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Target
Gastrin/cholecystokinin type B receptor
Ligand
BDBM50196157
Substrate
n/a
Meas. Tech.
ChEMBL_466361 (CHEMBL924691)
Ki
40±n/a nM
Citation
 Rosen, MD; Hack, MD; Allison, BD; Phuong, VK; Woods, CR; Morton, MF; Prendergast, CE; Barrett, TD; Schubert, C; Li, L; Wu, X; Wu, J; Freedman, JM; Shankley, NP; Rabinowitz, MH Discovery of potent cholecystokinin-2 receptor antagonists: elucidation of key pharmacophore elements by X-ray crystallographic and NMR conformational analysis. Bioorg Med Chem 16:3917-25 (2008) [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:
BDBM50196157
Synonyms:
1-[2-[(2,1,3-benzothiadiazol-4-ylsulfonyl)amino]-4-chlorobenzoyl]-piperidine | CHEMBL437908 | N-(5-chloro-2-(piperidine-1-carbonyl)phenyl)benzo[c][1,2,5]thiadiazole-4-sulfonamide
Type:
Small organic molecule
Emp. Form.:
C18H17ClN4O3S2
Mol. Mass.:
436.936
SMILES:
Clc1ccc(C(=O)N2CCCCC2)c(NS(=O)(=O)c2cccc3nsnc23)c1
Structure:
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