Compile Data Set for Download or QSAR
Report error Found 72 Enz. Inhib. hit(s) with all data for entry = 50045685
TargetHistone-lysine N-methyltransferase EZH2(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50010823(CHEMBL3264787)
Affinity DataEC50:  7.00E+3nMAssay Description:Inhibition of EZH2 in human HeLa cells assessed as reduction of H3K27me3 and H3K27me2 level after 96 hrs by ELISA methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMed
TargetProtein arginine N-methyltransferase 3 [N508S](Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50427768(CHEMBL2325441)
Affinity DataKd:  9.50E+3nMAssay Description:Binding affinity to 6xHis-tagged recombinant human PRMT3 by surface plasmon resonance analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetN-lysine methyltransferase SMYD2(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50396022(CHEMBL2169920)
Affinity DataKd:  500nMAssay Description:Binding affinity to recombinant human full-length SMYD2 (1 to 433) by ITC analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetHistone-lysine N-methyltransferase EHMT1(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50396024(CHEMBL1232453)
Affinity DataKd:  136nMAssay Description:Binding affinity to recombinant human GLP (951 to 1235) by isothermal titration calorimetric analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50443016(CHEMBL3087498)
Affinity DataKd:  0.0600nMAssay Description:Binding affinity to DOT1L (unknown origin) by surface plasmon resonance analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50396023(CHEMBL2169919)
Affinity DataKd:  0.25nMAssay Description:Binding affinity to DOT1L (unknown origin) by surface plasmon resonance analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50396023(CHEMBL2169919)
Affinity DataIC50: 0.400nMAssay Description:Inhibition of recombinant human DOT1L (1 to 416) using [3H]-SAM, SAM and nucleosome as substrate assessed as incorporation of radioactivity into nucl...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetHistone-lysine N-methyltransferase SETD7(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50075073(CHEMBL3414622)
Affinity DataIC50: 2nMAssay Description:Inhibition of full-length human SETD7 expressed in Escherichia coli BL21 (DE3) using biotinylated histone H3 (1 to 25) as substrate after 1 hr by Fla...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50075098(CHEMBL3414626 | US9446064, A2 | US10143704, Compou...)
Affinity DataIC50: 3nMAssay Description:Inhibition of DOT1L in human MV4-11 cells expressing MLL-AF4 assessed as reduction of H3K79me2 level after 4 days by ELISA methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50075098(CHEMBL3414626 | US9446064, A2 | US10143704, Compou...)
Affinity DataIC50: 3.5nMAssay Description:Inhibition of DOT1L in human MV4-11 cells expressing MLL-AF4 assessed as cell growth inhibition after 14 days by Guava Viacount assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50443016(CHEMBL3087498)
Affinity DataIC50: 8.80nMAssay Description:Inhibition of DOT1L in human MCF10A cells assessed as reduction of H3K79 levelMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
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 EZH2(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50075054(CHEMBL3414574)
Affinity DataIC50: 13nMAssay Description:Inhibition of N-terminal FLAG tagged human EZH2 Y641F mutant expressed in baculovirus infected Sf9 cells using H3K27 as substrate after 120 mins by m...More 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
LigandPNGBDBM50075054(CHEMBL3414574)
Affinity DataIC50: 15nMAssay Description:Inhibition of N-terminal FLAG tagged full-length human EZH2 expressed in baculovirus infected Sf9 cells using H3K27 as substrate after 120 mins by ma...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMed
TargetN-lysine methyltransferase SMYD2(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50075102(CHEMBL3414623)
Affinity DataIC50: 15nMAssay Description:Inhibition of SMYD2 (unknown origin)More 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
LigandPNGBDBM50075074(CHEMBL3414629)
Affinity DataIC50: 17nMAssay 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 EZH2(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50075072(CHEMBL3414620)
Affinity DataIC50: 21nMAssay 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, H3 lysine-79 specific(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50443025(CHEMBL3087638)
Affinity DataIC50: 38nMAssay Description:Inhibition of human DOT1L (1 to 472) using [3H]-SAM/oligo-nucleosome as substrate preincubated for 10 mins followed by substrate addition measured af...More 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
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, H3 lysine-79 specific(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50396023(CHEMBL2169919)
Affinity DataIC50: 84nMAssay Description:Inhibition of DOT1L in human MCF10A cells assessed as reduction of H3K79 levelMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetHistone-lysine N-methyltransferase EHMT1(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50396024(CHEMBL1232453)
Affinity DataIC50: 100nMAssay Description:Inhibition of recombinant human GLP (951 to 1235) using Histone H3 peptide (1 to 15) as substrate preincubated on ice for 10 mins followed by 5 mins ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetN-lysine methyltransferase SMYD2(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50396022(CHEMBL2169920)
Affinity DataIC50: 120nMAssay Description:Inhibition of recombinant human full-length SMYD2 (1 to 433) using biotin-aminohexanoyl GSRAHSSHLKSKKGQSTSRH as substrate after 75 mins by AlphaScree...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
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
TargetN-lysine methyltransferase KMT5A(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50106497(NSC-663284 | 6-Chloro-7-(2-morpholin-4-yl-ethylami...)
