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

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ChEMBL ligand: CHEMBL982 (JF-1, JKB-121, Nalmefene, Nalmefene hydrochloride dihydrate, Nalmefene hydrochloride hydrate, 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 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]