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Target
Cholecystokinin receptor type A
Ligand
BDBM50329178
Substrate
n/a
Meas. Tech.
ChEMBL_674626 (CHEMBL1273773)
EC50
63.8±n/a nM
Citation
Elliott, RL; Cameron, KO; Chin, JE; Bartlett, JA; Beretta, EE; Chen, Y; Jardine, Pda S; Dubins, JS; Gillaspy, ML; Hargrove, DM; Kalgutkar, AS; LaFlamme, JA; Lame, ME; Martin, KA; Maurer, TS; Nardone, NA; Oliver, RM; Scott, DO; Sun, D; Swick, AG; Trebino, CE; Zhang, Y Discovery of N-benzyl-2-[(4S)-4-(1H-indol-3-ylmethyl)-5-oxo-1-phenyl-4,5-dihydro-6H-[1,2,4]triazolo[4,3-a][1,5]benzodiazepin-6-yl]-N-isopropylacetamide, an orally active, gut-selective CCK1 receptor agonist for the potential treatment of obesity. Bioorg Med Chem Lett 20:6797-801 (2010) [PubMed] Article
More Info.:
Target
Name:
Cholecystokinin receptor type A
Synonyms:
CCKAR_RAT | Cckar | Cholecystokinin peripheral | Cholecystokinin receptor | Cholecystokinin receptor type A
Type:
Enzyme Catalytic Domain
Mol. Mass.:
49676.37
Organism:
RAT
Description:
Cholecystokinin central 0 RAT::P30551
Residue:
444
Sequence:
MSHSPARQHLVESSRMDVVDSLLMNGSNITPPCELGLENETLFCLDQPQPSKEWQSALQILLYSIIFLLSVLGNTLVITVLIRNKRMRTVTNIFLLSLAVSDLMLCLFCMPFNLIPNLLKDFIFGSAVCKTTTYFMGTSVSVSTFNLVAISLERYGAICRPLQSRVWQTKSHALKVIAATWCLSFTIMTPYPIYSNLVPFTKNNNQTANMCRFLLPSDAMQQSWQTFLLLILFLLPGIVMVVAYGLISLELYQGIKFDASQKKSAKEKKPSTGSSTRYEDSDGCYLQKSRPPRKLELQQLSSGSGGSRLNRIRSSSSAANLIAKKRVIRMLIVIVVLFFLCWMPIFSANAWRAYDTVSAEKHLSGTPISFILLLSYTSSCVNPIIYCFMNKRFRLGFMATFPCCPNPGPPGVRGEVGEEEDGRTIRALLSRYSYSHMSTSAPPP
Inhibitor
Name:
BDBM50329178
Synonyms:
(S)-3-(3-(1-(2-(isopropyl(phenyl)amino)-2-oxoethyl)-2,4-dioxo-5-phenyl-2,3,4,5-tetrahydro-1H-benzo[b][1,4]diazepin-3-yl)ureido)benzoic acid | CHEMBL1269257
Type:
Small organic molecule
Emp. Form.:
C34H31N5O6
Mol. Mass.:
605.6398
SMILES:
CC(C)N(C(=O)CN1c2ccccc2N(c2ccccc2)C(=O)[C@@H](NC(=O)Nc2cccc(c2)C(O)=O)C1=O)c1ccccc1 |r|