Affinity DataIC50: 210nMAssay Description:Inhibition of N-terminal His6-tagged human SETD8 (191 to 352) assessed as incorporation of [3H]-methyl group from [3H-Me]-SAM to biotinylated H4K20 p...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMed
TargetN-lysine methyltransferase KMT5A(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50075100(CHEMBL3414625)
Affinity DataIC50: 500nMAssay Description:Inhibition of N-terminal His6-tagged human SETD8 (191 to 352) assessed as incorporation of [3H]-methyl group from [3H-Me]-SAM to biotinylated H4K20 p...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMed
TargetN-lysine methyltransferase SMYD2(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50075102(CHEMBL3414623)
Affinity DataIC50: 600nMAssay Description:Inhibition of SMYD2 in human KYSE-150 cells assessed as reduction of monomethylation of p53 K370 by sandwich ELISA methodMore 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
LigandPNGBDBM325835(US9637472, Compound A-29 | US10273223, Compound A-...)
Affinity DataIC50: 620nMAssay 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
TargetHistone-lysine N-methyltransferase EHMT1(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50300028(N-(1-benzylpiperidin-4-yl)-6,7-dimethoxy-2-(4-meth...)
Affinity DataIC50: 700nMAssay Description:Inhibition of N-terminal hexahistidine-tagged SET domain of human GLP (951 to 1235) expressed in Escherichia coli BL21 (DE3) using Histone H3 peptide...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMed
TargetN-lysine methyltransferase KMT5A(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50075099(TCMDC-124224 | CHEMBL580421)
Affinity DataIC50: 700nMAssay Description:Inhibition of N-terminal His6-tagged human SETD8 (191 to 352) assessed as incorporation of [3H]-methyl group from [3H-Me]-SAM to biotinylated H4K20 p...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase SETD2(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50075101(CHEMBL3414624)
Affinity DataIC50: 800nMAssay Description:Inhibition of human SETD2 (1347 to 1711) using histamine H3 (20 to 50) as substrate assessed as transfer of [3H]-Me of [3H-Me]-SAM to peptide substra...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetProtein arginine N-methyltransferase 3 [N508S](Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50427768(CHEMBL2325441)
Affinity DataIC50: 1.60E+3nMAssay Description:Inhibition of recombinant human PRMT3 (211 to 531) using histone-4 (1 to 24) as substrate by S-adenosylhomocysteine hydrolase-coupled assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetHistone-lysine N-methyltransferase EHMT2(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50396029(CHEMBL1222849)
Affinity DataIC50: 1.70E+3nMAssay Description:Inhibition of G9a (unknown origin) using SAM/biotinylated H3 as substrate preincubated for 1 hr followed by substrate addition measured after 2 hrs b...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EHMT2(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50300028(N-(1-benzylpiperidin-4-yl)-6,7-dimethoxy-2-(4-meth...)
Affinity DataIC50: 1.70E+3nMAssay Description:Inhibition of G9a (685 to 1000) (unknown origin) assessed as H3K9me2 level by mass spectrophotometric analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EHMT2(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50300028(N-(1-benzylpiperidin-4-yl)-6,7-dimethoxy-2-(4-meth...)
Affinity DataIC50: 1.90E+3nMAssay Description:Inhibition of N-terminal hexahistidine-tagged SET domain of human G9a (913 to 1193) expressed in Escherichia coli BL21 (DE3) using Histone H3 peptide...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase SETD7(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50075101(CHEMBL3414624)
Affinity DataIC50: 2.20E+3nMAssay Description:Inhibition of full-length human SETD7 using histamine H3 (1 to 21) as substrate assessed as transfer of [3H]-Me of [3H-Me]-SAM to peptide substrate a...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EHMT2(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50315537(chaetocin | CHEMBL1089316)
Affinity DataIC50: 2.50E+3nMAssay Description:Inhibition of G9a (unknown origin) using SAM/biotinylated H3 as substrate preincubated for 1 hr followed by substrate addition measured after 2 hrs b...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMed
TargetHistone-arginine methyltransferase CARM1(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50075097(CHEMBL3414627)
Affinity DataIC50: 2.60E+3nMAssay Description:Inhibition of recombinant human GST-tagged CARM1More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMed
TargetHistone-arginine methyltransferase CARM1(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50075101(CHEMBL3414624)
Affinity DataIC50: 3.00E+3nMAssay Description:Inhibition of human CARM1 (19 to 608) using histamine H3 (1 to 40) as substrate assessed as transfer of [3H]-Me of [3H-Me]-SAM to peptide substrate a...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMed
TargetProtein arginine N-methyltransferase 1 [11-371](Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50075075(CHEMBL3414628)
Affinity DataIC50: 3.90E+3nMAssay Description:Inhibition of recombinant GST-tagged PRMT1 (unknown origin) using GST-P3 as substrate after 90 mins by scintillation counting analysis in presence of...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMed
TargetProtein arginine N-methyltransferase 1 [11-371](Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50075097(CHEMBL3414627)
Affinity DataIC50: 4.20E+3nMAssay Description:Inhibition of recombinant human GST-tagged PRMT1 using GST-Npl3 as substrateMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EHMT2(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50075052(CHEMBL3414617)
Affinity DataIC50: 6.30E+3nMAssay Description:Inhibition of G9a (unknown origin) by mass spectrophotometric analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMed
TargetN-lysine methyltransferase KMT5A(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50051116(CHEMBL3318284)
Affinity DataIC50: 6.50E+3nMAssay Description:Inhibition of SETD8 (unknown origin) using H4 (1 to 24) as substrate assessed as incorporation of [3H]-methyl group from [3H-Me]-SAM to peptide subst...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMed
TargetProtein arginine N-methyltransferase 1 [11-371](Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50446401(CHEMBL3109656)
Affinity DataIC50: 8.80E+3nMAssay Description:Inhibition of recombinant human PRMT1 using GST-Npl3 as substrate incubated for 15 mins prior to protein addition measured after 1 hr by colorimetric...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMed
TargetProtein arginine N-methyltransferase 1 [11-371](Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50075101(CHEMBL3414624)
Affinity DataIC50: 9.50E+3nMAssay Description:Inhibition of human PRMT1 (10 to 352) using RGG peptide as substrate assessed as transfer of [3H]-Me of [3H-Me]-SAM to peptide substrate after 1.5 hr...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EHMT1(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50300028(N-(1-benzylpiperidin-4-yl)-6,7-dimethoxy-2-(4-meth...)
Affinity DataIC50: 3.80E+4nMAssay Description:Inhibition of GLP (610 to 917) (unknown origin) assessed as H3K9me2 level by mass spectrophotometric analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EHMT2(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50425312(CHEMBL2315527)
Affinity DataIC50: 5.00E+4nMAssay Description:Inhibition of G9a (unknown origin) using SAM/biotinylated H3 as substrate preincubated for 1 hr followed by substrate addition measured after 2 hrs b...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMed
TargetHistone-lysine N-methyltransferase EHMT2(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50396028(CHEMBL1222848)
Affinity DataIC50: 5.00E+4nMAssay Description:Inhibition of G9a (unknown origin) using SAM/biotinylated H3 as substrate preincubated for 1 hr followed by substrate addition measured after 2 hrs b...More 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
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
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50075098(CHEMBL3414626 | US9446064, A2 | US10143704, Compou...)
Affinity DataKi:  0.0800nMAssay Description:Inhibition of human DOT1L using oligo-nucleosome/[3H]-SAM as substrate preincubated for 30 mins followed by substrate addition measured after 120 min...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetHistone-lysine N-methyltransferase, H3 lysine-79 specific(Human)
Icahn School of Medicine At Mount Sinai

Curated by ChEMBL
LigandPNGBDBM50396023(CHEMBL2169919)
Affinity DataKi:  0.300nMAssay Description:Inhibition of human DOT1L using oligo-nucleosome/[3H]-SAM as substrate preincubated for 30 mins followed by substrate addition measured after 120 min...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
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