Reaction Details Report a problem with these data
Target
Cholecystokinin receptor type A
Ligand
BDBM50245181
Substrate
n/a
Meas. Tech.
ChEMBL_513418 (CHEMBL976505)
EC50
0.097±n/a nM
Citation
Berger, R; Zhu, C; Hansen, AR; Harper, B; Chen, Z; Holt, TG; Hubert, J; Lee, SJ; Pan, J; Qian, S; Reitman, ML; Strack, AM; Weingarth, DT; Wolff, M; Macneil, DJ; Weber, AE; Edmondson, SD 2-Substituted piperazine-derived imidazole carboxamides as potent and selective CCK1R agonists for the treatment of obesity. Bioorg Med Chem Lett 18:4833-7 (2008) [PubMed] Article
More Info.:
Target
Name:
Cholecystokinin receptor type A
Synonyms:
CCK-A receptor | CCK-AR | CCK1-R | CCKAR | CCKAR_HUMAN | CCKRA | Cholecystokinin receptor | Cholecystokinin receptor type A | Cholecystokinin-1 Receptor
Type:
G Protein-Coupled Receptor (GPCR)
Mol. Mass.:
47859.34
Organism:
Homo sapiens (Human)
Description:
Stable expression of human CCK-1 receptors in HEK 293 cells.
Residue:
428
Sequence:
MDVVDSLLVNGSNITPPCELGLENETLFCLDQPRPSKEWQPAVQILLYSLIFLLSVLGNTLVITVLIRNKRMRTVTNIFLLSLAVSDLMLCLFCMPFNLIPNLLKDFIFGSAVCKTTTYFMGTSVSVSTFNLVAISLERYGAICKPLQSRVWQTKSHALKVIAATWCLSFTIMTPYPIYSNLVPFTKNNNQTANMCRFLLPNDVMQQSWHTFLLLILFLIPGIVMMVAYGLISLELYQGIKFEASQKKSAKERKPSTTSSGKYEDSDGCYLQKTRPPRKLELRQLSTGSSSRANRIRSNSSAANLMAKKRVIRMLIVIVVLFFLCWMPIFSANAWRAYDTASAERRLSGTPISFILLLSYTSSCVNPIIYCFMNKRFRLGFMATFPCCPNPGPPGARGEVGEEEEGGTTGASLSRFSYSHMSASVPPQ
Inhibitor
Name:
BDBM50245181
Synonyms:
3-((R)-3-((carboxymethoxy)methyl)-4-(1-(3-ethoxyphenyl)-2-p-tolyl-1H-imidazole-4-carbonyl)piperazin-1-yl)-1-naphthoic acid | CHEMBL508772
Type:
Small organic molecule
Emp. Form.:
C37H36N4O7
Mol. Mass.:
648.7043
SMILES:
CCOc1cccc(c1)-n1cc(nc1-c1ccc(C)cc1)C(=O)N1CCN(C[C@@H]1COCC(O)=O)c1cc(C(O)=O)c2ccccc2c1 |r|