Target
Gastrin/cholecystokinin type B receptor
Ligand
BDBM50019187
Substrate
n/a
Meas. Tech.
ChEBML_75463
IC50
190±n/a nM
Citation
 Evans, BERittle, KEBock, MGDiPardo, RMFreidinger, RMWhitter, WLLundell, GFVeber, DFAnderson, PSChang, 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:
BDBM50019187
Synonyms:
(R)-1H-Indole-2-carboxylic acid [5-(2-fluoro-phenyl)-1-methyl-2-oxo-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl]-amide: 0.1C4H10O | (S)-1H-Indole-2-carboxylic acid [5-(2-fluoro-phenyl)-1-methyl-2-oxo-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl]-amide: 0.2C4H10O | 1H-Indole-2-carboxylic acid [5-(2-fluoro-phenyl)-1-methyl-2-oxo-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl]-amide | 1H-Indole-2-carboxylic acid [5-(2-fluoro-phenyl)-1-methyl-2-oxo-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl]-amide: 0.75CH2Cl2. 0.5C4H10O | CHEMBL73522
Type:
Small organic molecule
Emp. Form.:
C25H19FN4O2
Mol. Mass.:
426.4424
SMILES:
CN1c2ccccc2C(=NC(NC(=O)c2cc3ccccc3[nH]2)C1=O)c1ccccc1F |c:9|
Structure:
Search PDB for entries with ligand similarity: