levorphanol [Ligand Id: 7595] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL592 (IDS-NL-007, RO 1-5431, Levorphanol)
  • Acetylcholinesterase in Electrophorus electricus [ChEMBL: CHEMBL4078] [UniProtKB: O42275]
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  • 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]
  • κ receptor/Kappa opioid receptor in Mouse [ChEMBL: CHEMBL4329] [GtoPdb: 318] [UniProtKB: P33534]
  • Kappa opioid receptor in Guinea pig [ChEMBL: CHEMBL3952] [UniProtKB: P41144]
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  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Mouse [ChEMBL: CHEMBL3465] [GtoPdb: 2552] [UniProtKB: O55242]
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  • Organic cation transporter 1/Solute carrier family 22 member 1 in Human [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Acetylcholinesterase in Electrophorus electricus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4078] [UniProtKB: O42275]
ChEMBL Inhibition of electric eel AChE by Ellman's method B 4.6 pKi 25000 nM Ki Bioorg. Med. Chem. (2010) 18: 5071-5080 [PMID:20580236]
δ receptor/Delta opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
ChEMBL Inhibition of [3H]naltrindole binding to opioid receptor delta 1 of Chinese hamster ovary membrane B 8.38 pKi 4.2 nM Ki J. Med. Chem. (2004) 47: 1886-1888 [PMID:15055988]
ChEMBL Inhibitory activity against Opioid receptor delta 1 in chinese Hamster Ovary (CHO) cell membranes was determined using [3H]naltrindole radioligand B 8.38 pKi 4.2 nM Ki J. Med. Chem. (2003) 46: 5162-5170 [PMID:14613319]
ChEMBL Binding affinity against opioid receptor delta 1 using [3H]naltrindole as radioligand in guinea pig brain membranes. B 8.38 pKi 4.2 nM Ki J. Med. Chem. (2004) 47: 165-174 [PMID:14695830]
ChEMBL Binding affinity towards Opioid receptor delta 1 in guinea pig brain membranes using [3H]naltrindole as radioligand B 8.38 pKi 4.2 nM Ki Bioorg. Med. Chem. Lett. (2001) 11: 2735-2740 [PMID:11591513]
ChEMBL Displacement of [3H]naltrindole from human delta opioid receptor expressed in CHO cells B 8.38 pKi 4.2 nM Ki J. Med. Chem. (2006) 49: 256-262 [PMID:16392810]
ChEMBL Displacement of [3H]naltrindole from human delta opioid receptors expressed in CHO cell membrane B 8.38 pKi 4.2 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 1508-1511 [PMID:17276685]
ChEMBL Displacement of [3H]Naltindole from human delta opioid receptor expressed in CHO cell membrane B 8.38 pKi 4.2 nM Ki Bioorg. Med. Chem. Lett. (2008) 18: 4474-4476 [PMID:18674902]
ChEMBL Displacement of [3H]-naltrindole from human delta opioid receptor expressed in CHO cells after 3 hrs by scintillation counting B 8.38 pKi 4.2 nM Ki J. Med. Chem. (2012) 55: 3878-3890 [PMID:22439881]
ChEMBL In vitro binding affinity against cloned human Opioid receptor delta 1 expressed in HEK 293S cells B 8.29 pIC50 5.1 nM IC50 J. Med. Chem. (2003) 46: 34-48 [PMID:12502358]
ChEMBL Inhibitory activity against opioid receptor delta of guinea pig was determined by using [3H]DADLE radioligand B 8.54 pIC50 2.9 nM IC50 J. Med. Chem. (1989) 32: 1259-1265 [PMID:2542556]
GluN2D/GluN3B/GluN1/GluN2A/GluN2B/GluN2C/GluN3A/Glutamate [NMDA] receptor in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094124] [GtoPdb: 459461455456457458460] [UniProtKB: O15399O60391Q05586Q12879Q13224Q14957Q8TCU5]
