BDBM50017293 CHEMBL3287735::US10647700, Compound GSK126
SMILES CC[C@H](C)n1cc(C)c2c(cc(cc12)-c1ccc(nc1)N1CCNCC1)C(=O)NCc1c(C)cc(C)[nH]c1=O
InChI Key InChIKey=FKSFKBQGSFSOSM-QFIPXVFZSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 19 hits for monomerid = 50017293
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Icahn School Of Medicine At Mount Sinai
Curated by ChEMBL
Icahn School Of Medicine At Mount Sinai
Curated by ChEMBL
Affinity DataKi: 0.5nMAssay Description:Inhibition of human wild-type EZH2 assessed as H3K27me0 level after 30 mins by scintillation counting analysis in presence of [3H]-SAMMore data for this Ligand-Target Pair
3D Structure (crystal)TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Icahn School Of Medicine At Mount Sinai
Curated by ChEMBL
Icahn School Of Medicine At Mount Sinai
Curated by ChEMBL
Affinity DataKi: 0.5nMAssay Description:Inhibition of human EZH2 Y641C mutant assessed as H3K27me2 level after 30 mins by scintillation counting analysis in presence of [3H]-SAMMore data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Icahn School Of Medicine At Mount Sinai
Curated by ChEMBL
Icahn School Of Medicine At Mount Sinai
Curated by ChEMBL
Affinity DataKi: 0.5nMAssay Description:Inhibition of human EZH2 Y641S mutant assessed as H3K27me2 level after 30 mins by scintillation counting analysis in presence of [3H]-SAMMore data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Icahn School Of Medicine At Mount Sinai
Curated by ChEMBL
Icahn School Of Medicine At Mount Sinai
Curated by ChEMBL
Affinity DataKi: 0.5nMAssay Description:Inhibition of human EZH2 Y641N mutant assessed as H3K27me2 level after 30 mins by scintillation counting analysis in presence of [3H]-SAMMore data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Icahn School Of Medicine At Mount Sinai
Curated by ChEMBL
Icahn School Of Medicine At Mount Sinai
Curated by ChEMBL
Affinity DataKi: 0.5nMAssay Description:Inhibition of human EZH2 Y641H mutant assessed as H3K27me2 level after 30 mins by scintillation counting analysis in presence of [3H]-SAMMore data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Icahn School Of Medicine At Mount Sinai
Curated by ChEMBL
Icahn School Of Medicine At Mount Sinai
Curated by ChEMBL
Affinity DataKi: 0.5nMAssay Description:Inhibition of human EZH2 Y641F mutant assessed as H3K27me2 level after 30 mins by scintillation counting analysis in presence of [3H]-SAMMore data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Icahn School Of Medicine At Mount Sinai
Curated by ChEMBL
Icahn School Of Medicine At Mount Sinai
Curated by ChEMBL
Affinity DataKi: 0.5nMAssay Description:Inhibition of human EZH2 A677G mutant assessed as H3K27me1 level after 30 mins by scintillation counting analysis in presence of [3H]-SAMMore data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Icahn School Of Medicine At Mount Sinai
Curated by ChEMBL
Icahn School Of Medicine At Mount Sinai
Curated by ChEMBL
Affinity DataKi: 0.5nMAssay Description:Inhibition of human EZH2 A677G mutant assessed as H3K27me0 level after 30 mins by scintillation counting analysis in presence of [3H]-SAMMore data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Icahn School Of Medicine At Mount Sinai
Curated by ChEMBL
Icahn School Of Medicine At Mount Sinai
Curated by ChEMBL
Affinity DataIC50: 10nMAssay Description:Inhibition of EZH2 (unknown origin)More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Icahn School Of Medicine At Mount Sinai
Curated by ChEMBL
Icahn School Of Medicine At Mount Sinai
Curated by ChEMBL
Affinity DataIC50: 9.90nMAssay Description:Inhibition of EZH2 (unknown origin)More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Icahn School Of Medicine At Mount Sinai
Curated by ChEMBL
Icahn School Of Medicine At Mount Sinai
Curated by ChEMBL
Affinity DataIC50: 2.70nMAssay Description:Inhibition of N-terminal His-tagged EZH2 in human PRC2 complex (2 to end residues) expressed in Sf9 cells using [3H]-SAM as substrate preincubated fo...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Icahn School Of Medicine At Mount Sinai
Curated by ChEMBL
Icahn School Of Medicine At Mount Sinai
Curated by ChEMBL
Affinity DataIC50: 5.5nMAssay Description:Inhibition of EZH2 Y641F mutant (unknown origin) using SAM as substrate incubated for 60 mins by luminescence microplate reader assayMore data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Icahn School Of Medicine At Mount Sinai
Curated by ChEMBL
Icahn School Of Medicine At Mount Sinai
Curated by ChEMBL
Affinity DataIC50: 13nMAssay Description:Inhibition of EZH2 (unknown origin) using SAM as substrate incubated for 60 mins by luminescence microplate reader assayMore data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2 [Y641F](Homo sapiens (Human))
Tarapeutics Science
US Patent
Tarapeutics Science
US Patent
Affinity DataIC50: 121nMAssay Description:Enzymatic activity assay was conducted using EZH2(Y641F) TR-FRET assay KIT from Cisbio company on compounds that were shown to be active in primary s...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Icahn School Of Medicine At Mount Sinai
Curated by ChEMBL
Icahn School Of Medicine At Mount Sinai
Curated by ChEMBL
Affinity DataIC50: 280nMAssay Description:Inhibition of EZH2 in human HeLa cells assessed as reduction in H3K27me3 levels incubated for 72 hrs by ELISA methodMore data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Icahn School Of Medicine At Mount Sinai
Curated by ChEMBL
Icahn School Of Medicine At Mount Sinai
Curated by ChEMBL
Affinity DataIC50: 1nMAssay Description:Inhibition of EZH2 (unknown origin) using biotinylated nucleosome, H3K27me3 activator and [3H]-SAM incubated for 60 mins by top-count based methodMore data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Icahn School Of Medicine At Mount Sinai
Curated by ChEMBL
Icahn School Of Medicine At Mount Sinai
Curated by ChEMBL
Affinity DataIC50: 9.90nMAssay Description:Inhibition of wild-type EZH2 (unknown origin)More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12(Homo sapiens (Human))
Korea Research Institute Of Chemical Technology
Curated by ChEMBL
Korea Research Institute Of Chemical Technology
Curated by ChEMBL
Affinity DataIC50: 16nMAssay Description:Inhibition of EZH2 histone methyltransferase activity in EZH2/SUZ12/EED protein complex (unknown origin) using histone H3 peptide/S-adenosylmethionin...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2(Homo sapiens (Human))
Icahn School Of Medicine At Mount Sinai
Curated by ChEMBL
Icahn School Of Medicine At Mount Sinai
Curated by ChEMBL
Affinity DataIC50: 2nMAssay Description:Inhibition of EZH2 Y641N mutant (unknown origin) using biotinylated nucleosome, H3K27me3 activator and [3H]-SAM incubated for 60 mins by top-count ba...More data for this Ligand-Target Pair