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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB (change energy unit to kcal/mol)

Found 55 hits in this display   

TargetSigma non-opioid intracellular receptor 1(Cavia porcellus (Guinea pig))
The State University Of New Jersey

Curated by ChEMBL
LigandPNGBDBM50366613(DEXTROMETHORPHAN)
Affinity DataKi:  10nMAssay Description:Displacement of [3H]-(+)-pentazocine from sigma-1 receptor in guinea pig brain membranes incubated for 1 hr in presence of 250 uM phenytoin liquid sc...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMu-type opioid receptor(Rattus norvegicus (rat))
R. W. Johnson Pharmaceutical Research Institute

Curated by PDSP Ki Database
LigandPNGBDBM50003560(4-methoxy-17-methyl-17-azatetracyclo[7.5.3.01,10.0...)
Affinity DataKi:  11.2nMMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetSodium-dependent serotonin transporter(Homo sapiens (Human))
The University Of Kansas

Curated by ChEMBL
LigandPNGBDBM213826(Dextromethorphan | US11535596, Compound Dextrometh...)
Affinity DataKi:  18nMAssay Description:Displacement of [3H]-Citalopram from SERT receptor (unknown origin) expressed in HEK cell membrane incubated for 2 hrs by liquid scintillation counte...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSodium-dependent serotonin transporter(Rattus norvegicus (rat))
R. W. Johnson Pharmaceutical Research Institute

Curated by PDSP Ki Database
LigandPNGBDBM50003560(4-methoxy-17-methyl-17-azatetracyclo[7.5.3.01,10.0...)
Affinity DataKi:  23nMMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetSodium-dependent serotonin transporter(Rattus norvegicus (rat))
R. W. Johnson Pharmaceutical Research Institute

Curated by PDSP Ki Database
LigandPNGBDBM50003560(4-methoxy-17-methyl-17-azatetracyclo[7.5.3.01,10.0...)
Affinity DataKi:  35.8nMMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetSigma non-opioid intracellular receptor 1(Cavia porcellus (Guinea pig))
The State University Of New Jersey

Curated by ChEMBL
LigandPNGBDBM50366613(DEXTROMETHORPHAN)
Affinity DataKi:  63nMAssay Description:Displacement of [3H]-(+)-pentazocine from sigma-1 receptor in guinea pig brain membranes incubated for 1 hr by liquid scintillation counting methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSigma non-opioid intracellular receptor 1(Homo sapiens (Human))
The University Of Kansas

Curated by ChEMBL
LigandPNGBDBM213826(Dextromethorphan | US11535596, Compound Dextrometh...)
Affinity DataKi:  73nMAssay Description:Displacement of [3H]-Citalopram from sigma-1 receptor (unknown origin) expressed in HEK cell membrane incubated for 2 hrs by liquid scintillation cou...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSigma non-opioid intracellular receptor 1(Homo sapiens (Human))
The University Of Kansas

Curated by ChEMBL
LigandPNGBDBM213826(Dextromethorphan | US11535596, Compound Dextrometh...)
Affinity DataKi:  96.3nMAssay Description:In vitro binding assays for the phencyclidine site of NMDA-type glutamate receptors, and for sigma-1 receptors, both of which are known to be bound b...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetNorepinephrine transporter(RAT)
R. W. Johnson Pharmaceutical Research Institute

Curated by PDSP Ki Database
LigandPNGBDBM50003560(4-methoxy-17-methyl-17-azatetracyclo[7.5.3.01,10.0...)
Affinity DataKi:  179nMMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetKappa-type opioid receptor(Rattus norvegicus (rat))
R. W. Johnson Pharmaceutical Research Institute

Curated by PDSP Ki Database
LigandPNGBDBM50003560(4-methoxy-17-methyl-17-azatetracyclo[7.5.3.01,10.0...)
Affinity DataKi:  225nMMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetNorepinephrine transporter(RAT)
R. W. Johnson Pharmaceutical Research Institute

