Target
Gastrin/cholecystokinin type B receptor
Ligand
BDBM50286113
Substrate
n/a
Meas. Tech.
ChEBML_47827
IC50
1.8±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:
BDBM50286113
Synonyms:
1-((2S,4R)-2-Methyl-6-phenyl-2,4-dihydro-1H-3,5,10b-triaza-benzo[e]azulen-4-yl)-3-m-tolyl-urea | CHEMBL103119
Type:
Small organic molecule
Emp. Form.:
C26H25N5O
Mol. Mass.:
423.5096
SMILES:
C[C@H]1CN2C(=N1)[C@H](NC(=O)Nc1cccc(C)c1)N=C(c1ccccc1)c1ccccc21 |c:4,t:20|
Structure:
Search PDB for entries with ligand similarity: