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 USA (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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]