TargetHistone-lysine N-methyltransferase EZH2/Polycomb protein EED [40-441]/Polycomb protein SUZ12 [559-739](Human)
Novartis Institutes For Biomedical Research
Novartis Institutes For Biomedical Research
Affinity DataKd: 114nMpH: 8.0 T: 2°CAssay Description:ITC experiments were performed by Auto ITC200 (Microcal) at 25 °C. ITC sample cell was filled with 10 μM PRC2 in titration buffer (25 mM HEPES p...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12(Human)
Novartis
US Patent
Novartis
US Patent
Affinity DataIC50: 0.100nMAssay Description:Representative compounds of the present invention were serially and separately diluted 3-fold in DMSO to obtain a total of eight or twelve concentrat...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12(Human)
Novartis
US Patent
Novartis
US Patent
Affinity DataIC50: 0.100nMAssay Description:Representative compounds of the present invention were serially and separately diluted 3-fold in DMSO to obtain a total of eight or twelve concentrat...More data for this Ligand-Target Pair
TargetHistone-binding protein RBBP4/Histone-lysine N-methyltransferase EZH1/Polycomb protein EED/Polycomb protein SUZ12/Zinc finger protein AEBP2(Human)
Shanghai Hengrui Pharmaceutical
Curated by ChEMBL
Shanghai Hengrui Pharmaceutical
Curated by ChEMBL
Affinity DataIC50: 0.100nMAssay Description:Inhibition of human N-terminal His-tagged EZH2/flag-tagged EED/SUZ12/AEBP2/RBAP48 A677G mutant (2 to end residues) expressed in baculovirus infected ...More data for this Ligand-Target Pair
TargetHistone-binding protein RBBP4/Histone-lysine N-methyltransferase EZH1/Polycomb protein EED/Polycomb protein SUZ12/Zinc finger protein AEBP2(Human)
Shanghai Hengrui Pharmaceutical
Curated by ChEMBL
Shanghai Hengrui Pharmaceutical
Curated by ChEMBL
Affinity DataIC50: 0.400nMAssay Description:Inhibition of human N-terminal His-tagged EZH2/flag-tagged EED/SUZ12/AEBP2/RBAP48 A677G mutant (2 to end residues) expressed in baculovirus infected ...More data for this Ligand-Target Pair
TargetHistone-binding protein RBBP4/Histone-lysine N-methyltransferase EZH1/Polycomb protein EED/Polycomb protein SUZ12/Zinc finger protein AEBP2(Human)
Shanghai Hengrui Pharmaceutical
Curated by ChEMBL
Shanghai Hengrui Pharmaceutical
Curated by ChEMBL
Affinity DataIC50: 0.5nMAssay Description:Inhibition of human N-terminal His-tagged EZH2/flag-tagged EED/SUZ12/AEBP2/RBAP48 A677G mutant (2 to end residues) expressed in baculovirus infected ...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12(Human)
Novartis
US Patent
Novartis
US Patent
Affinity DataIC50: 0.600nMAssay Description:Representative compounds of the present invention were serially and separately diluted 3-fold in DMSO to obtain a total of eight or twelve concentrat...More data for this Ligand-Target Pair
TargetHistone-binding protein RBBP4/Histone-lysine N-methyltransferase EZH1/Polycomb protein EED/Polycomb protein SUZ12/Zinc finger protein AEBP2(Human)
Shanghai Hengrui Pharmaceutical
Curated by ChEMBL
Shanghai Hengrui Pharmaceutical
Curated by ChEMBL
Affinity DataIC50: 0.600nMAssay Description:Inhibition of human N-terminal His-tagged EZH2/flag-tagged EED/SUZ12/AEBP2/RBAP48 A677G mutant (2 to end residues) expressed in baculovirus infected ...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12(Human)
Novartis
US Patent
Novartis
US Patent
Affinity DataIC50: 0.700nMAssay Description:Representative compounds of the present invention were serially and separately diluted 3-fold in DMSO to obtain a total of eight or twelve concentrat...More data for this Ligand-Target Pair
TargetHistone-binding protein RBBP4/Histone-lysine N-methyltransferase EZH1/Polycomb protein EED/Polycomb protein SUZ12/Zinc finger protein AEBP2(Human)
Shanghai Hengrui Pharmaceutical
Curated by ChEMBL
Shanghai Hengrui Pharmaceutical
Curated by ChEMBL
Affinity DataIC50: 0.800nMAssay Description:Inhibition of human N-terminal His-tagged EZH2/flag-tagged EED/SUZ12/AEBP2/RBAP48 A677G mutant (2 to end residues) expressed in baculovirus infected ...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12(Human)
Novartis
US Patent
Novartis
US Patent
Affinity DataIC50: 0.900nMAssay Description:Cell lysates were transferred to the wells of a 384-well plate and the final volume was adjusted to 50 μL per well with PBS. The plate was seale...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12(Human)
Novartis
US Patent
Novartis
US Patent
Affinity DataIC50: 1nMAssay Description:Cell lysates were transferred to the wells of a 384-well plate and the final volume was adjusted to 50 μL per well with PBS. The plate was seale...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12(Human)
Novartis
US Patent
Novartis
US Patent
Affinity DataIC50: 1.30nMAssay Description:Cell lysates were transferred to the wells of a 384-well plate and the final volume was adjusted to 50 μL per well with PBS. The plate was seale...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12(Human)
Novartis
US Patent
Novartis
US Patent
Affinity DataIC50: 1.40nMAssay Description:Cell lysates were transferred to the wells of a 384-well plate and the final volume was adjusted to 50 μL per well with PBS. The plate was seale...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12(Human)
Novartis
US Patent
Novartis
US Patent
Affinity DataIC50: 1.40nMAssay Description:Cell lysates were transferred to the wells of a 384-well plate and the final volume was adjusted to 50 μL per well with PBS. The plate was seale...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12(Human)
Novartis
US Patent
Novartis
US Patent
Affinity DataIC50: 1.5nMpH: 8.0Assay Description:To assess the compounds potency in the EED-H3K27Me3 competition binding assay, compounds were serially diluted 3-fold in DMSO to obtain a total of tw...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12(Human)
Novartis
US Patent
Novartis
US Patent
Affinity DataIC50: 1.60nMAssay Description:Cell lysates were transferred to the wells of a 384-well plate and the final volume was adjusted to 50 μL per well with PBS. The plate was seale...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12(Human)
Novartis
US Patent
Novartis
US Patent
Affinity DataIC50: 1.70nMpH: 8.0Assay Description:To assess the compounds potency in the EED-H3K27Me3 competition binding assay, compounds were serially diluted 3-fold in DMSO to obtain a total of tw...More data for this Ligand-Target Pair
TargetHistone-binding protein RBBP4/Histone-lysine N-methyltransferase EZH2/Polycomb protein EED [40-441]/Polycomb protein SUZ12(Human)
Shanghai Institute of Material Medica, Chinese Academy of Sciences
US Patent
Shanghai Institute of Material Medica, Chinese Academy of Sciences
US Patent
Affinity DataIC50: 1.70nMAssay Description:The TR-FRET method was used to measure the PRC2 enzyme activity. First, the enzyme was mixed with compounds at different concentrations and incubated...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12(Human)
Novartis
US Patent
Novartis
US Patent
Affinity DataIC50: 1.90nMAssay Description:Cell lysates were transferred to the wells of a 384-well plate and the final volume was adjusted to 50 μL per well with PBS. The plate was seale...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12(Human)
Novartis
US Patent
Novartis
US Patent
Affinity DataIC50: 1.90nMpH: 8.0Assay Description:To assess the compounds potency in the EED-H3K27Me3 competition binding assay, compounds were serially diluted 3-fold in DMSO to obtain a total of tw...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12(Human)
Novartis
US Patent
Novartis
US Patent
Affinity DataIC50: 1.90nMpH: 8.0Assay Description:Representative compounds of the present disclosure were serially and separately diluted 3-fold in DMSO to obtain a total of eight or twelve concentra...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12(Human)
Novartis
US Patent
Novartis
US Patent
Affinity DataIC50: 2nMAssay Description:Cell lysates were transferred to the wells of a 384-well plate and the final volume was adjusted to 50 μL per well with PBS. The plate was seale...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12(Human)
Novartis
US Patent
Novartis
US Patent
Affinity DataIC50: 2nMAssay Description:Cell lysates were transferred to the wells of a 384-well plate and the final volume was adjusted to 50 μL per well with PBS. The plate was seale...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12(Human)
Novartis
US Patent
Novartis
US Patent
Affinity DataIC50: 2nMAssay Description:Representative compounds of the present invention were serially and separately diluted 3-fold in DMSO to obtain a total of eight or twelve concentrat...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12(Human)
Novartis
US Patent
Novartis
US Patent
Affinity DataIC50: 2nMAssay Description:Representative compounds of the present invention were serially and separately diluted 3-fold in DMSO to obtain a total of eight or twelve concentrat...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12(Human)
Novartis
US Patent
Novartis
US Patent
Affinity DataIC50: 2.10nMAssay Description:Cell lysates were transferred to the wells of a 384-well plate and the final volume was adjusted to 50 μL per well with PBS. The plate was seale...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12(Human)
Novartis
US Patent
Novartis
US Patent
Affinity DataIC50: 2.10nMAssay Description:Representative compounds of the present invention were serially and separately diluted 3-fold in DMSO to obtain a total of eight or twelve concentrat...More data for this Ligand-Target Pair
TargetHistone-binding protein RBBP4/Histone-lysine N-methyltransferase EZH2 [Y641F]/Polycomb protein EED/Polycomb protein SUZ12/Zinc finger protein AEBP2(Human)
Shanghai Haihe Pharmaceutical
US Patent
Shanghai Haihe Pharmaceutical
US Patent
Affinity DataIC50: 2.15nMAssay Description:EZH2Y641F: PRC2 complex experimental method: Experimental method: PRC2 complex (EZH2 Y641F/EED/SUZ12/RbAp48/AEBP2), H3(1-50) me1 substrate, methyl do...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12(Human)
Novartis
US Patent
Novartis
US Patent
Affinity DataIC50: 2.20nMpH: 8.0Assay Description:To assess the compounds potency in the EED-H3K27Me3 competition binding assay, compounds were serially diluted 3-fold in DMSO to obtain a total of tw...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12(Human)
Novartis
US Patent
Novartis
US Patent
Affinity DataIC50: 2.20nMAssay Description:Cell lysates were transferred to the wells of a 384-well plate and the final volume was adjusted to 50 μL per well with PBS. The plate was seale...More data for this Ligand-Target Pair
TargetHistone-binding protein RBBP4/Histone-lysine N-methyltransferase EZH2/Polycomb protein EED [40-441]/Polycomb protein SUZ12(Human)
Shanghai Institute of Material Medica, Chinese Academy of Sciences
US Patent
Shanghai Institute of Material Medica, Chinese Academy of Sciences
US Patent
Affinity DataIC50: 2.20nMAssay Description:The TR-FRET method was used to measure the PRC2 enzyme activity. First, the enzyme was mixed with compounds at different concentrations and incubated...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12(Human)
Novartis
US Patent
Novartis
US Patent
Affinity DataIC50: 2.30nMpH: 8.0Assay Description:To assess the compounds potency in the EED-H3K27Me3 competition binding assay, compounds were serially diluted 3-fold in DMSO to obtain a total of tw...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12(Human)
Novartis
US Patent
Novartis
US Patent
Affinity DataIC50: 2.30nMAssay Description:Representative compounds of the present invention were serially and separately diluted 3-fold in DMSO to obtain a total of eight or twelve concentrat...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12(Human)
Novartis
US Patent
Novartis
US Patent
Affinity DataIC50: 2.30nMAssay Description:To assess the compounds' potency in the EED-H3K27Me3 competition binding assay, compounds were serially diluted 3-fold in DMSO to obtain a total ...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12(Human)
Novartis
US Patent
Novartis
US Patent
Affinity DataIC50: 2.40nMpH: 8.0Assay Description:To assess the compounds potency in the EED-H3K27Me3 competition binding assay, compounds were serially diluted 3-fold in DMSO to obtain a total of tw...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12(Human)
Novartis
US Patent
Novartis
US Patent
Affinity DataIC50: 2.40nMpH: 8.0Assay Description:To assess the compounds potency in the EED-H3K27Me3 competition binding assay, compounds were serially diluted 3-fold in DMSO to obtain a total of tw...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12(Human)
