Reaction Details Report a problem with these data
Target
Cholecystokinin receptor type A
Ligand
BDBM50072425
Substrate
n/a
Meas. Tech.
ChEMBL_49894 (CHEMBL661736)
IC50
79±n/a nM
Citation
Aquino, CJ; Armour, DR; Berman, JM; Birkemo, LS; Carr, RA; Croom, DK; Dezube, M; Dougherty, RW; Ervin, GN; Grizzle, MK; Head, JE; Hirst, GC; James, MK; Johnson, MF; Miller, LJ; Queen, KL; Rimele, TJ; Smith, DN; Sugg, EE Discovery of 1,5-benzodiazepines with peripheral cholecystokinin (CCK-A) receptor agonist activity. 1. Optimization of the agonist"trigger". J Med Chem 39:562-9 (1996) [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:
BDBM50072425
Synonyms:
2-[2,4-Dioxo-5-phenyl-3-(3-phenyl-ureido)-2,3,4,5-tetrahydro-benzo[b][1,4]diazepin-1-yl]-N-isopropyl-N-(4-methoxy-phenyl)-acetamide | CHEMBL108130
Type:
Small organic molecule
Emp. Form.:
C34H33N5O5
Mol. Mass.:
591.6563
SMILES:
COc1ccc(cc1)N(C(C)C)C(=O)CN1c2ccccc2N(c2ccccc2)C(=O)C(NC(=O)Nc2ccccc2)C1=O