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

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ChEMBL ligand: CHEMBL982 (ORF-11676, JF-1, Selincro, Nalmefene, SRD174, ORF 11676, Nalmetrene, SRD-174, JKB-121, ORF-1167, ORF 1167, Nalmefeno)
  • δ receptor/Delta-type opioid receptor in Human [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
  • δ receptor/Delta-type opioid receptor in Rat [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533]
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  • κ receptor/Kappa-type opioid receptor in Human [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
  • Kappa-type opioid receptor in Guinea pig [ChEMBL: CHEMBL3952] [UniProtKB: P41144]
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  • μ receptor/Mu-type opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
  • μ receptor/Mu-type 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-type 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]
ChEMBL Antagonist activity against human DOR expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation pretreated for 15 mins followed by forskolin addition measured after 30 mins by HitHunter cAMP assay F 6.9 pIC50 125.89 nM IC50 J Med Chem (2025) 68: 13057-13074 [PMID:40499097]
δ receptor/Delta-type 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-type 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]
ChEMBL Antagonist activity against human KOR expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation pretreated for 15 mins followed by forskolin addition measured after 30 mins by HitHunter cAMP assay F 5.12 pIC50 7600 nM IC50 J Med Chem (2025) 68: 13057-13074 [PMID:40499097]
ChEMBL Antagonist activity against human KOR expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation pretreated for 15 mins followed by forskolin addition measured after 30 mins by HitHunter cAMP assay F 8.1 pIC50 7.94 nM IC50 J Med Chem (2025) 68: 13057-13074 [PMID:40499097]
Kappa-type 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-type 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 Binding affinity to MOR (unknown origin) assessed as inhibition constant B 9.52 pKi 0.3 nM Ki J Med Chem (2024) 67: 603-619 [PMID:38156970]
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]
ChEMBL Antagonist activity against human MOR expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation pretreated for 15 mins followed by forskolin addition measured after 30 mins by HitHunter cAMP assay F 5.68 pIC50 2100 nM IC50 J Med Chem (2025) 68: 13057-13074 [PMID:40499097]
ChEMBL Antagonist activity against human MOR expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation pretreated for 15 mins followed by forskolin addition measured after 30 mins by HitHunter cAMP assay F 8.7 pIC50 2 nM IC50 J Med Chem (2025) 68: 13057-13074 [PMID:40499097]
μ receptor/Mu-type 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 37:

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]