Target
Gastrin/cholecystokinin type B receptor
Ligand
BDBM85145
Substrate
n/a
Ki
10.96±n/a nM
Comments
PDSP_16
Citation
 Henke, BRAquino, CJBirkemo, LSCroom, DKDougherty, RWErvin, GNGrizzle, MKHirst, GCJames, MKJohnson, MFQueen, KLSherrill, RGSugg, EESuh, EMSzewczyk, JWUnwalla, RJYingling, JWillson, TM Optimization of 3-(1H-indazol-3-ylmethyl)-1,5-benzodiazepines as potent, orally active CCK-A agonists. J Med Chem 40:2706-25 (1997) [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:
BDBM85145
Synonyms:
CCK-A Agonist 15
Type:
Small organic molecule
Emp. Form.:
C36H34N4O4
Mol. Mass.:
586.6796
SMILES:
COc1ccc(cc1)N(C(C)C)C(=O)CN1c2ccccc2N(c2ccccc2)C(=O)C(Cc2c[nH]c3ccccc23)C1=O
Structure:
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