TargetLysine-specific histone demethylase 1A(Homo sapiens (Human))
Constellation Pharmaceuticals
Curated by ChEMBL
Constellation Pharmaceuticals
Curated by ChEMBL
Affinity DataKi: 6.10nMAssay Description:Time dependant inhibition of recombinant N-terminal His-tagged LSD1 (unknown origin) expressed in Escherichia coli expression system assessed as inhi...More data for this Ligand-Target Pair
TargetLysine-specific histone demethylase 1A(Homo sapiens (Human))
Constellation Pharmaceuticals
Curated by ChEMBL
Constellation Pharmaceuticals
Curated by ChEMBL
Affinity DataKi: 9.60nMAssay Description:Time dependant inhibition of recombinant N-terminal His-tagged LSD1 (unknown origin) expressed in Escherichia coli expression system assessed as inhi...More data for this Ligand-Target Pair
Affinity DataIC50: 0.0160nMAssay Description:Full length KDM2B was cloned, expressed, and purified to homogeneity. Compound inhibition of KDM2B demethylase activity was assessed by monitoring th...More data for this Ligand-Target Pair
Affinity DataIC50: 0.0210nMAssay Description:Full length KDM2B was cloned, expressed, and purified to homogeneity. Compound inhibition of KDM2B demethylase activity was assessed by monitoring th...More data for this Ligand-Target Pair
Affinity DataIC50: 0.0210nMAssay Description:Full length KDM2B was cloned, expressed, and purified to homogeneity. Compound inhibition of KDM2B demethylase activity was assessed by monitoring th...More data for this Ligand-Target Pair
Affinity DataIC50: 0.0250nMpH: 7.0 T: 2°CAssay Description:Full length KDM5A enzyme was expressed and purified inhouse. Biotin-H3K4me3 peptide was purchased from New England Biolabs. HTRF reagents (containing...More data for this Ligand-Target Pair
Affinity DataIC50: 0.0270nMAssay Description:Full length KDM2B was cloned, expressed, and purified to homogeneity. Compound inhibition of KDM2B demethylase activity was assessed by monitoring th...More data for this Ligand-Target Pair
Affinity DataIC50: 0.0310nMAssay Description:Full length KDM2B was cloned, expressed, and purified to homogeneity. Compound inhibition of KDM2B demethylase activity was assessed by monitoring th...More data for this Ligand-Target Pair
Affinity DataIC50: 0.0340nMAssay Description:Full length KDM2B was cloned, expressed, and purified to homogeneity. Compound inhibition of KDM2B demethylase activity was assessed by monitoring th...More data for this Ligand-Target Pair
Affinity DataIC50: 0.0350nMAssay Description:Full length KDM2B was cloned, expressed, and purified to homogeneity. Compound inhibition of KDM2B demethylase activity was assessed by monitoring th...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals
US Patent
Constellation Pharmaceuticals
US Patent
Affinity DataIC50: 0.0370nMAssay Description:EZH2 biochemical assay (IC50): Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM P...More data for this Ligand-Target Pair
Affinity DataIC50: 0.0370nMpH: 7.0 T: 2°CAssay Description:Full length KDM5A enzyme was expressed and purified inhouse. Biotin-H3K4me3 peptide was purchased from New England Biolabs. HTRF reagents (containing...More data for this Ligand-Target Pair
Affinity DataIC50: 0.0370nMAssay Description:Full length KDM2B was cloned, expressed, and purified to homogeneity. Compound inhibition of KDM2B demethylase activity was assessed by monitoring th...More data for this Ligand-Target Pair
Affinity DataIC50: 0.0380nMpH: 7.0 T: 2°CAssay Description:Full length KDM5A enzyme was expressed and purified inhouse. Biotin-H3K4me3 peptide was purchased from New England Biolabs. HTRF reagents (containing...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals
US Patent
Constellation Pharmaceuticals
US Patent
Affinity DataIC50: 0.0380nMAssay Description:EZH2 biochemical assay (IC50): Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM P...More data for this Ligand-Target Pair
Affinity DataIC50: 0.0390nMpH: 7.0 T: 2°CAssay Description:Full length KDM5A enzyme was expressed and purified inhouse. Biotin-H3K4me3 peptide was purchased from New England Biolabs. HTRF reagents (containing...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals
US Patent
Constellation Pharmaceuticals
US Patent
Affinity DataIC50: 0.0390nMAssay Description:EZH2 biochemical assay (IC50): Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM P...More data for this Ligand-Target Pair
Affinity DataIC50: 0.0390nMAssay Description:Full length KDM2B was cloned, expressed, and purified to homogeneity. Compound inhibition of KDM2B demethylase activity was assessed by monitoring th...More data for this Ligand-Target Pair
Affinity DataIC50: 0.0410nMAssay Description:Full length KDM2B was cloned, expressed, and purified to homogeneity. Compound inhibition of KDM2B demethylase activity was assessed by monitoring th...More data for this Ligand-Target Pair
Affinity DataIC50: 0.0410nMAssay Description:Full length KDM2B was cloned, expressed, and purified to homogeneity. Compound inhibition of KDM2B demethylase activity was assessed by monitoring th...More data for this Ligand-Target Pair
Affinity DataIC50: 0.0430nMAssay Description:Full length KDM2B was cloned, expressed, and purified to homogeneity. Compound inhibition of KDM2B demethylase activity was assessed by monitoring th...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals
US Patent
Constellation Pharmaceuticals
US Patent
Affinity DataIC50: 0.0430nMAssay Description:EZH2 biochemical assay (IC50): Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM P...More data for this Ligand-Target Pair
Affinity DataIC50: 0.0460nMpH: 7.0 T: 2°CAssay Description:Full length KDM5A enzyme was expressed and purified inhouse. Biotin-H3K4me3 peptide was purchased from New England Biolabs. HTRF reagents (containing...More data for this Ligand-Target Pair
Affinity DataIC50: 0.0460nMAssay Description:Full length KDM2B was cloned, expressed, and purified to homogeneity. Compound inhibition of KDM2B demethylase activity was assessed by monitoring th...More data for this Ligand-Target Pair
Affinity DataIC50: 0.0470nMAssay Description:Full length KDM2B was cloned, expressed, and purified to homogeneity. Compound inhibition of KDM2B demethylase activity was assessed by monitoring th...More data for this Ligand-Target Pair
Affinity DataIC50: 0.0470nMpH: 7.0 T: 2°CAssay Description:Full length KDM5A enzyme was expressed and purified inhouse. Biotin-H3K4me3 peptide was purchased from New England Biolabs. HTRF reagents (containing...More data for this Ligand-Target Pair
Affinity DataIC50: 0.0480nMAssay Description:Full length KDM2B was cloned, expressed, and purified to homogeneity. Compound inhibition of KDM2B demethylase activity was assessed by monitoring th...More data for this Ligand-Target Pair
Affinity DataIC50: 0.0490nMAssay Description:Full length KDM2B was cloned, expressed, and purified to homogeneity. Compound inhibition of KDM2B demethylase activity was assessed by monitoring th...More data for this Ligand-Target Pair
Affinity DataIC50: 0.0490nMAssay Description:Full length KDM2B was cloned, expressed, and purified to homogeneity. Compound inhibition of KDM2B demethylase activity was assessed by monitoring th...More data for this Ligand-Target Pair
Affinity DataIC50: 0.0490nMAssay Description:Full length KDM2B was cloned, expressed, and purified to homogeneity. Compound inhibition of KDM2B demethylase activity was assessed by monitoring th...More data for this Ligand-Target Pair
Affinity DataIC50: 0.0490nMAssay Description:Full length KDM2B was cloned, expressed, and purified to homogeneity. Compound inhibition of KDM2B demethylase activity was assessed by monitoring th...More data for this Ligand-Target Pair
Affinity DataIC50: 0.0490nMpH: 7.0 T: 2°CAssay Description:Full length KDM5A enzyme was expressed and purified inhouse. Biotin-H3K4me3 peptide was purchased from New England Biolabs. HTRF reagents (containing...More data for this Ligand-Target Pair
Affinity DataIC50: 0.0500nMAssay Description:Full length KDM2B was cloned, expressed, and purified to homogeneity. Compound inhibition of KDM2B demethylase activity was assessed by monitoring th...More data for this Ligand-Target Pair
Affinity DataIC50: 0.0500nMAssay Description:Full length KDM2B was cloned, expressed, and purified to homogeneity. Compound inhibition of KDM2B demethylase activity was assessed by monitoring th...More data for this Ligand-Target Pair
