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

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL52440 (Dextromethorphan, Dimetane-DX)
1 CHEMBL52440_lig_chart_1 Glutamate [NMDA] receptor Human
There should be some charts here, you may need to enable JavaScript!
2 CHEMBL52440_lig_chart_2 GluN1/GluN2A/GluN2B/GluN2C/GluN2D/GluN3B/GluN3A HumanRat
There should be some charts here, you may need to enable JavaScript!
  • M2 receptor/Muscarinic acetylcholine receptor M2 in Rat [ChEMBL: CHEMBL309] [GtoPdb: 14] [UniProtKB: P10980]
  • This target only has 1 pki data point
  • 5
3 CHEMBL52440_lig_chart_3 Muscarinic acetylcholine receptor M2 Rat
There should be some charts here, you may need to enable JavaScript!
  • nicotinic acetylcholine receptor α3 subunit/nicotinic acetylcholine receptor β4 subunit/Neuronal acetylcholine receptor; alpha3/beta4 in Rat [ChEMBL: CHEMBL1907593] [GtoPdb: 464474] [UniProtKB: P04757P12392]
  • This target only has 0 pki data point
  • 0
4 CHEMBL52440_lig_chart_4 Neuronal acetylcholine receptor; alpha3/beta4 Rat
There should be some charts here, you may need to enable JavaScript!
  • SERT/Serotonin transporter in Human [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
  • This target only has 1 pki data point
  • 8.84
5 CHEMBL52440_lig_chart_5 Serotonin transporter Human
There should be some charts here, you may need to enable JavaScript!
  • Sigma-1 receptor in Guinea pig [ChEMBL: CHEMBL4153] [UniProtKB: Q60492]
  • This target only has 0 pki data point
  • 0
6 CHEMBL52440_lig_chart_6 Sigma-1 receptor Guinea pig
There should be some charts here, you may need to enable JavaScript!
  • 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]
  • 5.29
7 CHEMBL52440_lig_chart_7 Sigma opioid receptor HumanRat
There should be some charts here, you may need to enable JavaScript!
  • Organic cation transporter 1/Solute carrier family 22 member 1 in Human [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245]
  • This target only has 0 pki data point
  • 0
8 CHEMBL52440_lig_chart_8 Solute carrier family 22 member 1 Human
There should be some charts here, you may need to enable JavaScript!
  • TAS2R46/Taste receptor type 2 member 46 in Human [ChEMBL: CHEMBL4523253] [GtoPdb: 679] [UniProtKB: P59540]
  • This target only has 0 pki data point
  • 0
9 CHEMBL52440_lig_chart_9 Taste receptor type 2 member 46 Human
There should be some charts here, you may need to enable JavaScript!
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]