null
SMILES CCN(C1CCOCC1)c1cc(cc(C(=O)NCc2c(C)cc(C)[nH]c2=O)c1C)-c1ccc(CN2CCOCC2)cc1
InChI Key InChIKey=NSQSAUGJQHDYNO-UHFFFAOYSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 45 hits for monomerid = 172038
In DepthDetails
Affinity DataKi: 2.5nMAssay Description:Inhibition of wild-type human EZH2 by flash plate assayMore data for this Ligand-Target Pair
Affinity DataIC50: 11.1nMT: 2°CAssay Description:The assays were all performed in a buffer consisting of 20 mM bicine (pH=7.6), 0.5 mM DTT, 0.005% BSG and 0.002% Tween20, prepared on the day of use....More data for this Ligand-Target Pair
Affinity DataIC50: 13.0nMT: 2°CAssay Description:The assays were all performed in a buffer consisting of 20 mM bicine (pH=7.6), 0.5 mM DTT, 0.005% BSG and 0.002% Tween20, prepared on the day of use....More data for this Ligand-Target Pair
Affinity DataIC50: 11.1nMT: 2°CAssay Description:The assays were all performed in a buffer consisting of 20 mM bicine (pH=7.6), 0.5 mM DTT, 0.005% BSG and 0.002% Tween20, prepared on the day of use....More data for this Ligand-Target Pair
Affinity DataIC50: 1nMAssay 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
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
Affinity DataIC50: 20nMAssay 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
Affinity DataEC50: 200nMAssay Description:Inhibition of methyltransferase activity of EZH2 in human G401 cells assessed as H3K27 trimethylation after 4 hrs by ELISAMore data for this Ligand-Target Pair
Affinity DataIC50: 13nMAssay Description:The assays were all performed in a buffer consisting of 20 mM bicine (pH=7.6), 0.5 mM DTT, 0.005% BSG and 0.002% Tween20, prepared on the day of use....More data for this Ligand-Target Pair
Affinity DataIC50: 11.1nMAssay Description:The assays were all performed in a buffer consisting of 20 mM bicine (pH=7.6), 0.5 mM DTT, 0.005% BSG and 0.002% Tween20, prepared on the day of use....More data for this Ligand-Target Pair
Affinity DataIC50: 3.19nMAssay Description:The assays were all performed in a buffer consisting of 20 mM bicine (pH=7.6), 0.5 mM DTT, 0.005% BSG and 0.002% Tween20, prepared on the day of use....More data for this Ligand-Target Pair
Affinity DataIC50: 12.7nMAssay Description:The assays were all performed in a buffer consisting of 20 mM bicine (pH=7.6), 0.5 mM DTT, 0.005% BSG and 0.002% Tween20, prepared on the day of use....More data for this Ligand-Target Pair
TargetPolycomb protein EED(Homo sapiens (Human))
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Affinity DataIC50: 40nMAssay Description:Antagonist activity against hPR (human progesterone receptor) compared to that of progesterone (100%)More data for this Ligand-Target Pair
TargetPolycomb protein EED(Homo sapiens (Human))
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Novartis Institutes for BioMedical Research
Curated by ChEMBL
Affinity DataIC50: 2nMAssay Description:Agonist activity was determined against hPR (human progesterone receptor) compared to that of progesterone (100%)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(Homo sapiens (Human))
Shanghai Hengrui Pharmaceutical Co. Ltd.
Curated by ChEMBL
Shanghai Hengrui Pharmaceutical Co. Ltd.
