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

Data  3 KI  61 IC50  3 Kd  10 EC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
Find this compound or compounds like it in BindingDB:
   Substructure
Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 77 hits for monomerid = 172038   

TargetHistone-lysine N-methyltransferase EZH1(Human)
Hanmi Pharmaceutical

US Patent
LigandPNGBDBM172038(US10647700, Compound EPZ6438 | BDBM190183 | US1015...)
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
In Depth
Date in BDB:
2/20/2023
Entry Details
Go to US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
University of Pennsylvania

Curated by ChEMBL
LigandPNGBDBM172038(US10647700, Compound EPZ6438 | BDBM190183 | US1015...)
Affinity DataEC50:  200nMAssay Description:Inhibition of EZH2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/19/2024
Entry Details
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
University of Pennsylvania

Curated by ChEMBL
LigandPNGBDBM172038(US10647700, Compound EPZ6438 | BDBM190183 | US1015...)
Affinity DataIC50: 4nMAssay Description:Inhibition of Ezh2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/15/2024
Entry Details
PubMed
TargetHistone-lysine N-methyltransferase EZH1(Human)
Hanmi Pharmaceutical

US Patent
LigandPNGBDBM172038(US10647700, Compound EPZ6438 | BDBM190183 | US1015...)
Affinity DataIC50: 392nMAssay Description:Inhibition of Ezh1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/15/2024
Entry Details
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
University of Pennsylvania

Curated by ChEMBL
LigandPNGBDBM172038(US10647700, Compound EPZ6438 | BDBM190183 | US1015...)
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
In Depth
Date in BDB:
6/25/2023
Entry Details
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
University of Pennsylvania

Curated by ChEMBL
LigandPNGBDBM172038(US10647700, Compound EPZ6438 | BDBM190183 | US1015...)
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
In Depth
Date in BDB:
6/21/2023
Entry Details
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
University of Pennsylvania

Curated by ChEMBL
LigandPNGBDBM172038(US10647700, Compound EPZ6438 | BDBM190183 | US1015...)
Affinity DataIC50: 13nMAssay Description:Inhibition of EZH2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/21/2023
Entry Details
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
University of Pennsylvania

Curated by ChEMBL
LigandPNGBDBM172038(US10647700, Compound EPZ6438 | BDBM190183 | US1015...)
Affinity DataIC50: 4nMAssay Description:Inhibition of EZH2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/19/2023
Entry Details
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
University of Pennsylvania

Curated by ChEMBL
LigandPNGBDBM172038(US10647700, Compound EPZ6438 | BDBM190183 | US1015...)
Affinity DataIC50: 20nMAssay Description:Inhibition of EZH2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/20/2023
Entry Details
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
University of Pennsylvania

Curated by ChEMBL
LigandPNGBDBM172038(US10647700, Compound EPZ6438 | BDBM190183 | US1015...)
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 Depth
Date in BDB:
2/20/2023
Entry Details
Go to US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
University of Pennsylvania

Curated by ChEMBL
LigandPNGBDBM172038(US10647700, Compound EPZ6438 | BDBM190183 | US1015...)
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
In Depth
Date in BDB:
12/16/2024
Entry Details
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
University of Pennsylvania

Curated by ChEMBL
LigandPNGBDBM172038(US10647700, Compound EPZ6438 | BDBM190183 | US1015...)
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
In Depth
Date in BDB:
3/5/2023
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
University of Pennsylvania

Curated by ChEMBL
LigandPNGBDBM172038(US10647700, Compound EPZ6438 | BDBM190183 | US1015...)
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
In Depth
Date in BDB:
8/23/2022
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
University of Pennsylvania

Curated by ChEMBL
LigandPNGBDBM172038(US10647700, Compound EPZ6438 | BDBM190183 | US1015...)
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
In Depth
Date in BDB:
8/23/2022
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
University of Pennsylvania

Curated by ChEMBL
LigandPNGBDBM172038(US10647700, Compound EPZ6438 | BDBM190183 | US1015...)
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
In Depth
Date in BDB:
8/23/2022
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
University of Pennsylvania

Curated by ChEMBL
LigandPNGBDBM172038(US10647700, Compound EPZ6438 | BDBM190183 | US1015...)
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
In Depth
Date in BDB:
8/23/2022
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
University of Pennsylvania

Curated by ChEMBL
LigandPNGBDBM172038(US10647700, Compound EPZ6438 | BDBM190183 | US1015...)
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
In Depth
Date in BDB:
8/23/2022
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
University of Pennsylvania

Curated by ChEMBL
LigandPNGBDBM172038(US10647700, Compound EPZ6438 | BDBM190183 | US1015...)
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
In Depth
Date in BDB:
8/23/2022
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
University of Pennsylvania

Curated by ChEMBL
LigandPNGBDBM172038(US10647700, Compound EPZ6438 | BDBM190183 | US1015...)
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
In Depth
Date in BDB:
3/21/2016
Entry Details
Go to US Patent

TargetHistone-lysine N-methyltransferase EZH1(Human)
Hanmi Pharmaceutical

US Patent
LigandPNGBDBM172038(US10647700, Compound EPZ6438 | BDBM190183 | US1015...)
Affinity DataIC50: 1.17E+3nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/12/2025
Entry Details
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
University of Pennsylvania

Curated by ChEMBL
LigandPNGBDBM172038(US10647700, Compound EPZ6438 | BDBM190183 | US1015...)
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
University of Pennsylvania

Curated by ChEMBL
LigandPNGBDBM172038(US10647700, Compound EPZ6438 | BDBM190183 | US1015...)
Affinity DataIC50: 1.40nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
University of Pennsylvania

Curated by ChEMBL
LigandPNGBDBM172038(US10647700, Compound EPZ6438 | BDBM190183 | US1015...)
Affinity DataIC50: 2.5nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
University of Pennsylvania

Curated by ChEMBL
LigandPNGBDBM172038(US10647700, Compound EPZ6438 | BDBM190183 | US1015...)
Affinity DataIC50: 2.20nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
University of Pennsylvania

Curated by ChEMBL
LigandPNGBDBM172038(US10647700, Compound EPZ6438 | BDBM190183 | US1015...)
Affinity DataIC50: 4.30nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
University of Pennsylvania

Curated by ChEMBL
LigandPNGBDBM172038(US10647700, Compound EPZ6438 | BDBM190183 | US1015...)
Affinity DataIC50: 1.70nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetHistone-lysine N-methyltransferase EZH1(Human)
Hanmi Pharmaceutical

US Patent
LigandPNGBDBM172038(US10647700, Compound EPZ6438 | BDBM190183 | US1015...)
Affinity DataIC50: 93nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
University of Pennsylvania

Curated by ChEMBL
LigandPNGBDBM172038(US10647700, Compound EPZ6438 | BDBM190183 | US1015...)
Affinity DataIC50: 1.90nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
University of Pennsylvania

Curated by ChEMBL
LigandPNGBDBM172038(US10647700, Compound EPZ6438 | BDBM190183 | US1015...)
Affinity DataIC50: 1.20nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
University of Pennsylvania

Curated by ChEMBL
LigandPNGBDBM172038(US10647700, Compound EPZ6438 | BDBM190183 | US1015...)
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
In Depth
Date in BDB:
8/23/2022
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
University of Pennsylvania

Curated by ChEMBL
LigandPNGBDBM172038(US10647700, Compound EPZ6438 | BDBM190183 | US1015...)
Affinity DataIC50: 170nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/12/2025
Entry Details
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
University of Pennsylvania

Curated by ChEMBL
LigandPNGBDBM172038(US10647700, Compound EPZ6438 | BDBM190183 | US1015...)
Affinity DataIC50: 1.60nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/12/2025
Entry Details
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
University of Pennsylvania

Curated by ChEMBL
LigandPNGBDBM172038(US10647700, Compound EPZ6438 | BDBM190183 | US1015...)
Affinity DataIC50: 1.20nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/12/2025
Entry Details
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
University of Pennsylvania

Curated by ChEMBL
LigandPNGBDBM172038(US10647700, Compound EPZ6438 | BDBM190183 | US1015...)
Affinity DataIC50: 17nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/11/2025
Entry Details
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
University of Pennsylvania

Curated by ChEMBL
LigandPNGBDBM172038(US10647700, Compound EPZ6438 | BDBM190183 | US1015...)
Affinity DataKd:  9.10nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/11/2025
Entry Details
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
University of Pennsylvania

Curated by ChEMBL
LigandPNGBDBM172038(US10647700, Compound EPZ6438 | BDBM190183 | US1015...)
Affinity DataIC50: 11nMAssay Description:Inhibition of EZH2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/19/2024
Entry Details
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
University of Pennsylvania

Curated by ChEMBL
LigandPNGBDBM172038(US10647700, Compound EPZ6438 | BDBM190183 | US1015...)
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
In Depth
Date in BDB:
12/17/2024
Entry Details
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
University of Pennsylvania

Curated by ChEMBL
LigandPNGBDBM172038(US10647700, Compound EPZ6438 | BDBM190183 | US1015...)
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
In Depth
Date in BDB:
12/13/2024
Entry Details
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
University of Pennsylvania

Curated by ChEMBL
LigandPNGBDBM172038(US10647700, Compound EPZ6438 | BDBM190183 | US1015...)
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
In Depth
Date in BDB:
7/3/2017
Entry Details
Go to US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
University of Pennsylvania

Curated by ChEMBL
LigandPNGBDBM172038(US10647700, Compound EPZ6438 | BDBM190183 | US1015...)
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
In Depth
Date in BDB:
8/23/2022
Entry Details Article
PubMed
LigandPNGBDBM172038(US10647700, Compound EPZ6438 | BDBM190183 | US1015...)
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
In Depth
Date in BDB:
4/9/2019
Entry Details
Go to US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
University of Pennsylvania

Curated by ChEMBL
LigandPNGBDBM172038(US10647700, Compound EPZ6438 | BDBM190183 | US1015...)
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
In Depth
Date in BDB:
4/9/2019
Entry Details
Go to US Patent

LigandPNGBDBM172038(US10647700, Compound EPZ6438 | BDBM190183 | US1015...)
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
In Depth
Date in BDB:
4/9/2019
Entry Details
Go to US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
University of Pennsylvania

Curated by ChEMBL
LigandPNGBDBM172038(US10647700, Compound EPZ6438 | BDBM190183 | US1015...)
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
In Depth
Date in BDB:
4/9/2019
Entry Details
Go to US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
University of Pennsylvania

Curated by ChEMBL
LigandPNGBDBM172038(US10647700, Compound EPZ6438 | BDBM190183 | US1015...)
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
In Depth
Date in BDB:
6/24/2017
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
University of Pennsylvania

Curated by ChEMBL
LigandPNGBDBM172038(US10647700, Compound EPZ6438 | BDBM190183 | US1015...)
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
In Depth
Date in BDB:
11/17/2016
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
University of Pennsylvania

Curated by ChEMBL
LigandPNGBDBM172038(US10647700, Compound EPZ6438 | BDBM190183 | US1015...)
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
In Depth
Date in BDB:
11/17/2016
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
University of Pennsylvania

Curated by ChEMBL
LigandPNGBDBM172038(US10647700, Compound EPZ6438 | BDBM190183 | US1015...)
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
In Depth
Date in BDB:
11/17/2016
Entry Details Article
PubMed
TargetPolycomb protein EED(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM172038(US10647700, Compound EPZ6438 | BDBM190183 | US1015...)
Affinity DataIC50: 40nMAssay Description:Inhibition of EED in human G401 cells assessed as reduction in global H3K27me3 level after 48 hrs by ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/12/2019
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
University of Pennsylvania

Curated by ChEMBL
LigandPNGBDBM172038(US10647700, Compound EPZ6438 | BDBM190183 | US1015...)
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
In Depth
Date in BDB:
7/3/2017
Entry Details
Go to US Patent

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