dextrorphan [Ligand Id: 9052] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1254766 (Levorphanol d-form, D-levorphanol, Dextro-dromoran, Dextrorphane, Ent-17-methylmorphinan-3-ol, Dextrorfano, Dextrorphan, RO-1-6794, RO 1-6794) |
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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 | 4.7 | pKi | 20000 | nM | Ki | Bioorg Med Chem (2010) 18: 5071-5080 [PMID:20580236] |
| CYP2D6/Cytochrome P450 2D6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL289] [GtoPdb: 1329] [UniProtKB: P10635] | ||||||||
| ChEMBL | Inhibition Assay: Six test compound concentrations (0.1, 0.25, 1, 2.5, 10, 25 μM in DMSO; final DMSO concentration=0.25%) are incubated with human liver microsomes (0.5 mg/mL) and NADPH (1 mM) in the presence of the probe substrate dextromethorphan (5 μM) for 5 mM at 37° C. The selective CYP2D6 inhibitor, quinidine, is screened alongside the test compounds as a positive control. | B | 4.75 | pIC50 | 17700 | nM | IC50 | US-9333197-B2. Apoptosis signal-regulating kinase inhibitor (2016) |
| ChEMBL | Inhibition Assay: Six test compound concentrations (0.1, 0.25, 1, 2.5, 10, 25 μM in DMSO; final DMSO concentration=0.25%) are incubated with human liver microsomes (0.5 mg/mL) and NADPH (1 mM) in the presence of the probe substrate dextromethorphan (5 μM) for 5 mM at 37° C. The selective CYP2D6 inhibitor, quinidine, is screened alongside the test compounds as a positive control. | B | 4.75 | pIC50 | 17700 | nM | IC50 | US-9333197-B2. Apoptosis signal-regulating kinase inhibitor (2016) |
| 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 | The compound was tested for its ability to block PCP N-methyl-D-aspartate glutamate receptor at the PCP (phencyclidine) binding site in postmortem human frontal cortex. | B | 6.66 | pKi | 220 | nM | Ki | J Med Chem (1998) 41: 393-400 [PMID:9464369] |
| GtoPdb | Measured vs. exogenously expressed zeta1/epsilon3 (GRIN1/GRIN2C) subunits, at pH 6.9 | - | 6.94 | pIC50 | 114 | nM | IC50 | J Physiol (Lond.) (2007) 581: 107-28 [PMID:17303642] |
| GluN1/GluN2A/Glutamate NMDA receptor; GRIN1/GRIN2A in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907604] [GtoPdb: 455, 456] [UniProtKB: Q05586, Q12879] | ||||||||
| ChEMBL | Antagonist activity at NR1/NR2A receptor (unknown origin) expressed in Xenopus laevis oocytes assessed as inhibition of glutamate/glycine-induced current at pH 7.6 at -40mV holding potential by two-electrode voltage-clamp electrophysiology | B | 5.89 | pIC50 | 1300 | nM | IC50 | Bioorg Med Chem (2014) 22: 1983-1992 [PMID:24630693] |
| ChEMBL | Inhibition of human GluN1/GluN2A NMDA receptor expressed in HEK293 cells assessed as reduction in glutamate induced current at -70 mV holding potential by whole-cell patch clamp technique | B | 6.55 | pIC50 | 280 | nM | IC50 | Eur J Med Chem (2025) 287: 117349-117349 [PMID:39952098] |
| GluN1/GluN2B/Glutamate NMDA receptor; GRIN1/GRIN2B in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907603] [GtoPdb: 455, 457] [UniProtKB: Q05586, Q13224] | ||||||||
| ChEMBL | Antagonist activity at NR1/2B receptor expressed in xenopus laevis at pH 6.9 by two electrode voltage clamp method | F | 6.61 | pIC50 | 246 | nM | IC50 | J Med Chem (2008) 51: 3765-3776 [PMID:18540667] |
| MRGPRX2/Mas-related G-protein coupled receptor member X2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5849] [GtoPdb: 157] [UniProtKB: Q96LB1] | ||||||||
| ChEMBL | Agonist activity at N-terminal Flag-tagged human MRGPRX2 receptor expressed in tetracycline-induced FLP-IN/T-REX 293 cells assessed as increase in intracellular calcium release by FLIPR assay | F | 5.22 | pEC50 | 6000 | nM | EC50 | Nat Chem Biol (2017) 13: 529-536 [PMID:28288109] |
| ChEMBL | Agonist activity at MRGPRX2 (unknown origin) expressed in HTLA cells assessed as induction of beta-arrestin 2 recruitment incubated for 18 to 24 hrs by PRESTO-Tango assay | F | 5.37 | pEC50 | 4300 | nM | EC50 | Nat Chem Biol (2017) 13: 529-536 [PMID:28288109] |
| ChEMBL | Agonist activity at MRGPRX2 (unknown origin) expressed in HTLA cells assessed as induction of beta-arrestin 2 recruitment incubated for 18 to 24 hrs by PRESTO-Tango assay | F | 5.38 | pEC50 | 4168.69 | nM | EC50 | Nat Chem Biol (2017) 13: 529-536 [PMID:28288109] |
| ChEMBL | Agonist activity at N-terminal Flag-tagged human MRGPRX2 receptor expressed in tetracycline-induced FLP-IN/T-REX 293 cells assessed as increase in intracellular calcium release by FLIPR assay | F | 5.41 | pEC50 | 3890.45 | nM | EC50 | Nat Chem Biol (2017) 13: 529-536 [PMID:28288109] |
| μ receptor/Mu-type opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
| ChEMBL | Agonist activity at human mu-opioid receptor stably expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated with compound for 10 mins followed by forskolin induction and measured after 30 mins by LANCE Ultra cAMP assay | F | 4.96 | pEC50 | 11000 | nM | EC50 | Eur J Med Chem (2025) 287: 117349-117349 [PMID:39952098] |
| NET/Sodium-dependent noradrenaline transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975] | ||||||||
| ChEMBL | Inhibition of human NET | B | 5.55 | pIC50 | 2840 | nM | IC50 | Eur J Med Chem (2025) 287: 117349-117349 [PMID:39952098] |
| 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 | 5.22 | pIC50 | 6000 | nM | IC50 | J Med Chem (2019) 62: 9890-9905 [PMID:31597043] |
ChEMBL data shown on this page come from version 37:
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]
