ChEMBL ligand: CHEMBL52440 (Dextromethorphan, Dextromethorphane, Dextrometorfano, Dimetane-DX, NSC-751452)
GluN2D/GluN3B/GluN1/GluN2A/GluN2B/GluN2C/GluN3A/Glutamate [NMDA] receptor in Human [ChEMBL: CHEMBL2094124] [GtoPdb: 459, 461, 455, 456, 457, 458, 460] [UniProtKB: O15399, O60391, Q05586, Q12879, Q13224, Q14957, Q8TCU5] There should be some charts here, you may need to enable JavaScript!
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] GluN1/GluN2A/GluN2B/GluN2C/GluN2D/GluN3B/GluN3A/Glutamate NMDA receptor in Rat [ChEMBL: CHEMBL1907608] [GtoPdb: 455, 456, 457, 458, 459, 461, 460] [UniProtKB: P35439, Q00959, Q00960, Q00961, Q62645, Q8VHN2, Q9R1M7] 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] 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: 464, 474] [UniProtKB: P04757, P12392] There should be some charts here, you may need to enable JavaScript!
SERT/Serotonin transporter in Human [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645] There should be some charts here, you may need to enable JavaScript!
Sigma-1 receptor in Guinea pig [ChEMBL: CHEMBL4153] [UniProtKB: Q60492] 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] 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] 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] 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: 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 (2013)

ChEMBL data shown on this page come from version 34:

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]