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TargetG-protein coupled bile acid receptor 1
LigandBDBM50003568
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1335566
EC50 2.0±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:M-BAR | Membrane-type receptor for bile acids
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:
BDBM50003568
NameBDBM50003568
Synonyms:CHEMBL3234583
TypeSmall organic molecule
Emp. Form.C31H31F3N6O4
Mol. Mass.608.6108
SMILESOC(=O)Cc1ccc(OC2CCN(CC2)c2cc(nc(n2)C(F)(F)F)N2CC[C@H]2C(=O)NCCc2ccc(cc2)C#N)cc1 |r|
Structure
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