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Target
Cholecystokinin receptor type A
Ligand
BDBM50329179
Substrate
n/a
Meas. Tech.
ChEMBL_674626 (CHEMBL1273773)
EC50
445.8±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 
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:
BDBM50329179
Synonyms:
2-((4S)-4-((1H-indol-3-yl)methyl)-5-oxo-1-phenyl-4H-benzo[b][1,2,4]triazolo[4,3-d][1,4]diazepin-6(5H)-yl)-N-benzyl-N-isopropylacetamide | CHEMBL1269258
Type:
Small organic molecule
Emp. Form.:
C37H34N6O2
Mol. Mass.:
594.7049
SMILES:
CC(C)N(Cc1ccccc1)C(=O)CN1c2ccccc2-n2c(nnc2-c2ccccc2)[C@H](Cc2c[nH]c3ccccc23)C1=O |r|
Structure:
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