dextromethorphan [Ligand Id: 6953] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL52440 (Dextromethorphan, Dimetane-DX)
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  • M2 receptor/Muscarinic acetylcholine receptor M2 in Rat [ChEMBL: CHEMBL309] [GtoPdb: 14] [UniProtKB: P10980]
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  • nicotinic acetylcholine receptor α3 subunit/nicotinic acetylcholine receptor β4 subunit/Neuronal acetylcholine receptor; alpha3/beta4 in Rat [ChEMBL: CHEMBL1907593] [GtoPdb: 464474] [UniProtKB: P04757P12392]
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  • SERT/Serotonin transporter in Human [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
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  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Rat [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9]
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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
GluN2D/GluN3B/GluN1/GluN2A/GluN2B/GluN2C/GluN3A/Glutamate [NMDA] receptor in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094124] [GtoPdb: 459461455456457458460] [UniProtKB: O15399O60391Q05586Q12879Q13224Q14957Q8TCU5]
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: 455456457458459461460] [UniProtKB: Q05586Q12879Q13224Q14957O15399O60391Q8TCU5]
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: 455456457458459461460] [UniProtKB: P35439Q00959Q00960Q00961Q62645Q8VHN2Q9R1M7]
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: 464474] [UniProtKB: P04757P12392]
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 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 B 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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]