Curated by PDSP Ki Database
LigandPNGBDBM50003560(4-methoxy-17-methyl-17-azatetracyclo[7.5.3.01,10.0...)
Affinity DataKi:  240nMMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetDelta-type opioid receptor(Rattus norvegicus (rat))
R. W. Johnson Pharmaceutical Research Institute

Curated by PDSP Ki Database
LigandPNGBDBM50003560(4-methoxy-17-methyl-17-azatetracyclo[7.5.3.01,10.0...)
Affinity DataKi:  249nMMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetSigma non-opioid intracellular receptor 1(Homo sapiens (Human))
The University Of Kansas

Curated by ChEMBL
LigandPNGBDBM50366613(DEXTROMETHORPHAN)
Affinity DataKi:  348nMAssay Description:Inhibition of [3H](+)-pentazocine binding to Sigma receptor type 1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSigma non-opioid intracellular receptor 1(Homo sapiens (Human))
The University Of Kansas

Curated by ChEMBL
LigandPNGBDBM50003560(4-methoxy-17-methyl-17-azatetracyclo[7.5.3.01,10.0...)
Affinity DataKi:  521nMMore data for this Ligand-Target Pair
In DepthDetails PubMed
LigandPNGBDBM50003560(4-methoxy-17-methyl-17-azatetracyclo[7.5.3.01,10.0...)
Affinity DataKi:  768nMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSigma intracellular receptor 2(Homo sapiens (Human))
The University Of Kansas

Curated by ChEMBL
LigandPNGBDBM213826(Dextromethorphan | US11535596, Compound Dextrometh...)
Affinity DataKi:  862nMAssay Description:Displacement of [3H]-Citalopram from sigma-2 receptor (unknown origin) expressed in HEK cell membrane incubated for 2 hrs by liquid scintillation cou...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMu-type opioid receptor(Rattus norvegicus (rat))
R. W. Johnson Pharmaceutical Research Institute

Curated by PDSP Ki Database
LigandPNGBDBM50003560(4-methoxy-17-methyl-17-azatetracyclo[7.5.3.01,10.0...)
Affinity DataKi:  1.28E+3nMMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetGlutamate receptor ionotropic, NMDA 1(Homo sapiens (Human))
Center For Neurologic Study

US Patent
LigandPNGBDBM213826(Dextromethorphan | US11535596, Compound Dextrometh...)
Affinity DataKi:  4.52E+3nMAssay Description:In vitro binding assays for the phencyclidine site of NMDA-type glutamate receptors, and for sigma-1 receptors, both of which are known to be bound b...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetSodium channel protein type 1/2/3 subunit alpha(Rattus norvegicus)
Boehringer Ingelheim Pharma

Curated by ChEMBL
LigandPNGBDBM50366613(DEXTROMETHORPHAN)
Affinity DataKi:  4.80E+3nMAssay Description:Displacement of [3H]BTX from sodium channel of rat cerebral cortex synaptosomesMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50366613(DEXTROMETHORPHAN)
Affinity DataKi:  5.07E+3nMAssay Description:Binding affinity was measured as selectivity for sigma-1 site over muscarinic (M1) receptor in ratMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetKappa-type opioid receptor(Rattus norvegicus (rat))
R. W. Johnson Pharmaceutical Research Institute

Curated by PDSP Ki Database
LigandPNGBDBM50003560(4-methoxy-17-methyl-17-azatetracyclo[7.5.3.01,10.0...)
Affinity DataKi:  7.00E+3nMMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetMuscarinic acetylcholine receptor M2(RAT)
Albany Molecular Research

Curated by ChEMBL
LigandPNGBDBM50366613(DEXTROMETHORPHAN)
Affinity DataKi: >1.00E+4nMAssay Description:Binding affinity was measured against muscarinic (M2) receptor at 10 uM in rat using [3H]QN as radioligandMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDelta-type opioid receptor(Rattus norvegicus (rat))
R. W. Johnson Pharmaceutical Research Institute

Curated by PDSP Ki Database
LigandPNGBDBM50003560(4-methoxy-17-methyl-17-azatetracyclo[7.5.3.01,10.0...)
Affinity DataKi: >1.00E+4nMMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetSodium-dependent noradrenaline transporter(Homo sapiens (Human))
The University Of Kansas

Curated by ChEMBL
LigandPNGBDBM213826(Dextromethorphan | US11535596, Compound Dextrometh...)
Affinity DataKi: >1.00E+4nMAssay Description:Displacement of [3H]-Citalopram from NET (unknown origin) expressed in HEK cell membrane incubated for 2 hrs by liquid scintillation counter analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSigma non-opioid intracellular receptor 1(Cavia porcellus (Guinea pig))
The State University Of New Jersey

Curated by ChEMBL
LigandPNGBDBM50366613(DEXTROMETHORPHAN)
Affinity DataIC50:  15.2nMAssay Description:Displacement of [3H]pentazocine from sigma1 receptor in guinea pig membrane in presence of phenytoinMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2D6(Homo sapiens (Human))
Sichuan University

Curated by ChEMBL
LigandPNGBDBM50366613(DEXTROMETHORPHAN)
Affinity DataIC50:  41nMAssay Description:Inhibition of CYP2D6 in human liver microsomes incubated for 15 to 40 mins in presence of NADPHMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetCytochrome P450 2D6(Homo sapiens (Human))
Sichuan University

Curated by ChEMBL
LigandPNGBDBM50366613(DEXTROMETHORPHAN)
Affinity DataIC50:  43nMAssay Description:Inhibition of CYP2D6 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetSodium-dependent serotonin transporter(Homo sapiens (Human))
The University Of Kansas

Curated by ChEMBL
LigandPNGBDBM213826(Dextromethorphan | US11535596, Compound Dextrometh...)
Affinity DataIC50:  56nMAssay Description:Inhibition of human SERT receptor expressed in human HEK293 cells assessed as inhibition of substrate transport measured after 1 hr by flourescence b...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSigma non-opioid intracellular receptor 1(Homo sapiens (Human))
The University Of Kansas

Curated by ChEMBL
LigandPNGBDBM213826(Dextromethorphan | US11535596, Compound Dextrometh...)
Affinity DataIC50:  137nMAssay Description:In vitro binding assays for the phencyclidine site of NMDA-type glutamate receptors, and for sigma-1 receptors, both of which are known to be bound b...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetSigma non-opioid intracellular receptor 1(Cavia porcellus (Guinea pig))
The State University Of New Jersey

Curated by ChEMBL
LigandPNGBDBM50366613(DEXTROMETHORPHAN)
Affinity DataIC50:  232nMAssay Description:Displacement of [3H]pentazocine from sigma1 receptor in guinea pig membraneMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSodium channel protein type 1/2/3 subunit alpha(Rattus norvegicus)
Boehringer Ingelheim Pharma

Curated by ChEMBL
LigandPNGBDBM50003560(4-methoxy-17-methyl-17-azatetracyclo[7.5.3.01,10.0...)
Affinity DataIC50:  1.30E+3nMAssay Description:Binding of [3H]batrachotoxin (BTX) to rat brain sodium channelMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSodium channel protein type 1/2/3 subunit alpha(Rattus norvegicus)
Boehringer Ingelheim Pharma

Curated by ChEMBL
LigandPNGBDBM50366613(DEXTROMETHORPHAN)
Affinity DataIC50:  1.30E+3nMAssay Description:Inhibition of [3H]batrachotoxin binding to rat brain sodium channelMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2D6(Homo sapiens (Human))
Sichuan University

