Target
Gastrin/cholecystokinin type B receptor
Ligand
BDBM50286120
Substrate
n/a
Meas. Tech.
ChEBML_47827
IC50
12±n/a nM
Citation
 Showell, GABourrain, SFletcher, SRNeduvelil, JGFletcher, AEFreedman, SBPatel, SSmith, AJMarshall, GRGraham, MISohal, BMatassa, VG C5-piperazinyl-1,4-benzodiazepines, water-soluble, orally bioa vailable CCKB/gastrin receptor antagonists Bioorg Med Chem Lett 5:3023-3026 (1995)    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:
BDBM50286120
Synonyms:
1-[5-(4-Methyl-piperazin-1-yl)-2-oxo-1-propyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl]-3-(3-trifluoromethyl-phenyl)-urea | CHEMBL105273
Type:
Small organic molecule
Emp. Form.:
C25H29F3N6O2
Mol. Mass.:
502.532
SMILES:
CCCN1c2ccccc2C(=NC(NC(=O)Nc2cccc(c2)C(F)(F)F)C1=O)N1CCN(C)CC1 |c:11|
Structure:
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