nalorphine [Ligand Id: 1629] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL415284 (Nalorphine)
  • δ receptor/Delta opioid receptor in Human [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
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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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  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
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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 Displacement of [3H]Naltrindole form human delta opioid receptor expressed in CHO cells B 6.92 pKi 120 nM Ki Bioorg. Med. Chem. Lett. (2009) 19: 203-208 [PMID:19027293]
GtoPdb - - 7.4 pKi - - - NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407]
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
ChEMBL Binding affinity to human kappa opioid receptor B 8.7 pKi 2 nM Ki J. Med. Chem. (2016) 59: 810-840 [PMID:26390077]
GtoPdb - - 9.1 pKi - - - NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407];
J Pharmacol Exp Ther (1997) 282: 676-84 [PMID:9262330]
ChEMBL Displacement of [3H]U69593 form human kappa opioid receptor expressed in CHO cells B 9.42 pKi 0.38 nM Ki Bioorg. Med. Chem. Lett. (2009) 19: 203-208 [PMID:19027293]
Kappa opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3952] [UniProtKB: P41144]
ChEMBL Binding affinity to Opioid receptor kappa 1 in guinea pig cortex using [3H]EKC as radioligand B 7.82 pKi 15 nM Ki J. Med. Chem. (1988) 31: 555-560 [PMID:2831363]
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
GtoPdb - - 8.9 pKi - - - NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407]
ChEMBL Binding affinity to human mu opioid receptor B 9.44 pKi 0.36 nM Ki J. Med. Chem. (2016) 59: 810-840 [PMID:26390077]
ChEMBL Displacement of [3H]DAMGO form human mu opioid receptor expressed in CHO cells B 9.72 pKi 0.19 nM Ki Bioorg. Med. Chem. Lett. (2009) 19: 203-208 [PMID:19027293]
μ receptor/Mu opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535]
ChEMBL Binding affinity to Opioid receptor mu 1 in rat brain using [3H]-NAL as radioligand B 8.19 pKi 6.5 nM Ki J. Med. Chem. (1988) 31: 555-560 [PMID:2831363]
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
ChEMBL Inhibition of specific binding of [125I]-PIPAG to sigma binding site in Guinea pig brain membranes B 5.3 pIC50 5000 nM IC50 J. Med. Chem. (1992) 35: 4683-4689 [PMID:1469697]
ChEMBL Inhibition of specific binding of [3H]DTG to sigma binding site in Guinea pig brain membranes B 5.4 pIC50 4000 nM IC50 J. Med. Chem. (1992) 35: 4683-4689 [PMID:1469697]
ChEMBL Inhibition of specific binding of [3H]3-PPP to sigma binding site in Guinea pig brain membranes B 5.55 pIC50 2850 nM IC50 J. Med. Chem. (1992) 35: 4683-4689 [PMID:1469697]
ChEMBL Inhibition of specific binding of [3H]NANM of sigma binding site in Guinea pig brain membranes B 5.74 pIC50 1800 nM IC50 J. Med. Chem. (1992) 35: 4683-4689 [PMID:1469697]
ChEMBL Inhibition of specific binding of [125I]PIPAG to sigma receptor in Guinea pig brain membranes B 6.13 pIC50 735 nM IC50 J. Med. Chem. (1992) 35: 4683-4689 [PMID:1469697]
ChEMBL Inhibition of specific binding of [3H]DTG to sigma receptor in Guinea pig brain membranes B 6.2 pIC50 625 nM IC50 J. Med. Chem. (1992) 35: 4683-4689 [PMID:1469697]
ChEMBL Inhibition of specific binding of [3H]3-PPP to sigma receptor in Guinea pig brain membranes B 7.03 pIC50 93 nM IC50 J. Med. Chem. (1992) 35: 4683-4689 [PMID:1469697]
ChEMBL Inhibition of specific binding of [3H]NANM of sigma receptor in Guinea pig brain membranes B 7.32 pIC50 48 nM IC50 J. Med. Chem. (1992) 35: 4683-4689 [PMID:1469697]

ChEMBL data shown on this page come from version 28:

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]