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Target
Gastrin/cholecystokinin type B receptor
Ligand
BDBM85154
Substrate
n/a
Ki
1000±n/a nM
Comments
PDSP_6
Citation
Henke, BR; Aquino, CJ; Birkemo, LS; Croom, DK; Dougherty, RW; Ervin, GN; Grizzle, MK; Hirst, GC; James, MK; Johnson, MF; Queen, KL; Sherrill, RG; Sugg, EE; Suh, EM; Szewczyk, JW; Unwalla, RJ; Yingling, J; Willson, 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
More Info.:
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:
Human
Description:
Stable expression of human CCK-2 receptors in HEK 293 cells.
Residue:
447
Sequence:
MELLKLNRSVQGTGPGPGASLCRPGAPLLNSSSVGNLSCEPPRIRGAGTRELELAIRITLYAVIFLMSVGGNMLIIVVLGLSRRLRTVTNAFLLSLAVSDLLLAVACMPFTLLPNLMGTFIFGTVICKAVSYLMGVSVSVSTLSLVAIALERYSAICRPLQARVWQTRSHAARVIVATWLLSGLLMVPYPVYTVVQPVGPRVLQCVHRWPSARVRQTWSVLLLLLLFFIPGVVMAVAYGLISRELYLGLRFDGDSDSDSQSRVRNQGGLPGAVHQNGRCRPETGAVGEDSDGCYVQLPRSRPALELTALTAPGPGSGSRPTQAKLLAKKRVVRMLLVIVVLFFLCWLPVYSANTWRAFDGPGAHRALSGAPISFIHLLSYASACVNPLVYCFMHRRFRQACLETCARCCPRPPRARPRALPDEDPPTPSIASLSRLSYTTISTLGPG
Inhibitor
Name:
BDBM85154
Synonyms:
2,3,4,5-Tetrahydro-3-(1H-indazole-3-ylmethyl)-N-(4-methoxyphenyl)-N-(1-methylethyl)-2,4-dioxo-5-phenyl-1H-1,5-benzodiazepine-1-acetamide | CCK-A Agonist 1 | GW 5823 | GW-5823 | N-Isopropyl-N-(4-methoxyphenyl)-3-(1H-indazol-3-ylmethyl)-5-phenyl-2,4-dioxo-2,3,4,5-tetrahydro-1H-1,5-benzodiazepine-1-acetamide
Type:
Small organic molecule
Emp. Form.:
C35H33N5O4
Mol. Mass.:
587.6676
SMILES:
COc1ccc(cc1)N(C(C)C)C(=O)CN1c2ccccc2N(c2ccccc2)C(=O)C(Cc2n[nH]c3ccccc23)C1=O