nalmefene [Ligand Id: 1628] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL982 (JF-1, JKB-121, Nalmefene, Nalmetrene, ORF 1167, ORF-1167, ORF 11676, ORF-11676, Revex, Selincro, SRD-174, SRD174)
  • δ receptor/Delta opioid receptor in Human [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
  • δ receptor/Delta opioid receptor in Rat [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533]
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  • κ receptor/Kappa opioid receptor in Human [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
  • Kappa opioid receptor in Guinea pig [ChEMBL: CHEMBL3952] [UniProtKB: P41144]
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  • μ receptor/Mu opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
  • μ receptor/Mu opioid receptor in Rat [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
δ receptor/Delta opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
ChEMBL Activity at human delta opioid receptor by [35S]GTPgammaS binding assay F 9.04 pKd 0.91 nM Kd J Med Chem (2008) 51: 1913-1924 [PMID:18298057]
ChEMBL Displacement of [3H]naltrindole from human delta-opioid receptor expressed in CHO cell membranes after 3 hrs by scintillation counting B 7.8 pKi 16 nM Ki J Med Chem (2016) 59: 8712-8756 [PMID:27299736]
ChEMBL Displacement of [3H]DPDPE from human delta opioid receptor expressed in CHO cells B 7.88 pKi 13.26 nM Ki J Med Chem (2008) 51: 1913-1924 [PMID:18298057]
ChEMBL Displacement of [3H]DPDPE from delta opioid receptor expressed in HEK293 cells by visible spectrophotometry B 7.88 pKi 13.26 nM Ki Bioorg Med Chem (2009) 17: 6671-6681 [PMID:19683449]
ChEMBL Displacement of [3H]Naltrindole form human delta opioid receptor expressed in CHO cells B 8.03 pKi 9.3 nM Ki Bioorg Med Chem Lett (2009) 19: 203-208 [PMID:19027293]
GtoPdb - - 8.1 pKi - - - NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407]
δ receptor/Delta opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533]
ChEMBL Binding affinity towards delta-opioid receptor by displacement of [3H]DADL in rat brain homogenates B 8.47 pKi 3.4 nM Ki J Med Chem (1993) 36: 2842-2850 [PMID:8410999]
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
ChEMBL Displacement of [3H]U69593 from human kappa opioid receptor expressed in CHO cells B 8.99 pKi 1.03 nM Ki J Med Chem (2008) 51: 1913-1924 [PMID:18298057]
ChEMBL Displacement of [3H]U69593 from kappa opioid receptor expressed in HEK293 cells by visible spectrophotometry B 8.99 pKi 1.03 nM Ki Bioorg Med Chem (2009) 17: 6671-6681 [PMID:19683449]
GtoPdb - - 9.5 pKi - - - NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407]
ChEMBL Displacement of [3H]U69593 form human kappa opioid receptor expressed in CHO cells B 9.92 pKi 0.12 nM Ki Bioorg Med Chem Lett (2009) 19: 203-208 [PMID:19027293]
ChEMBL Displacement of [3H]U69,593 from human kappa-opioid receptor expressed in CHO cell membranes after 60 mins by scintillation counting B 10.08 pKi 0.08 nM Ki J Med Chem (2016) 59: 8712-8756 [PMID:27299736]
Kappa opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3952] [UniProtKB: P41144]
ChEMBL Binding affinity towards kappa opioid receptor by displacement of [3H]EKC in guinea pig cortical tissue B 8.7 pKi 2 nM Ki J Med Chem (1993) 36: 2842-2850 [PMID:8410999]
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
ChEMBL Activity at human mu opioid receptor by [35S]GTPgammaS binding assay F 9.53 pKd 0.3 nM Kd J Med Chem (2008) 51: 1913-1924 [PMID:18298057]
ChEMBL Displacement of [3H]DAMGO from human mu opioid receptor expressed in CHO cells B 9.04 pKi 0.91 nM Ki J Med Chem (2008) 51: 1913-1924 [PMID:18298057]
ChEMBL Displacement of [3H]DAMGO from mu opioid receptor expressed in HEK293 cells by visible spectrophotometry B 9.04 pKi 0.91 nM Ki Bioorg Med Chem (2009) 17: 6671-6681 [PMID:19683449]
ChEMBL Displacement of [3H]DAMGO form human mu opioid receptor expressed in CHO cells B 9.36 pKi 0.44 nM Ki Bioorg Med Chem Lett (2009) 19: 203-208 [PMID:19027293]
GtoPdb - - 9.5 pKi - - - NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407]
ChEMBL Displacement of [3H]DAMGO from human mu-opioid receptor expressed in CHO cell membranes after 60 mins by scintillation counting B 9.62 pKi 0.24 nM Ki J Med Chem (2016) 59: 8712-8756 [PMID:27299736]
μ receptor/Mu opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535]
ChEMBL Binding affinity towards mu-opioid receptor by the displacement of [3H]Nal in rat brain homogenates B 9.54 pKi 0.29 nM Ki J Med Chem (1993) 36: 2842-2850 [PMID:8410999]

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]