dextromethorphan [Ligand Id: 6953] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL52440 (Dextromethorphan, Dimetane-DX, NSC-751452) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 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 | 5.77 | pKi | 1680 | 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 | - | 6.33 | pIC50 | 466 | 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 | - | 6.33 | pIC50 | 466 | 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 | Displacement of [3H]MK801 from NMDA receptor in rat brain neuronal membrane | B | 5.34 | pKi | 4540 | nM | Ki | Bioorg Med Chem (2009) 17: 3456-3462 [PMID:19345586] |
| ChEMBL | Binding affinity was measured against phencyclidine (PCP) receptor in rat using [3H]TCP as radioligand | B | 5.65 | pKi | 2246 | nM | Ki | J Med Chem (1994) 37: 1964-1970 [PMID:8027978] |
| ChEMBL | Displacement of [3H]MK-801 from NMDA receptor in Wistar rat brain membranes by scintillation counting analysis | B | 5.88 | pIC50 | 1320 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 4131-4135 [PMID:26296478] |
| M2 receptor/Muscarinic acetylcholine receptor M2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL309] [GtoPdb: 14] [UniProtKB: P10980] | ||||||||
| ChEMBL | Binding affinity was measured against muscarinic (M2) receptor at 10 uM in rat using [3H]QN as radioligand | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1994) 37: 1964-1970 [PMID:8027978] |
| nicotinic acetylcholine receptor α3 subunit/nicotinic acetylcholine receptor β4 subunit/Neuronal acetylcholine receptor; alpha3/beta4 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907593] [GtoPdb: 464, 474] [UniProtKB: P04757, P12392] | ||||||||
| ChEMBL | Non-competitive inhibition of rat alpha3beta4 nAChR expressed in KX cells assessed as reduction in current by whole-cell patch clamp assay | B | 4.96 | pIC50 | 11050 | nM | IC50 | Bioorg Med Chem (2014) 22: 6846-6856 [PMID:25464883] |
| SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645] | ||||||||
| ChEMBL | DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) | B | 8.84 | pKi | 1.44 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) | B | 8.57 | pIC50 | 2.71 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| Sigma-1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4153] [UniProtKB: Q60492] | ||||||||
| ChEMBL | Displacement of [3H]-(+)-pentazocine from sigma-1 receptor in guinea pig brain membranes incubated for 1 hr by liquid scintillation counting method | B | 7.2 | pKi | 63 | nM | Ki | J Med Chem (2021) 64: 890-904 [PMID:33372782] |
| ChEMBL | Displacement of [3H]-(+)-pentazocine from sigma-1 receptor in guinea pig brain membranes incubated for 1 hr in presence of 250 uM phenytoin liquid scintillation counting method | B | 8 | pKi | 10 | nM | Ki | J Med Chem (2021) 64: 890-904 [PMID:33372782] |
| ChEMBL | Displacement of [3H]pentazocine from sigma1 receptor in guinea pig membrane | B | 6.63 | pIC50 | 232 | nM | IC50 | Bioorg Med Chem (2008) 16: 755-761 [PMID:18029187] |
| ChEMBL | Displacement of [3H]pentazocine from sigma1 receptor in guinea pig membrane in presence of phenytoin | B | 7.82 | pIC50 | 15.2 | nM | IC50 | Bioorg Med Chem (2008) 16: 755-761 [PMID:18029187] |
| sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720] | ||||||||
| GtoPdb | Sigma receptor cloned from Jurkat cells, identified as SIGMAR1. | - | 6.28 | pKi | 521 | nM | Ki | J Pharmacol Exp Ther (1999) 289: 251-60 [PMID:10087012] |
| ChEMBL | Inhibition of [3H](+)-pentazocine binding to Sigma receptor type 1 | B | 6.46 | pKi | 348 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 1807-1809 [PMID:15026077] |
| sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9] | ||||||||
| ChEMBL | Binding affinity was measured as selectivity for sigma-1 site over muscarinic (M1) receptor in rat | B | 5.29 | pKi | 5070 | nM | Ki | J Med Chem (1994) 37: 1964-1970 [PMID:8027978] |
| 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 | 4.82 | pIC50 | 15000 | nM | IC50 | J Med Chem (2019) 62: 9890-9905 [PMID:31597043] |
| ChEMBL | Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay | B | 4.98 | pIC50 | 10450 | nM | IC50 | J Med Chem (2017) 60: 2685-2696 [PMID:28230985] |
| TAS2R46/Taste receptor type 2 member 46 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523253] [GtoPdb: 679] [UniProtKB: P59540] | ||||||||
| ChEMBL | Agonist activity at human TAS2R46 stably expressed in HEK293T/Galpha16-gustducin 44 cells assessed as effect on calcium flux by measuring deltaF/F0 ratio by Fluo-4-AM dye based FLIPR assay | F | 4.51 | pEC50 | 31000 | nM | EC50 | US-8603762-B2. Methods to identify modulators of the interaction between dextromethorphan and the bitter taste receptor TAS2R46 (null) |
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]
