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TargetG-protein coupled bile acid receptor 1
LigandBDBM50003310
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1335566 (CHEMBL3239421)
EC50 120±n/a nM
Citation Phillips, DPGao, WYang, YZhang, GLerario, IKLau, TLJiang, JWang, XNguyen, DGBhat, BGTrotter, CSullivan, HWelzel, GLandry, JChen, YJoseph, SBLi, CGordon, WPRichmond, WJohnson, KBretz, ABursulaya, BPan, SMcNamara, PSeidel, HM Discovery of trifluoromethyl(pyrimidin-2-yl)azetidine-2-carboxamides as potent, orally bioavailable TGR5 (GPBAR1) agonists: structure-activity relationships, lead optimization, and chronic in vivo efficacy. J Med Chem57:3263-82 (2014) [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:GPBAR_MOUSE | Gpbar1 | M-BAR | Membrane-type receptor for bile acids | Tgr5
Type:PROTEIN
Mol. Mass.:35665.78
Organism:Mus musculus
Description:ChEMBL_1475560
Residue:329
Sequence:
MMTPNSTELSAIPMGVLGLSLALASLIVIANLLLALGIALDRHLRSPPAGCFFLSLLLAG
LLTGLALPMLPGLWSRNHQGYWSCLLLHLTPNFCFLSLLANLLLVHGERYMAVLQPLRPH
GSVRLALFLTWVSSLFFASLPALGWNHWSPDANCSSQAVFPAPYLYLEVYGLLLPAVGAT
ALLSVRVLATAHRQLCEIRRLERAVCRDVPSTLARALTWRQARAQAGATLLFLLCWGPYV
ATLLLSVLAYERRPPLGPGTLLSLISLGSTSAAAVPVAMGLGDQRYTAPWRTAAQRCLRV
LRGRAKRDNPGPSTAYHTSSQCSIDLDLN
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  Blast E-value cutoff:
BDBM50003310
n/a
NameBDBM50003310
Synonyms:CHEMBL3234558
TypeSmall organic molecule
Emp. Form.C19H23ClN4O
Mol. Mass.358.865
SMILESCc1nccc(n1)N1CCC[C@H](C1)C(=O)NCCc1ccc(Cl)cc1 |r|
Structure
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