGALGLSLALASLIITANLLLALGIAWDRRLRSPPAGCFFLSLLLA
GLLTGLALPTLPGLWNQSRRGYWSCLLVYLAPNFSFLSLLANLLLVHGERYMAVLRPLQP
PGSIRLALLLTWAGPLLFASLPALGWNHWTPGANCSSQAIFPAPYLYLEVYGLLLPAVGA
AAFLSVRVLATAHRQLQDICRLERAVCRDEPSALARALTWRQARAQAGAMLLFGLCWGPY
VATLLLSVLAYEQRPPLGPGTLLSLLSLGSASAAAVPVAMGLGDQRYTAPWRAAAQRCLQ
GLWGRASRDSPGPSIAYHPSSQSSVDLDLN
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50429128
n/a
NameBDBM50429128
Synonyms:CHEMBL2336232
TypeSmall organic molecule
Emp. Form.C21H22Cl2N4O2
Mol. Mass.433.331
SMILESCC(C)N(Cc1cccnc1)C(=O)c1c(C)nn(C)c1Oc1cccc(Cl)c1Cl
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least: