Affinity DataIC50: 2.60nMAssay 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(Homo sapiens (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
Affinity DataIC50: 4.5nMAssay Description:Inhibition of biotinylated H3K27me3 peptide (19 to 33 residues) binding to His-tagged EED (1 to 441 residues) (unknown origin) incubated for 30 mins ...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12(Homo sapiens (Human))
Novartis
US Patent
Novartis
US Patent
Affinity DataIC50: 5.90nMpH: 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
Affinity DataIC50: 5.90nMAssay 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
Affinity DataIC50: 8.90nMAssay 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(Homo sapiens (Human))
Novartis
US Patent
Novartis
US Patent
Affinity DataIC50: 8.90nMpH: 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
Affinity DataKd: 400nMAssay Description:Binding affinity to EED (unknown origin) assessed as dissociation constant by SPR analysisMore data for this Ligand-Target Pair