Curated by ChEMBL
LigandPNGBDBM50366613(DEXTROMETHORPHAN)
Affinity DataIC50:  1.80E+3nMAssay Description:Inhibition of MAMC O-dealkylation mediated by human Cytochrome P450 2D6 expressed in human lymphoblastoid cell lineMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50003560(4-methoxy-17-methyl-17-azatetracyclo[7.5.3.01,10.0...)
Affinity DataIC50:  2.00E+3nMAssay Description:Concentration required to inhibit [3H]naltrexone binding to Opioid receptorsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2D6(Homo sapiens (Human))
Sichuan University

Curated by ChEMBL
LigandPNGBDBM50366613(DEXTROMETHORPHAN)
Affinity DataIC50:  3.40E+3nMAssay Description:Inhibition of human CYP2D6 expressed in Escherichia coli JM109More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2D26(Rattus norvegicus)
Vrije Universiteit

Curated by ChEMBL
LigandPNGBDBM50366613(DEXTROMETHORPHAN)
Affinity DataIC50:  5.60E+3nMAssay Description:Inhibition of MAMC O-dealkylation mediated by rat Cytochrome P450 2D2 expressed in Saccharomyces cerevisiaeMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, NMDA 1(Homo sapiens (Human))
Center For Neurologic Study

US Patent
LigandPNGBDBM213826(Dextromethorphan | US11535596, Compound Dextrometh...)
Affinity DataIC50:  6.82E+3nMAssay Description:In vitro binding assays for the phencyclidine site of NMDA-type glutamate receptors, and for sigma-1 receptors, both of which are known to be bound b...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetSodium-dependent noradrenaline transporter(Homo sapiens (Human))
The University Of Kansas

Curated by ChEMBL
LigandPNGBDBM213826(Dextromethorphan | US11535596, Compound Dextrometh...)
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of human NET expressed in human HEK293 cells assessed as inhibition of substrate transport measured after 1 hr by flourescence based plate...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSodium channel protein type 1/2/3 subunit alpha(Rattus norvegicus)
Boehringer Ingelheim Pharma

Curated by ChEMBL
LigandPNGBDBM50366613(DEXTROMETHORPHAN)
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibitory effect against veratridine-induced glutamate release from rat brain slicesMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSolute carrier family 22 member 1(Homo sapiens (Human))
University Of California

Curated by ChEMBL
LigandPNGBDBM50366613(DEXTROMETHORPHAN)
Affinity DataIC50:  1.05E+4nMAssay Description:Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNeuronal acetylcholine receptor subunit alpha-3/beta-4(Rattus norvegicus (Rat))
Medical University Of Lublin

Curated by ChEMBL
LigandPNGBDBM50366613(DEXTROMETHORPHAN)
Affinity DataIC50:  1.11E+4nMAssay Description:Non-competitive inhibition of rat alpha3beta4 nAChR expressed in KX cells assessed as reduction in current by whole-cell patch clamp assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSolute carrier family 22 member 1(Homo sapiens (Human))
University Of California

Curated by ChEMBL
LigandPNGBDBM50366613(DEXTROMETHORPHAN)
Affinity DataIC50:  1.50E+4nMAssay Description:Inhibition of human OCT1 expressed in HEK293 cells assessed as reduction in ASP+ substrate uptake by microplate reader based analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2D3(Rattus norvegicus)
Vrije Universiteit

Curated by ChEMBL
LigandPNGBDBM50366613(DEXTROMETHORPHAN)
Affinity DataIC50:  1.86E+4nMAssay Description:Inhibition of MAMC O-dealkylation mediated by rat Cytochrome P450 2D3 expressed in Saccharomyces cerevisiaeMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2J2(Homo sapiens (Human))
Tongji University

Curated by ChEMBL
LigandPNGBDBM50366613(DEXTROMETHORPHAN)
Affinity DataIC50: >5.00E+4nMAssay Description:Inhibition of human recombinant CYP2J2 assessed as reduction in astemizole O-demethylation by LC-MS/MS methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetUDP-glucuronosyltransferase 2B10(Homo sapiens (Human))
Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences

LigandPNGBDBM213826(Dextromethorphan | US11535596, Compound Dextrometh...)
Affinity DataIC50:  6.20E+4nMAssay Description:Refer to Fisher et al., Drug Metab. Dispos., 28:560-566.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetUDP-glucuronosyltransferase 1A4(Homo sapiens (Human))
Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences

LigandPNGBDBM213826(Dextromethorphan | US11535596, Compound Dextrometh...)
Affinity DataIC50:  8.90E+4nMAssay Description:Refer to Fisher et al., Drug Metab. Dispos., 28:560-566.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSodium channel protein type 1/2/3 subunit alpha(Rattus norvegicus)
Boehringer Ingelheim Pharma

Curated by ChEMBL
LigandPNGBDBM50366613(DEXTROMETHORPHAN)
Affinity DataIC50: >1.00E+5nMAssay Description:Inhibition of [3H]saxitoxin binding to rat brain sodium channelMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2D4(Rattus norvegicus)
Vrije Universiteit

Curated by ChEMBL
LigandPNGBDBM50366613(DEXTROMETHORPHAN)
Affinity DataIC50:  1.36E+5nMAssay Description:Inhibition of MAMC O-dealkylation mediated by rat Cytochrome P450 2D4 expressed in Saccharomyces cerevisiaeMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2D1(Rattus norvegicus)
Vrije Universiteit

Curated by ChEMBL
LigandPNGBDBM50366613(DEXTROMETHORPHAN)
Affinity DataIC50:  2.64E+5nMAssay Description:Inhibition of MAMC O-dealkylation mediated by rat Cytochrome P450 2D1 expressed in Saccharomyces cerevisiaeMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetUDP-glucuronosyltransferase 2B7(Homo sapiens (Human))
Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences

LigandPNGBDBM213826(Dextromethorphan | US11535596, Compound Dextrometh...)
Affinity DataIC50: >3.00E+5nMAssay Description:Refer to Fisher et al., Drug Metab. Dispos., 28:560-566.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetUDP-glucuronosyltransferase 1-6(Homo sapiens (Human))
Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences

LigandPNGBDBM213826(Dextromethorphan | US11535596, Compound Dextrometh...)
Affinity DataIC50: >3.00E+5nMAssay Description:Refer to Fisher et al., Drug Metab. Dispos., 28:560-566.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetUDP-glucuronosyltransferase 1A1(Homo sapiens (Human))
Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences

LigandPNGBDBM213826(Dextromethorphan | US11535596, Compound Dextrometh...)
Affinity DataIC50: >3.00E+5nMAssay Description:Refer to Fisher et al., Drug Metab. Dispos., 28:560-566.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSodium channel protein type 1/2/3 subunit alpha(Rattus norvegicus)
Boehringer Ingelheim Pharma

Curated by ChEMBL
LigandPNGBDBM50003560(4-methoxy-17-methyl-17-azatetracyclo[7.5.3.01,10.0...)
Affinity DataIC50: >3.00E+5nMAssay Description:Binding of [3H]saxitoxin (STX) to rat brain sodium channelMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMas-related G-protein coupled receptor member X2(Homo sapiens (Human))
University of North Carolina

LigandPNGBDBM213826(Dextromethorphan | US11535596, Compound Dextrometh...)
Affinity DataEC50:  5.90E+3nMpH: 7.4 T: 2°CAssay Description:MRGPRX2 stable cells were maintained in DMEM containing 10% FBS, 100 μg/ml hygromycin B, and 15 μg/ml blasticidin. For the calcium mobiliza...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMas-related G-protein coupled receptor member X2(Homo sapiens (Human))
University of North Carolina

LigandPNGBDBM213826(Dextromethorphan | US11535596, Compound Dextrometh...)
Affinity DataEC50:  3.20E+3nMpH: 7.4 T: 2°CAssay Description:HTLA cells (HEK-T cells stably expressing a β-arrestin2-TEV fusion protein and a tTa-dependent luciferase reporter) were maintained in DMEM (Cor...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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