levorphanol [Ligand Id: 7595] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL592 (Aromarone, IDS-NL-007, Levorphan, Levorphanol, RO 1-5431) |
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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: 459, 461, 455, 456, 457, 458, 460] [UniProtKB: O15399, O60391, Q05586, Q12879, Q13224, Q14957, Q8TCU5] | ||||||||
| 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: 455, 456, 457, 458, 459, 461, 460] [UniProtKB: Q05586, Q12879, Q13224, Q14957, O15399, O60391, Q8TCU5] | ||||||||
| 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: 455, 456, 457, 458, 459, 461, 460] [UniProtKB: P35439, Q00959, Q00960, Q00961, Q62645, Q8VHN2, Q9R1M7] | ||||||||
| 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 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]