ChEMBL Inhibition of [3H]1 binding to dextromethorpin binding site of guinea pig microsomal pellet P3 N-methyl-D-aspartate glutamate receptor B 5.57 pIC50 2700 nM IC50 J. Med. Chem. (1992) 35: 4135-4142 [PMID:1433216]
ChEMBL Binding affinity against dextromethorpin binding site associated with N-methyl-D-aspartate glutamate receptor from guinea pig mitochondriall pellet P2 determined using [3H]1 as radioligand. B 5.6 pIC50 2500 nM IC50 J. Med. Chem. (1992) 35: 4135-4142 [PMID:1433216]
GtoPdb Measured vs. exogenously expressed zeta1/epsilon3 (GRIN1/GRIN2C) subunits, at pH 6.9 - 6.22 pIC50 601 nM IC50 J Physiol (Lond.) (2007) 581: 107-28 [PMID:17303642]
GluN1/GluN2A/GluN2B/GluN2C/GluN2D/GluN3B/GluN3A in Human [GtoPdb: 455456457458459461460] [UniProtKB: Q05586Q12879Q13224Q14957O15399O60391Q8TCU5]
GtoPdb Measured vs. exogenously expressed zeta1/epsilon3 (GRIN1/GRIN2C) subunits, at pH 6.9 - 6.22 pIC50 601 nM IC50 J Physiol (Lond.) (2007) 581: 107-28 [PMID:17303642]
GluN1/GluN2A/GluN2B/GluN2C/GluN2D/GluN3B/GluN3A/Glutamate NMDA receptor in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL1907608] [GtoPdb: 455456457458459461460] [UniProtKB: P35439Q00959Q00960Q00961Q62645Q8VHN2Q9R1M7]
ChEMBL Binding affinity against dextromethorpin binding site of N-methyl-D-aspartate glutamate receptor from rat brain using [3H]1 B 5.11 pIC50 7700 nM IC50 J. Med. Chem. (1992) 35: 4135-4142 [PMID:1433216]
ChEMBL Binding affinity against PCP binding site associated with N-methyl-D-aspartate glutamate receptor from rat synaptic plasma membrane(SPM) determined using [3H]TCP as radioligand. B 5.92 pIC50 1200 nM IC50 J. Med. Chem. (1992) 35: 4135-4142 [PMID:1433216]
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
ChEMBL Inhibition of [3H]U-69593 binding to Opioid receptor kappa 1 of Chinese hamster ovary membrane B 8.64 pKi 2.3 nM Ki J. Med. Chem. (2004) 47: 1886-1888 [PMID:15055988]
ChEMBL Inhibitory activity against Opioid receptor kappa 1 in chinese Hamster Ovary (CHO) cell membranes was determined using [3H]U-69593 radioligand B 8.64 pKi 2.3 nM Ki J. Med. Chem. (2003) 46: 5162-5170 [PMID:14613319]
ChEMBL Displacement of [3H]U69593 from human kappa opioid receptor expressed in CHO cells B 8.64 pKi 2.3 nM Ki J. Med. Chem. (2006) 49: 256-262 [PMID:16392810]
ChEMBL Displacement of [3H]U-69593 from human kappa opioid receptors expressed in CHO cell membrane B 8.64 pKi 2.3 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 1508-1511 [PMID:17276685]
ChEMBL Displacement of [3H]U69593 from human kappa opioid receptor expressed in CHO cell membrane B 8.64 pKi 2.3 nM Ki Bioorg. Med. Chem. Lett. (2008) 18: 4474-4476 [PMID:18674902]
ChEMBL Displacement of [3H]-U69,593 from human kappa opioid receptor expressed in CHO cells after 60 mins by scintillation counting B 8.64 pKi 2.3 nM Ki J. Med. Chem. (2012) 55: 3878-3890 [PMID:22439881]
ChEMBL In vitro binding affinity against cloned human Opioid receptor kappa 1 expressed in HEK 293S cells B 8.4 pIC50 4 nM IC50 J. Med. Chem. (2003) 46: 34-48 [PMID:12502358]
κ receptor/Kappa opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4329] [GtoPdb: 318] [UniProtKB: P33534]
ChEMBL Binding affinity for mouse opioid receptor kappa B 8 pKi 10 nM Ki J. Med. Chem. (1989) 32: 2221-2226 [PMID:2549247]
Kappa opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3952] [UniProtKB: P41144]
ChEMBL Binding affinity against opioid receptor kappa 1 using [3H]-U-69,593 as radioligand in guinea pig brain membranes. B 8.64 pKi 2.3 nM Ki J. Med. Chem. (2004) 47: 165-174 [PMID:14695830]
ChEMBL Binding affinity towards Opioid receptor kappa 1 in guinea pig brain membranes using [3H]U-69593 as radioligand B 8.64 pKi 2.3 nM Ki Bioorg. Med. Chem. Lett. (2001) 11: 2735-2740 [PMID:11591513]
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
ChEMBL Inhibition of [3H]-DAMGO binding to Opioid receptor mu 1 of Chinese hamster ovary membrane B 9.68 pKi 0.21 nM Ki J. Med. Chem. (2004) 47: 1886-1888 [PMID:15055988]
ChEMBL Inhibitory activity against Opioid receptor mu 1 in chinese Hamster Ovary (CHO) cells membranes was determined using [3H]-DAMGO radioligand B 9.68 pKi 0.21 nM Ki J. Med. Chem. (2003) 46: 5162-5170 [PMID:14613319]
ChEMBL Displacement of [3H]DAMGO from human mu opioid receptor expressed in CHO cells B 9.68 pKi 0.21 nM Ki J. Med. Chem. (2006) 49: 256-262 [PMID:16392810]
ChEMBL Displacement of [3H]DAMGO from human mu opioid receptors expressed in CHO cell membrane B 9.68 pKi 0.21 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 1508-1511 [PMID:17276685]
ChEMBL Displacement of [3H]DAMGO from human mu opioid receptor expressed in CHO cell membrane B 9.68 pKi 0.21 nM Ki Bioorg. Med. Chem. Lett. (2008) 18: 4474-4476 [PMID:18674902]
ChEMBL Displacement of [3H]-DAMGO from human mu opioid receptor expressed in CHO cells after 60 mins by scintillation counting B 9.68 pKi 0.21 nM Ki J. Med. Chem. (2012) 55: 3878-3890 [PMID:22439881]
ChEMBL In vitro binding affinity against cloned human Opioid receptor mu 1 expressed in HEK 293S cells B 9.89 pIC50 0.13 nM IC50 J. Med. Chem. (2003) 46: 34-48 [PMID:12502358]
GtoPdb - - 9.89 pIC50 0.13 nM IC50 J Med Chem (2003) 46: 34-48 [PMID:12502358]
μ receptor/Mu opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2858] [GtoPdb: 319] [UniProtKB: P42866]
ChEMBL Binding affinity for mouse opioid receptor mu B 9.52 pKi 0.3 nM Ki J. Med. Chem. (1989) 32: 2221-2226 [PMID:2549247]
ChEMBL Inhibitory potency against Opioid receptor mu 1 in mouse vas deferens assay F 6.56 pIC50 278 nM IC50 J. Med. Chem. (1982) 25: 1432-1438 [PMID:6296388]
Mu opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4354] [UniProtKB: P97266]
ChEMBL Binding affinity against opioid receptor mu 1 using [3H]DAMGO as radioligand in guinea pig brain membranes. B 9.68 pKi 0.21 nM Ki J. Med. Chem. (2004) 47: 165-174 [PMID:14695830]
ChEMBL Binding affinity towards Opioid receptor mu 1 in guinea pig brain membranes using [3H]DAMGO as radioligand B 9.68 pKi 0.21 nM Ki Bioorg. Med. Chem. Lett. (2001) 11: 2735-2740 [PMID:11591513]
ChEMBL Inhibitory potency against Opioid receptor mu 1 in the guinea pig ileum assay F 7.77 pIC50 17 nM IC50 J. Med. Chem. (1982) 25: 1432-1438 [PMID:6296388]
ChEMBL Inhibitory activity against opioid receptor mu of guinea pig brain using [3H]DAGO radioligand B 9.22 pIC50 0.6 nM IC50 J. Med. Chem. (1989) 32: 1259-1265 [PMID:2542556]
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3465] [GtoPdb: 2552] [UniProtKB: O55242]
ChEMBL Binding affinity for mouse sigma opioid receptor B 8.72 pKi 1.9 nM Ki J. Med. Chem. (1989) 32: 2221-2226 [PMID:2549247]
Organic cation transporter 1/Solute carrier family 22 member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245]
ChEMBL Inhibition of human OCT1 expressed in HEK293 cells assessed as reduction in ASP+ substrate uptake by microplate reader based analysis B 5.1 pIC50 8000 nM IC50 J Med Chem (2019) 62: 9890-9905 [PMID:31597043]

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, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]