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

Found 18 hits in this display   

TargetHistamine H1 receptor(Homo sapiens (Human))
Neurocrine Biosciences

Curated by ChEMBL
LigandPNGBDBM50297309((-)-(R)-N,N-dimethyl-2-(3-(1-(pyridin-2-yl)ethyl)b...)
Affinity DataKi:  4nMAssay Description:Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells by liquid scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Homo sapiens (Human))
Neurocrine Biosciences

Curated by ChEMBL
LigandPNGBDBM50297309((-)-(R)-N,N-dimethyl-2-(3-(1-(pyridin-2-yl)ethyl)b...)
Affinity DataKi:  4nMAssay Description:Inhibition of histamine H1 receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Neurocrine Biosciences

Curated by ChEMBL
LigandPNGBDBM50297309((-)-(R)-N,N-dimethyl-2-(3-(1-(pyridin-2-yl)ethyl)b...)
Affinity DataKi: >5nMAssay Description:Displacement of [3H]Dofetilide from human ERGMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMuscarinic acetylcholine receptor M1(Homo sapiens (Human))
Neurocrine Biosciences

Curated by ChEMBL
LigandPNGBDBM50297309((-)-(R)-N,N-dimethyl-2-(3-(1-(pyridin-2-yl)ethyl)b...)
Affinity DataKi:  5.30nMAssay Description:Displacement of [3H]N-methylscopolamine from human muscarinic M1 receptor expressed in CHO Flp-In cells by liquid scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Homo sapiens (Human))
Neurocrine Biosciences

Curated by ChEMBL
LigandPNGBDBM50297309((-)-(R)-N,N-dimethyl-2-(3-(1-(pyridin-2-yl)ethyl)b...)
Affinity DataKi:  12nMAssay Description:Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMuscarinic acetylcholine receptor M1(Homo sapiens (Human))
Neurocrine Biosciences

Curated by ChEMBL
LigandPNGBDBM50297309((-)-(R)-N,N-dimethyl-2-(3-(1-(pyridin-2-yl)ethyl)b...)
Affinity DataKi:  1.40E+3nMAssay Description:Displacement of [3H]N-methylscopolamine from human muscarinic M1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Neurocrine Biosciences

Curated by ChEMBL
LigandPNGBDBM50297309((-)-(R)-N,N-dimethyl-2-(3-(1-(pyridin-2-yl)ethyl)b...)
Affinity DataKi:  1.40E+3nMAssay Description:Inhibition of human ERG expressed in HEK cells assessed as blockade of potassium tail current by standard patch clamp analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Homo sapiens (Human))
Neurocrine Biosciences

Curated by ChEMBL
LigandPNGBDBM50297309((-)-(R)-N,N-dimethyl-2-(3-(1-(pyridin-2-yl)ethyl)b...)
Affinity DataKi:  4.00E+3nMAssay Description:Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Neurocrine Biosciences

Curated by ChEMBL
LigandPNGBDBM50297309((-)-(R)-N,N-dimethyl-2-(3-(1-(pyridin-2-yl)ethyl)b...)
Affinity DataKi: >5.00E+3nMAssay Description:Displacement of [3H]Dofetilide from human ERGMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Neurocrine Biosciences

Curated by ChEMBL
LigandPNGBDBM50297309((-)-(R)-N,N-dimethyl-2-(3-(1-(pyridin-2-yl)ethyl)b...)
Affinity DataIC50:  1.40E+3nMAssay Description:Inhibition of human ERG expressed in HEK293 cells by patch-clamp techniqueMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMuscarinic acetylcholine receptor M1(Homo sapiens (Human))
Neurocrine Biosciences

Curated by ChEMBL
LigandPNGBDBM50297309((-)-(R)-N,N-dimethyl-2-(3-(1-(pyridin-2-yl)ethyl)b...)
Affinity DataIC50:  5.30E+3nMAssay Description:Displacement of [3H]N-methylscopolamine from human muscarinic M1 receptor expressed in CHO Flp-In cells after 90 mins by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2D6(Homo sapiens (Human))
Neurocrine Biosciences

Curated by ChEMBL
LigandPNGBDBM50297309((-)-(R)-N,N-dimethyl-2-(3-(1-(pyridin-2-yl)ethyl)b...)
Affinity DataIC50:  6.90E+3nMAssay Description:Inhibition of recombinant CYP2D6 after 30 mins by fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 3A4(Homo sapiens (Human))
Neurocrine Biosciences

Curated by ChEMBL
LigandPNGBDBM50297309((-)-(R)-N,N-dimethyl-2-(3-(1-(pyridin-2-yl)ethyl)b...)
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of CYP3A4More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 3A4(Homo sapiens (Human))
Neurocrine Biosciences

Curated by ChEMBL
LigandPNGBDBM50297309((-)-(R)-N,N-dimethyl-2-(3-(1-(pyridin-2-yl)ethyl)b...)
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of recombinant CYP3A4 after 30 mins by fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 3A4(Homo sapiens (Human))
Neurocrine Biosciences

Curated by ChEMBL
LigandPNGBDBM50297309((-)-(R)-N,N-dimethyl-2-(3-(1-(pyridin-2-yl)ethyl)b...)
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of recombinant CYP3A4 after 30 mins by fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2D6(Homo sapiens (Human))
Neurocrine Biosciences

Curated by ChEMBL
LigandPNGBDBM50297309((-)-(R)-N,N-dimethyl-2-(3-(1-(pyridin-2-yl)ethyl)b...)
Affinity DataIC50:  2.80E+4nMAssay Description:Inhibition of CYP2D6More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2D6(Homo sapiens (Human))
Neurocrine Biosciences

Curated by ChEMBL
LigandPNGBDBM50297309((-)-(R)-N,N-dimethyl-2-(3-(1-(pyridin-2-yl)ethyl)b...)
Affinity DataIC50:  2.80E+4nMAssay Description:Inhibition of recombinant CYP2D6 after 30 mins by fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2D6(Homo sapiens (Human))
Neurocrine Biosciences

Curated by ChEMBL
LigandPNGBDBM50297309((-)-(R)-N,N-dimethyl-2-(3-(1-(pyridin-2-yl)ethyl)b...)
Affinity DataIC50:  2.82E+4nMAssay Description:Inhibition of recombinant CYP2D6 in presence of NADPH generating systemMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed