BDBM172038 BDBM190183::US10155002, Compound 44::US10647700, Compound EPZ6438::US11052093, Compound 143::US11535629, Compound Control A::US9090562, 143::US9090562, 44::US9394283, 1
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 62 hits for monomerid = 172038
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: 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: 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: 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: 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
Affinity DataIC50: 20nMAssay Description:Inhibition of EZH2 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 4nMAssay Description:Inhibition of EZH2 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 13nMAssay Description:Inhibition of EZH2 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 200nMAssay Description:Inhibition of EZH2 (unknown origin) assessed as reduction in H3K27me3 level treated for 4 days by cellular assay based Western blot analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 150nMAssay Description:Inhibition of EZH2 (unknown origin) using H3-derivede peptide (21 to 44) as substrate incubated for 60 min in presence of SAM by MTase-Glo assayMore data for this Ligand-Target Pair
Affinity DataIC50: 392nMAssay Description:Inhibition of Ezh1 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 4nMAssay Description:Inhibition of Ezh2 (unknown origin)More data for this Ligand-Target Pair
Affinity DataEC50: 200nMAssay Description:Inhibition of EZH2 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 2.70nMAssay Description:Inhibition of human EZH2 using SAM as substrate incubated for 1 hr by microplate luminescence based HMT assayMore data for this Ligand-Target Pair
Affinity DataIC50: 22nMAssay Description:Inhibition of EZH2 (unknown origin) using SAM as substrate preincubated for 10 mins followed by substrate addition and measured after 4 hrs by HTRF a...More data for this Ligand-Target Pair
Affinity DataIC50: 31nMAssay Description:Inhibition of N-terminal FLAG-tagged recombinant full-length human EZH2 Y641F mutant in PRC2 complex expressed in baculovirus infected Sf9 cells usin...More data for this Ligand-Target Pair
Affinity DataIC50: 11nMAssay Description:Inhibition of EZH2 (unknown origin)More 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: 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
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: 6.20nMAssay Description:Test compounds were serially diluted 3-fold in DMSO in a 10 point-curve and 1 uL was spotted into a 384-well microplate in duplicate using a Platemat...More data for this Ligand-Target Pair
Affinity DataIC50: 11.1nMAssay Description:Test compounds were serially diluted 3-fold in DMSO in a 10 point-curve and 1 uL was spotted into a 384-well microplate in duplicate using a Platemat...More data for this Ligand-Target Pair
Affinity DataIC50: 2.20nMAssay Description:Test compounds were serially diluted 3-fold in DMSO in a 10 point-curve and 1 uL was spotted into a 384-well microplate in duplicate using a Platemat...More data for this Ligand-Target Pair
Affinity DataIC50: 1.5nMAssay Description:Test compounds were serially diluted 3-fold in DMSO in a 10 point-curve and 1 uL was spotted into a 384-well microplate in duplicate using a Platemat...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 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: 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: 0.340nMAssay Description:Inhibition of wild type EZH2 (unknown origin) by AlphaLISA assayMore data for this Ligand-Target Pair
Affinity DataIC50: 5.03nMAssay 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: 7.07nMAssay 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: 655nMAssay 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: 1.50E+3nMAssay 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