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 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]
