BDBM50075051 CHEMBL3360855::EPZ005687::US10273223, Compound C-1::US9175331, 7::US9637472, Compound C-1

SMILES Cc1cc(C)c(CNC(=O)c2cc(cc3n(ncc23)C2CCCC2)-c2ccc(CN3CCOCC3)cc2)c(=O)[nH]1

InChI Key InChIKey=ZOIBZSZLMJDVDQ-UHFFFAOYSA-N

Data  2 KI  16 IC50  1 EC50

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

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 19 hits for monomerid = 50075051   

TargetHistone-lysine N-methyltransferase EZH2(Human)
Epizyme

US Patent
LigandPNGBDBM50075051(CHEMBL3360855 | US9175331, 7 | EPZ005687 | US96374...)
Affinity DataIC50: 300nMAssay Description:eneral Procedure for Wild-Type PRC2 Enzyme Assay on Oligonucleosome Substrate. The assays was performed in a buffer consisting of 20 mM bicine (pH=7....More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/20/2020
Entry Details
Go to US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Epizyme

US Patent
LigandPNGBDBM50075051(CHEMBL3360855 | US9175331, 7 | EPZ005687 | US96374...)
Affinity DataIC50: 54nMAssay Description:Inhibition of C-terminal recombinant human EZH2More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/19/2024
Entry Details
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Epizyme

US Patent
LigandPNGBDBM50075051(CHEMBL3360855 | US9175331, 7 | EPZ005687 | US96374...)
Affinity DataIC50: 54nMAssay 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 EZH2(Human)
Epizyme

US Patent
LigandPNGBDBM50075051(CHEMBL3360855 | US9175331, 7 | EPZ005687 | US96374...)
Affinity DataIC50: 2.90E+3nMAssay Description:Inhibition of EZH2 in human OCILY19 cells assessed as reduction in H3K27me3 level treated for 96 hrs by 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)
Epizyme

US Patent
LigandPNGBDBM50075051(CHEMBL3360855 | US9175331, 7 | EPZ005687 | US96374...)
Affinity DataIC50: 54nMAssay 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)
Epizyme

US Patent
LigandPNGBDBM50075051(CHEMBL3360855 | US9175331, 7 | EPZ005687 | US96374...)
Affinity DataIC50: 54nMAssay 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)
Epizyme

US Patent
LigandPNGBDBM50075051(CHEMBL3360855 | US9175331, 7 | EPZ005687 | US96374...)
Affinity DataIC50: 54nMAssay Description:Inhibition of EZH2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/22/2023
Entry Details
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Epizyme

US Patent
LigandPNGBDBM50075051(CHEMBL3360855 | US9175331, 7 | EPZ005687 | US96374...)
Affinity DataIC50: 54nMAssay Description:Inhibition of EZH2 in human PRC2 complex preincubated for 30 mins followed by histone h3 peptide (21 to 44 residues) and S-adenosylmethionine and mea...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/29/2022
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH1(Human)
Northwestern University

Curated by ChEMBL
LigandPNGBDBM50075051(CHEMBL3360855 | US9175331, 7 | EPZ005687 | US96374...)
Affinity DataIC50: 45nMAssay Description:Inhibition of EZH1 in PRC2 complex (unknown origin) using biotinylated peptide as substrate in presence of S-adenosylmethionineMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/29/2022
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Epizyme

US Patent
LigandPNGBDBM50075051(CHEMBL3360855 | US9175331, 7 | EPZ005687 | US96374...)
Affinity DataIC50: 95nMAssay 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
In Depth
Date in BDB:
8/8/2016
Entry Details
Go to US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Epizyme

US Patent
LigandPNGBDBM50075051(CHEMBL3360855 | US9175331, 7 | EPZ005687 | US96374...)
Affinity DataIC50: 300nMAssay Description:Recombinant PRC2 Enzymes. Human PRC2 enzymes were purified as 4-component enzyme complexes co-expressed in Spodoptera frugiperda (sf9) cells using a ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/29/2019
Entry Details
Go to US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Epizyme

US Patent
LigandPNGBDBM50075051(CHEMBL3360855 | US9175331, 7 | EPZ005687 | US96374...)
Affinity DataEC50:  2.90E+3nMAssay 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)
Epizyme

US Patent
LigandPNGBDBM50075051(CHEMBL3360855 | US9175331, 7 | EPZ005687 | US96374...)
Affinity DataIC50: 80nMAssay Description:Inhibition of wild-type EZH2 in human OCI-LY19 cells assessed as reduction of H3K27me3 level after 96 hrs by ELISA assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Epizyme

US Patent
LigandPNGBDBM50075051(CHEMBL3360855 | US9175331, 7 | EPZ005687 | US96374...)
Affinity DataIC50: 5.40E+4nMAssay Description:Inhibition of human EZH2 using SAM and histone H3 (16 to 30) as substrate preincubated for 30 mins followed by substrate addition measured after 90 m...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMed
LigandPNGBDBM50075051(CHEMBL3360855 | US9175331, 7 | EPZ005687 | US96374...)
Affinity DataIC50: 8.20nMAssay 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
In Depth
Date in BDB:
8/8/2016
Entry Details
Go to US Patent

LigandPNGBDBM50075051(CHEMBL3360855 | US9175331, 7 | EPZ005687 | US96374...)
Affinity DataIC50: 11.3nMAssay 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
In Depth
Date in BDB:
8/8/2016
Entry Details
Go to US Patent

LigandPNGBDBM50075051(CHEMBL3360855 | US9175331, 7 | EPZ005687 | US96374...)
Affinity DataIC50: 75nMAssay 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
In Depth
Date in BDB:
8/8/2016
Entry Details
Go to US Patent

TargetHistone-lysine N-methyltransferase EZH2(Human)
Epizyme

US Patent
LigandPNGBDBM50075051(CHEMBL3360855 | US9175331, 7 | EPZ005687 | US96374...)
Affinity DataKi:  24nMAssay Description:Competitive inhibition of wild type EZH2 in human PRC2 complex using S-adenosylmethionine as substrate by Michaelis-Menten plot analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/29/2022
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Epizyme

US Patent
LigandPNGBDBM50075051(CHEMBL3360855 | US9175331, 7 | EPZ005687 | US96374...)
Affinity DataKi:  24nMAssay Description:Competitive inhibition of human EZH2 using SAM and histone H3 (16 to 30) as substrate preincubated for 30 mins followed by substrate addition measure...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMed