Target
Gastrin/cholecystokinin type B receptor
Ligand
BDBM50002901
Substrate
n/a
Meas. Tech.
ChEMBL_439002 (CHEMBL889348)
Ki
6±n/a nM
Citation
 McDonald, IMBlack, JWBuck, IMDunstone, DJGriffin, EPHarper, EAHull, RAKalindjian, SBLilley, EJLinney, IDPether, MJRoberts, SPShaxted, MESpencer, JSteel, KISykes, DAWalker, MKWatt, GFWright, LWright, PTXun, W Optimization of 1,3,4-benzotriazepine-based CCK(2) antagonists to obtain potent, orally active inhibitors of gastrin-mediated gastric acid secretion. J Med Chem 50:3101-12 (2007) [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:
BDBM50002901
Synonyms:
CHEMBL227277
Type:
Small organic molecule
Emp. Form.:
C32H37N5O5
Mol. Mass.:
571.6667
SMILES:
CC(C)(C)C(=O)CN1c2ccccc2C(=NN(CC(=O)Nc2cccc3n(CC(O)=O)ccc23)C1=O)C1CCCCC1 |c:15|
Structure:
Search PDB for entries with ligand similarity: