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Target
Cholecystokinin receptor type A
Ligand
BDBM50380731
Substrate
n/a
Meas. Tech.
ChEMBL_813376 (CHEMBL2019603)
IC50
68.6±n/a nM
Citation
 Cameron, KO; Beretta, EE; Chen, Y; Chu-Moyer, M; Fernando, D; Gao, H; Kohrt, J; Lavergne, S; Jardine, Pda S; Guzman-Perez, A; Hoth, C; Perry, DA; Hadcock, JR; Gautreau, D; Makowski, M; Perez, S; Polivkova, J; Rogers, L; Scott, DO; Swick, AG; Thiede, L; Trebino, CE; Trilles, RV; Wilmowski, J; Zhang, Y Discovery of new piperidine amide triazolobenzodiazepinones as intestinal-selective CCK1 receptor agonists. Bioorg Med Chem Lett 22:2943-7 (2012) [PubMed]  Article 
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:
BDBM50380731
Synonyms:
CHEMBL2017692
Type:
Small organic molecule
Emp. Form.:
C38H34N6O2
Mol. Mass.:
606.7156
SMILES:
O=C(CN1c2ccccc2-n2c(nnc2-c2ccccc2)C(Cc2c[nH]c3ccccc23)C1=O)N1CCC(Cc2ccccc2)C1
Structure:
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