BDBM50300028 CHEMBL569864::N-(1-benzylpiperidin-4-yl)-6,7-dimethoxy-2-(4-methyl-1,4-diazepan-1-yl)quinazolin-4-amine
SMILES COc1cc2nc(nc(NC3CCN(Cc4ccccc4)CC3)c2cc1OC)N1CCCN(C)CC1
InChI Key InChIKey=OSXFATOLZGZLSK-UHFFFAOYSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 32 hits for monomerid = 50300028
TargetHistone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
University Of North Carolina
Curated by ChEMBL
University Of North Carolina
Curated by ChEMBL
Affinity DataIC50: 1.70E+3nMAssay Description:Inhibition of G9aMore data for this Ligand-Target Pair
TargetDNA (cytosine-5)-methyltransferase 1(Homo sapiens (Human))
University Of Navarra
Curated by ChEMBL
University Of Navarra
Curated by ChEMBL
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of DNMT1 (unknown origin)More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EHMT1(Homo sapiens (Human))
University Of North Carolina
Curated by ChEMBL
University Of North Carolina
Curated by ChEMBL
3D Structure (crystal)TargetHistone-lysine N-methyltransferase EHMT1(Homo sapiens (Human))
University Of North Carolina
Curated by ChEMBL
University Of North Carolina
Curated by ChEMBL
Affinity DataIC50: 34nMAssay Description:Activity at methyl transferase activity GLP by enzyme coupled S-adenocylehomocystein detection assayMore data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EHMT1(Homo sapiens (Human))
University Of North Carolina
Curated by ChEMBL
University Of North Carolina
Curated by ChEMBL
Affinity DataIC50: 27nMAssay Description:Activity at methyl transferase activity GLP by chemiluminescence based oxygen tunneling assayMore data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
University Of North Carolina
Curated by ChEMBL
University Of North Carolina
Curated by ChEMBL
Affinity DataKd: 130nMAssay Description:Binding affinity to G9a by isothermal titration colorimetryMore data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
University Of North Carolina
Curated by ChEMBL
University Of North Carolina
Curated by ChEMBL
Affinity DataIC50: 2.50E+5nMAssay Description:Inhibition of methyl transferase activity of G9a assessed as inhibition of H3K9 methylation by chemiluminescence based oxygen tunneling assayMore data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
University Of North Carolina
Curated by ChEMBL
University Of North Carolina
Curated by ChEMBL
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
TargetHistone-lysine N-methyltransferase EHMT1(Homo sapiens (Human))
University Of North Carolina
Curated by ChEMBL
University Of North Carolina
Curated by ChEMBL
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
TargetHistone-lysine N-methyltransferase EHMT1(Homo sapiens (Human))
University Of North Carolina
Curated by ChEMBL
University Of North Carolina
Curated by ChEMBL
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
TargetHistone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
University Of North Carolina
Curated by ChEMBL
University Of North Carolina
Curated by ChEMBL
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
TargetHistone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
University Of North Carolina
Curated by ChEMBL
University Of North Carolina
Curated by ChEMBL
Affinity DataIC50: 110nMAssay Description:Inhibition of G9a by Alpha screen assayMore data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
University Of North Carolina
Curated by ChEMBL
University Of North Carolina
Curated by ChEMBL
Affinity DataIC50: 1.70E+3nMAssay Description:Inhibition of recombinant G9aMore data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EHMT1(Homo sapiens (Human))
University Of North Carolina
Curated by ChEMBL
University Of North Carolina
Curated by ChEMBL
Affinity DataIC50: 3.80E+4nMAssay Description:Inhibition of Histone H3 lysine 9 of GLP methyltransferaseMore data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
University Of North Carolina
Curated by ChEMBL
University Of North Carolina
Curated by ChEMBL
Affinity DataIC50: 1.80E+5nMAssay Description:Activity at methyl transferase activity G9a by enzyme coupled S-adenocylehomocystein detection assayMore data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
University Of North Carolina
Curated by ChEMBL
University Of North Carolina
Curated by ChEMBL
Affinity DataIC50: 2.70E+3nMAssay Description:Inhibition of lysine methyltransferase G9aMore data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
University Of North Carolina
Curated by ChEMBL
University Of North Carolina
Curated by ChEMBL
Affinity DataIC50: 1.90E+3nMAssay Description:Inhibition of human N-terminal hexahistidine-tagged G9a SET domain amino acid 913 to 1193 expressed in Escherichia coli BL21 (DE3) using Histone H3 p...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EHMT1(Homo sapiens (Human))
University Of North Carolina
Curated by ChEMBL
University Of North Carolina
Curated by ChEMBL
Affinity DataIC50: 700nMAssay Description:Inhibition of human N-terminal hexahistidine-tagged GLP SET domain amino acid 951 to 1235 expressed in Escherichia coli BL21 (DE3) using Histone H3 p...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
University Of North Carolina
Curated by ChEMBL
University Of North Carolina
Curated by ChEMBL
Affinity DataIC50: 1.90E+3nMAssay Description:Inhibition of N-terminal hexahistidine-tagged human G9a (913 to 1193 residues) expressed in Escherichia coli BL21 (DE3)-Gold cells using histone H3 (...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
University Of North Carolina
Curated by ChEMBL
University Of North Carolina
Curated by ChEMBL
Affinity DataIC50: 1.90E+3nMAssay Description:Inhibition of human cytomegalovirus DNA polymerase (95 uL) activity in a solution containing 6.4 mM HEPES (pH 7.5), incubation for 12 minutes at 26 d...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EHMT1(Homo sapiens (Human))
University Of North Carolina
Curated by ChEMBL
University Of North Carolina
Curated by ChEMBL
Affinity DataIC50: 700nMAssay Description:Inhibition of EHMT1 (unknown origin)More data for this Ligand-Target Pair
TargetDNA (cytosine-5)-methyltransferase 1(Homo sapiens (Human))
University Of Navarra
Curated by ChEMBL
University Of Navarra
Curated by ChEMBL
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of human DNMT1 using polydeoxyinosine polydeoxycytosine DNA as substrate after 15 mins in presence of SAM by TR-FRET assayMore data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
University Of North Carolina
Curated by ChEMBL
University Of North Carolina
Curated by ChEMBL
Affinity DataIC50: 1.20E+3nMAssay Description:Inhibition of human G9a using biotinylated-H3K9 peptide as substrate after 1 hr in presence of SAM by TR-FRET assayMore data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
University Of North Carolina
Curated by ChEMBL
University Of North Carolina
Curated by ChEMBL
Affinity DataIC50: 1.90E+3nMAssay Description:Inhibition of G9a (unknown origin) by mas spectrometric methodMore data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
University Of North Carolina
Curated by ChEMBL
University Of North Carolina
Curated by ChEMBL
Affinity DataIC50: 4.56E+3nMAssay Description:Inhibition of G9a in human MDA-MB-231 cells assessed as reduction in H3K9me2 level after 2 days by immunofluorescence in-cell western analysisMore data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
University Of North Carolina
Curated by ChEMBL
University Of North Carolina
Curated by ChEMBL
Affinity DataIC50: 67nMAssay Description:Inhibition of G9a (unknown origin) using [histone H3 1 to 25 residues] and SAM substrate by scintillation proximity assayMore data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
University Of North Carolina
Curated by ChEMBL
University Of North Carolina
Curated by ChEMBL
Affinity DataIC50: 180nMAssay Description:Inhibition of G9a (unknown origin)More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
University Of North Carolina
Curated by ChEMBL
University Of North Carolina
Curated by ChEMBL
Affinity DataIC50: 2.00E+3nMAssay Description:Inhibition of human G9a using core histone H3 as substrate incubated for 1 hr in presence of [3H]-SAM by filter binding methodMore data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
University Of North Carolina
Curated by ChEMBL
University Of North Carolina
Curated by ChEMBL
Affinity DataIC50: 1.90E+3nMAssay Description:Inhibition of recombinant human G9a (685 to 1000 residues) using H3 peptide (1 to 20 residues) by mass spectrometryMore data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EHMT1(Homo sapiens (Human))
University Of North Carolina
Curated by ChEMBL
University Of North Carolina
Curated by ChEMBL
Affinity DataIC50: 700nMAssay Description:Inhibition of recombinant human GLP (610 to 917 residues) using H3 peptide (1 to 20 residues) by mass spectrometryMore data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
University Of North Carolina
Curated by ChEMBL
University Of North Carolina
Curated by ChEMBL
Affinity DataIC50: 1.20E+3nMAssay Description:Inhibition of G9a (685 to 1000 residues) (unknown origin) expressed in Escherichia coli BL21More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EHMT2(Homo sapiens (Human))
University Of North Carolina
Curated by ChEMBL
University Of North Carolina
Curated by ChEMBL
Affinity DataIC50: 290nMAssay Description:Inhibition of G9a by Alpha screen assayMore data for this Ligand-Target Pair