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Target
Gastrin/cholecystokinin type B receptor
Ligand
BDBM50061209
Substrate
n/a
Meas. Tech.
ChEMBL_47829 (CHEMBL662571)
IC50
>1000±n/a nM
Citation
 Selnick, HG; Liverton, NJ; Baldwin, JJ; Butcher, JW; Claremon, DA; Elliott, JM; Freidinger, RM; King, SA; Libby, BE; McIntyre, CJ; Pribush, DA; Remy, DC; Smith, GR; Tebben, AJ; Jurkiewicz, NK; Lynch, JJ; Salata, JJ; Sanguinetti, MC; Siegl, PK; Slaughter, DE; Vyas, K Class III antiarrhythmic activity in vivo by selective blockade of the slowly activating cardiac delayed rectifier potassium current IKs by (R)-2-(2,4-trifluoromethyl)-N-[2-oxo-5-phenyl-1-(2,2,2-trifluoroethyl)- 2, 3-dihydro-1H-benzo[e][1,4]diazepin-3-yl]acetamide. J Med Chem 40:3865-8 (1998) [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:
BDBM50061209
Synonyms:
2-(2,4-Bis-trifluoromethyl-phenyl)-N-[(R)-2-oxo-5-phenyl-1-(2,2,2-trifluoro-ethyl)-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl]-acetamide | CHEMBL16900 | L-768673
Type:
Small organic molecule
Emp. Form.:
C27H18F9N3O2
Mol. Mass.:
587.4363
SMILES:
FC(F)(F)CN1c2ccccc2C(=N[C@@H](NC(=O)Cc2ccc(cc2C(F)(F)F)C(F)(F)F)C1=O)c1ccccc1 |c:13|
Structure:
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