Curated by ChEMBL
Affinity DataIC50: 4nMAssay 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
Affinity DataIC50: 219nMAssay 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
Affinity DataIC50: 0.340nMAssay Description:Inhibition of wild type EZH2 (unknown origin) by AlphaLISA assayMore data for this Ligand-Target Pair
Affinity DataIC50: 3.19nMAssay Description:The assays were all performed in a buffer consisting of 20 mM bicine (pH=7.6), 0.5 mM DTT, 0.005% BSG and 0.002% Tween20, prepared on the day of use....More data for this Ligand-Target Pair
Affinity DataIC50: 12.7nMAssay Description:The assays were all performed in a buffer consisting of 20 mM bicine (pH=7.6), 0.5 mM DTT, 0.005% BSG and 0.002% Tween20, prepared on the day of use....More data for this Ligand-Target Pair
Affinity DataIC50: 4nMAssay Description:Inhibition of rat EZH2 using H3K27 peptides as substrateMore data for this Ligand-Target Pair
Affinity DataKd: 0.0935nMAssay Description:Inhibition of recombinant PRC2 complex (unknown origin) assessed as dissociation rate constant using H3K27me0 peptide substrate incubated for 3 hrs b...More data for this Ligand-Target Pair
Affinity DataKd: 12nMAssay Description:Inhibition of recombinant PRC2 complex (unknown origin) assessed as kd/ka using H3K27me0 peptide substrate incubated for 3 hrs by HMT assayMore data for this Ligand-Target Pair
Affinity DataIC50: 13nMAssay Description:Inhibition of EZH2 (unknown origin) using H3K27me0 peptide substrate incubated for 3 hrs by HMT assayMore data for this Ligand-Target Pair
Affinity DataIC50: 11nMAssay 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
Affinity DataEC50: 46nMAssay Description:Inhibition of EZH2 in human U2932 cells assessed as suppression H3K27 trimethylation measured after 72 hrs by immunoblot analysisMore data for this Ligand-Target Pair
Affinity DataEC50: 46nMAssay Description:Inhibition of EZH2 in human Raji cells assessed as suppression H3K27 trimethylation measured after 72 hrs by immunoblot analysisMore data for this Ligand-Target Pair
Affinity DataEC50: 51nMAssay Description:Inhibition of EZH2 in human Daudi cells assessed as suppression H3K27 trimethylation measured after 72 hrs by immunoblot analysisMore data for this Ligand-Target Pair
Affinity DataEC50: 6nMAssay Description:Inhibition of EZH2 A677G mutant in human Pfeiffer cells assessed as suppression H3K27 trimethylation measured after 72 hrs by immunoblot analysisMore data for this Ligand-Target Pair
Affinity DataEC50: 5nMAssay Description:Inhibition of EZH2 Y641F mutant in human WSUDLCL2 cells assessed as suppression H3K27 trimethylation measured after 72 hrs by immunoblot analysisMore data for this Ligand-Target Pair
Affinity DataEC50: 64nMAssay Description:Inhibition of EZH2 Y641N mutant in human KARPAS-422 cells assessed as suppression H3K27 trimethylation measured after 72 hrs by immunoblot analysisMore data for this Ligand-Target Pair
Affinity DataEC50: 62nMAssay Description:Inhibition of EZH2 Y641N mutant in human SU-DHL-6 cells assessed as suppression H3K27 trimethylation measured after 72 hrs by immunoblot analysisMore data for this Ligand-Target Pair
Affinity DataEC50: 64nMAssay Description:Inhibition of EZH2 Y641S mutant in human SU-DHL-4 cells assessed as suppression H3K27 trimethylation measured after 72 hrs by immunoblot analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 3.70nMAssay 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
Affinity DataIC50: 140nMAssay Description:The inhibitory activity of the synthesized compounds above against EZH1 or EZH2 methyltransferase was measured. The experiments were consigned to Rea...More data for this Ligand-Target Pair
Affinity DataIC50: 2.45nMAssay Description:The inhibitory activity of the synthesized compounds above against EZH1 or EZH2 methyltransferase was measured. The experiments were consigned to Rea...More data for this Ligand-Target Pair
In DepthDetails
Affinity DataIC50: 13.0nMT: 2°CAssay Description:The assays were all performed in a buffer consisting of 20 mM bicine (pH=7.6), 0.5 mM DTT, 0.005% BSG and 0.002% Tween20, prepared on the day of use....More data for this Ligand-Target Pair
Affinity DataIC50: 3.19nMT: 2°CAssay Description:The assays were all performed in a buffer consisting of 20 mM bicine (pH=7.6), 0.5 mM DTT, 0.005% BSG and 0.002% Tween20, prepared on the day of use....More data for this Ligand-Target Pair
Affinity DataIC50: 12.7nMT: 2°CAssay Description:The assays were all performed in a buffer consisting of 20 mM bicine (pH=7.6), 0.5 mM DTT, 0.005% BSG and 0.002% Tween20, prepared on the day of use....More data for this Ligand-Target Pair