Affinity DataIC50: 0.0500nMpH: 7.0 T: 2°CAssay Description:Full length KDM5A enzyme was expressed and purified inhouse. Biotin-H3K4me3 peptide was purchased from New England Biolabs. HTRF reagents (containing...More data for this Ligand-Target Pair
Affinity DataIC50: 0.0510nMpH: 7.0 T: 2°CAssay Description:Full length KDM5A enzyme was expressed and purified inhouse. Biotin-H3K4me3 peptide was purchased from New England Biolabs. HTRF reagents (containing...More data for this Ligand-Target Pair
Affinity DataIC50: 0.0510nMpH: 7.0 T: 2°CAssay Description:Full length KDM5A enzyme was expressed and purified inhouse. Biotin-H3K4me3 peptide was purchased from New England Biolabs. HTRF reagents (containing...More data for this Ligand-Target Pair
Affinity DataIC50: 0.0530nMpH: 7.0 T: 2°CAssay Description:Full length KDM5A enzyme was expressed and purified inhouse. Biotin-H3K4me3 peptide was purchased from New England Biolabs. HTRF reagents (containing...More data for this Ligand-Target Pair
Affinity DataIC50: 0.0530nMAssay Description:Full length KDM2B was cloned, expressed, and purified to homogeneity. Compound inhibition of KDM2B demethylase activity was assessed by monitoring th...More data for this Ligand-Target Pair
Affinity DataIC50: 0.0540nMpH: 7.0 T: 2°CAssay Description:Full length KDM5A enzyme was expressed and purified inhouse. Biotin-H3K4me3 peptide was purchased from New England Biolabs. HTRF reagents (containing...More data for this Ligand-Target Pair
Affinity DataIC50: 0.0540nMAssay Description:Full length KDM2B was cloned, expressed, and purified to homogeneity. Compound inhibition of KDM2B demethylase activity was assessed by monitoring th...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals
US Patent
Constellation Pharmaceuticals
US Patent
Affinity DataIC50: 0.0540nMAssay Description:EZH2 biochemical assay (IC50): Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM P...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals
US Patent
Constellation Pharmaceuticals
US Patent
Affinity DataIC50: 0.0540nMAssay Description:EZH2 biochemical assay (IC50): Compound potencies were assessed through incorporation of 3H-SAM into a biotinylated H3 peptide. Specifically, 30 pM P...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals
US Patent
Constellation Pharmaceuticals
US Patent
Affinity DataIC50: 0.0570nMAssay Description:Inhibition of N-terminal FLAG-tagged EZH2 in PRC2 complex (unknown origin) expressed in baculovirus infected Sf9 cells using H2N-RKQLATKAAR(Kme0)SAPA...More data for this Ligand-Target Pair
Affinity DataIC50: 0.0580nMpH: 7.0 T: 2°CAssay Description:Full length KDM5A enzyme was expressed and purified inhouse. Biotin-H3K4me3 peptide was purchased from New England Biolabs. HTRF reagents (containing...More data for this Ligand-Target Pair
Affinity DataIC50: 0.0580nMAssay Description:Full length KDM2B was cloned, expressed, and purified to homogeneity. Compound inhibition of KDM2B demethylase activity was assessed by monitoring th...More data for this Ligand-Target Pair
Affinity DataIC50: 0.0580nMpH: 7.0 T: 2°CAssay Description:Full length KDM5A enzyme was expressed and purified inhouse. Biotin-H3K4me3 peptide was purchased from New England Biolabs. HTRF reagents (containing...More data for this Ligand-Target Pair
Affinity DataIC50: 0.0590nMpH: 7.0 T: 2°CAssay Description:Full length KDM5A enzyme was expressed and purified inhouse. Biotin-H3K4me3 peptide was purchased from New England Biolabs. HTRF reagents (containing...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals
US Patent
Constellation Pharmaceuticals
US Patent
Affinity DataIC50: 0.0590nMAssay Description:Inhibition of N-terminal FLAG-tagged EZH2 in PRC2 complex (unknown origin) expressed in baculovirus infected Sf9 cells using H2N-RKQLATKAAR(Kme0)SAPA...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Constellation Pharmaceuticals
US Patent
Constellation Pharmaceuticals
US Patent
Affinity DataIC50: 0.0600nMAssay Description:Inhibition of N-terminal FLAG-tagged EZH2 in PRC2 complex (unknown origin) expressed in baculovirus infected Sf9 cells using H2N-RKQLATKAAR(Kme0)SAPA...More data for this Ligand-Target Pair