ICI 204448 [Ligand Id: 1650] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL23472 (ICI-204448)
  • κ receptor/Kappa opioid receptor in Human [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
  • κ receptor in Mouse [GtoPdb: 318] [UniProtKB: P33534]
  • κ receptor in Rat [GtoPdb: 318] [UniProtKB: P34975]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
ChEMBL Displacement of bound [3H]diprenorphine from membranes expressing cloned human kappa opioid receptor B 8.57 pKi 2.69 nM Ki Bioorg. Med. Chem. Lett. (2005) 15: 1091-1095 [PMID:15686919]
ChEMBL Agonistic activity at kappa opioid receptor of rabbit vas deferens F 8.13 pIC50 7.4 nM IC50 Bioorg. Med. Chem. Lett. (1992) 2: 1275-1278
κ receptor in Mouse [GtoPdb: 318] [UniProtKB: P33534]
GtoPdb - - 8.2 pIC50 - - - Proc. Natl. Acad. Sci. U.S.A. (1993) 90: 6736-40 [PMID:8393575]
κ receptor in Rat [GtoPdb: 318] [UniProtKB: P34975]
GtoPdb - - 8.8 pKi - - - Biochem. J. (1993) 295 ( Pt 3): 625-8 [PMID:8240267]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]