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Target
Gastrin/cholecystokinin type B receptor
Ligand
BDBM50059319
Substrate
n/a
Meas. Tech.
ChEMBL_47982 (CHEMBL657484)
IC50
0.1±n/a nM
Citation
 Castro, JL; Broughton, HB; Russell, MG; Rathbone, D; Watt, AP; Ball, RG; Chapman, KL; Patel, S; Smith, AJ; Marshall, GR; Matassa, VG 5-(Piperidin-2-yl)- and 5-(homopiperidin-2-yl)-1,4-benzodiazepines: high-affinity, basic ligands for the cholecystokinin-B receptor. J Med Chem 40:2491-501 (1997) [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:
BDBM50059319
Synonyms:
1-[(R)-5-(3-Aza-bicyclo[3.2.2]non-3-yl)-1-methyl-2-oxo-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl]-3-m-tolyl-urea | CHEMBL420783
Type:
Small organic molecule
Emp. Form.:
C26H31N5O2
Mol. Mass.:
445.5566
SMILES:
CN1c2ccccc2C(=N[C@@H](NC(=O)Nc2cccc(C)c2)C1=O)N1CC2CCC(CC2)C1 |wD:10.11,c:9,(-1.99,-1.96,;-1.66,-3.47,;-2.84,-4.41,;-4.17,-3.64,;-5.52,-4.43,;-5.52,-5.95,;-4.17,-6.72,;-2.84,-5.95,;-1.66,-6.91,;-.15,-6.56,;.51,-5.2,;2.05,-5.21,;2.83,-3.88,;2.06,-2.55,;4.37,-3.89,;5.14,-2.55,;6.71,-2.55,;7.48,-1.22,;6.68,.13,;5.14,.13,;4.41,1.5,;4.37,-1.22,;-.15,-3.8,;.81,-2.6,;-1.85,-8.42,;-3.34,-8.83,;-3.98,-9.96,;-3.36,-11.34,;-1.82,-11.66,;-.6,-10.63,;-2.5,-11.08,;-2.5,-9.54,;-.71,-9.12,)|
Structure:
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