Novartis
US Patent
Novartis
US Patent
Affinity DataIC50: 2.40nMpH: 8.0Assay Description:To assess the compounds potency in the EED-H3K27Me3 competition binding assay, compounds were serially diluted 3-fold in DMSO to obtain a total of tw...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12(Human)
Novartis
US Patent
Novartis
US Patent
Affinity DataIC50: 2.40nMAssay Description:Cell lysates were transferred to the wells of a 384-well plate and the final volume was adjusted to 50 μL per well with PBS. The plate was seale...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12(Human)
Novartis
US Patent
Novartis
US Patent
Affinity DataIC50: 2.40nMAssay Description:To assess the compounds' potency in the EED-H3K27Me3 competition binding assay, compounds were serially diluted 3-fold in DMSO to obtain a total ...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12(Human)
Novartis
US Patent
Novartis
US Patent
Affinity DataIC50: 2.40nMAssay Description:Representative compounds of the present invention were serially and separately diluted 3-fold in DMSO to obtain a total of eight or twelve concentrat...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12(Human)
Novartis
US Patent
Novartis
US Patent
Affinity DataIC50: 2.5nMAssay Description:Cell lysates were transferred to the wells of a 384-well plate and the final volume was adjusted to 50 μL per well with PBS. The plate was seale...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12(Human)
Novartis
US Patent
Novartis
US Patent
Affinity DataIC50: 2.5nMAssay Description:Cell lysates were transferred to the wells of a 384-well plate and the final volume was adjusted to 50 μL per well with PBS. The plate was seale...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12(Human)
Novartis
US Patent
Novartis
US Patent
Affinity DataIC50: 2.5nMAssay Description:Representative compounds of the present invention were serially and separately diluted 3-fold in DMSO to obtain a total of eight or twelve concentrat...More data for this Ligand-Target Pair
TargetHistone-binding protein RBBP4/Histone-lysine N-methyltransferase EZH2/Polycomb protein EED [40-441]/Polycomb protein SUZ12(Human)
Shanghai Institute of Material Medica, Chinese Academy of Sciences
US Patent
Shanghai Institute of Material Medica, Chinese Academy of Sciences
US Patent
Affinity DataIC50: 2.5nMAssay Description:The TR-FRET method was used to measure the PRC2 enzyme activity. First, the enzyme was mixed with compounds at different concentrations and incubated...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12(Human)
Novartis
US Patent
Novartis
US Patent
Affinity DataIC50: 2.60nMAssay Description:Cell lysates were transferred to the wells of a 384-well plate and the final volume was adjusted to 50 μL per well with PBS. The plate was seale...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12(Human)
Novartis
US Patent
Novartis
US Patent
Affinity DataIC50: 2.60nMpH: 8.0Assay Description:To assess the compounds potency in the EED-H3K27Me3 competition binding assay, compounds were serially diluted 3-fold in DMSO to obtain a total of tw...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12(Human)
Novartis
US Patent
Novartis
US Patent
Affinity DataIC50: 2.60nMpH: 8.0Assay Description:To assess the compounds potency in the EED-H3K27Me3 competition binding assay, compounds were serially diluted 3-fold in DMSO to obtain a total of tw...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12(Human)
Novartis
US Patent
Novartis
US Patent
Affinity DataIC50: 2.60nMAssay Description:Representative compounds of the present invention were serially and separately diluted 3-fold in DMSO to obtain a total of eight or twelve concentrat...More data for this Ligand-Target Pair
TargetHistone-binding protein RBBP4/Histone-lysine N-methyltransferase EZH2 [Y641F]/Polycomb protein EED/Polycomb protein SUZ12/Zinc finger protein AEBP2(Human)
Shanghai Haihe Pharmaceutical
US Patent
Shanghai Haihe Pharmaceutical
US Patent
Affinity DataIC50: 2.65nMAssay Description:EZH2Y641F: PRC2 complex experimental method: Experimental method: PRC2 complex (EZH2 Y641F/EED/SUZ12/RbAp48/AEBP2), H3(1-50) me1 substrate, methyl do...More data for this Ligand-Target Pair
