BDBM190179 EPZ005030::US10273223, Compound A-2::US9175331, 4::US9637472, Compound A-2

SMILES CC(C)n1ncc2c(cc(nc12)-c1ccc(CN2CCOCC2)cc1)C(=O)NCc1c(C)cc(C)[nH]c1=O

InChI Key InChIKey=WGDUEUOSWFHQIH-UHFFFAOYSA-N

Data  1 KI  8 IC50  1 EC50

  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 10 hits for monomerid = 190179   

TargetHistone-lysine N-methyltransferase EZH2(Human)
Epizyme

US Patent
LigandPNGBDBM190179(US9175331, 4 | EPZ005030 | US9637472, Compound A-2...)
Affinity DataIC50: 260nMAssay 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

LigandPNGBDBM190179(US9175331, 4 | EPZ005030 | US9637472, Compound A-2...)
Affinity DataIC50: 185nMAssay 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

LigandPNGBDBM190179(US9175331, 4 | EPZ005030 | US9637472, Compound A-2...)
Affinity DataIC50: 41.8nMAssay 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

LigandPNGBDBM190179(US9175331, 4 | EPZ005030 | US9637472, Compound A-2...)
Affinity DataIC50: 50.4nMAssay 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
LigandPNGBDBM190179(US9175331, 4 | EPZ005030 | US9637472, Compound A-2...)
Affinity DataEC50:  1.05E+4nMAssay 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
LigandPNGBDBM190179(US9175331, 4 | EPZ005030 | US9637472, Compound A-2...)
Affinity DataIC50: 3.00E+3nMAssay Description:Inhibition of methyltransferase activity of EZH2 in human lymphoma cells assessed as H3K27 methylationMore 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
LigandPNGBDBM190179(US9175331, 4 | EPZ005030 | US9637472, Compound A-2...)
Affinity DataIC50: 400nMAssay Description:Inhibition of methyltransferase activity of human EZH2 using chicken oligonucleotide as substrate by pull down assayMore 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
LigandPNGBDBM190179(US9175331, 4 | EPZ005030 | US9637472, Compound A-2...)
Affinity DataIC50: 650nMAssay 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
LigandPNGBDBM190179(US9175331, 4 | EPZ005030 | US9637472, Compound A-2...)
Affinity DataIC50: 650nMAssay 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
LigandPNGBDBM190179(US9175331, 4 | EPZ005030 | US9637472, Compound A-2...)
Affinity DataKi:  180nMAssay Description:Inhibition of wild type EZH2 in human PRC2 complex using S-adenosylmethionine and biotinylated histone peptides as substrateMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/29/2022
Entry Details Article
PubMed