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Target
Gastrin/cholecystokinin type B receptor
Ligand
BDBM50019217
Substrate
n/a
Meas. Tech.
ChEBML_75463
IC50
>10000±n/a nM
Citation
 Evans, BE; Rittle, KE; Bock, MG; DiPardo, RM; Freidinger, RM; Whitter, WL; Lundell, GF; Veber, DF; Anderson, PS; Chang, RS Methods for drug discovery: development of potent, selective, orally effective cholecystokinin antagonists. J Med Chem 31:2235-46 (1989) [PubMed]  Article 
Target
Name:
Gastrin/cholecystokinin type B receptor
Synonyms:
CCK-2 receptor | CCK-B receptor | CCK-BR | CCKBR | CCKRB | Cholecystokinin A | Cholecystokinin receptor | Cholecystokinin-2 Receptor | GASR_HUMAN | Gastrin/cholecystokinin type B receptor
Type:
G Protein-Coupled Receptor (GPCR)
Mol. Mass.:
48445.79
Organism:
Homo sapiens (Human)
Description:
Stable expression of human CCK-2 receptors in HEK 293 cells.
Residue:
447
Sequence:
MELLKLNRSVQGTGPGPGASLCRPGAPLLNSSSVGNLSCEPPRIRGAGTRELELAIRITLYAVIFLMSVGGNMLIIVVLGLSRRLRTVTNAFLLSLAVSDLLLAVACMPFTLLPNLMGTFIFGTVICKAVSYLMGVSVSVSTLSLVAIALERYSAICRPLQARVWQTRSHAARVIVATWLLSGLLMVPYPVYTVVQPVGPRVLQCVHRWPSARVRQTWSVLLLLLLFFIPGVVMAVAYGLISRELYLGLRFDGDSDSDSQSRVRNQGGLPGAVHQNGRCRPETGAVGEDSDGCYVQLPRSRPALELTALTAPGPGSGSRPTQAKLLAKKRVVRMLLVIVVLFFLCWLPVYSANTWRAFDGPGAHRALSGAPISFIHLLSYASACVNPLVYCFMHRRFRQACLETCARCCPRPPRARPRALPDEDPPTPSIASLSRLSYTTISTLGPG
  
Inhibitor
Name:
BDBM50019217
Synonyms:
5-Fluoro-1H-indole-2-carboxylic acid [5-(2-fluoro-phenyl)-2-oxo-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl]-amide | 5-Fluoro-1H-indole-2-carboxylic acid [5-(2-fluoro-phenyl)-2-oxo-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl]-amide: 0.23CHCL3 | CHEMBL308111
Type:
Small organic molecule
Emp. Form.:
C24H16F2N4O2
Mol. Mass.:
430.4062
SMILES:
Fc1ccc2[nH]c(cc2c1)C(=O)NC1N=C(c2ccccc2F)c2ccccc2NC1=O |t:16|
Structure:
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