BDBM50075071 CHEMBL3414619

SMILES CCCc1cc(C)[nH]c(=O)c1CNC(=O)c1cc(cc2n(ncc12)C(C)C)-c1ccc(nc1)N1CCN(CC1)C(C)C

InChI Key InChIKey=DPJNKUOXBZSZAI-UHFFFAOYSA-N

Data  1 KI  12 IC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 13 hits for monomerid = 50075071   

TargetHistone-lysine N-methyltransferase EZH2(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50075071(CHEMBL3414619)
Affinity DataIC50: 124nMAssay Description:Inhibition of EZH2 in human MCF10A cells assessed as reduction of H3K27me3 level after 72 hrs by Western blot analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50075071(CHEMBL3414619)
Affinity DataIC50: 10nMAssay Description:Inhibition of EZH2 (unknown origin) using biotinylated-histone H3 (1 to 24) as substrate after 1 hr by scintillation proximity assay in presence of [...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH1(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50075071(CHEMBL3414619)
Affinity DataIC50: 69nMAssay Description:Inhibition of EZH1 histone methyltransferase activity of EZH1/EED/SUZ12/RBBP4/AEBP2 protein complex (unknown origin) using histone H3 peptide as subs...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/2/2021
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50075071(CHEMBL3414619)
Affinity DataIC50: 10nMAssay Description:Inhibition of EZH2 histone methyltransferase activity of EZH2/EED/SUZ12 protein complex (unknown origin) using histone H3 peptide as substrate (21 to...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/2/2021
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50075071(CHEMBL3414619)
Affinity DataIC50: 2nMAssay Description:Inhibition of EZH2 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)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50075071(CHEMBL3414619)
Affinity DataIC50: 10nMAssay 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 EZH1(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50075071(CHEMBL3414619)
Affinity DataIC50: 45nMAssay Description:Inhibition of human recombinant full length EZH1 measured after 30 mins by scintillation proximity assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/19/2024
Entry Details
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50075071(CHEMBL3414619)
Affinity DataIC50: 10nMAssay Description:Inhibition of human EZH2 using core histone as substrate incubated for 1 hr by fluorescence based assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/19/2024
Entry Details
PubMed
TargetHistone-lysine N-methyltransferase EZH1(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50075071(CHEMBL3414619)
Affinity DataIC50: 45nMAssay Description:Inhibition of wildtype EZH1 expressed in human MCF-10A cells assessed as reduction in H3K27me3 level incubated for 1 hr by Western blot analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/19/2024
Entry Details
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50075071(CHEMBL3414619)
Affinity DataIC50: 10nMAssay Description:Inhibition of human EZH2 in human MCF-10A cells assessed as reduction in H3K27me3 levels incubated for 72 hrs by Western blot analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/19/2024
Entry Details
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50075071(CHEMBL3414619)
Affinity DataIC50: 10nMAssay Description:Inhibition of EZH2 (unknown origin) in PRC2 complex using H3 (1 to 24 residues) and 3H-SAM as substrate incubated for 1 hrs by Scintillation proximit...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/19/2024
Entry Details
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50075071(CHEMBL3414619)
Affinity DataIC50: 124nMAssay Description:Inhibition of human EZH2 in human MCF-10A cells assessed as reduction in H3K27me3 levels incubated for 72 hrs by In-cell western assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/19/2024
Entry Details
PubMed
TargetHistone-lysine N-methyltransferase EZH2(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50075071(CHEMBL3414619)
Affinity DataKi:  4.60nMAssay Description:Competitive inhibition of EZH2 (unknown origin) using biotinylated-histone H3 (1 to 24) as substrate by Lineweaver-Burk plot analysis in presence of ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMed