Report error Found 27 Enz. Inhib. hit(s) with Target = 'Histone-lysine N-methyltransferase SETDB1'
Affinity DataKd: 80nMAssay Description:Binding affinity N-terminal his tagged wild type human SETDB1 (190 to 410 residues ) expressed in Escherichia coli BL21 (DE3) assessed as dissociatio...More data for this Ligand-Target Pair
Affinity DataKd: 210nMAssay Description:Binding affinity N-terminal his tagged wild type human SETDB1 (190 to 410 residues ) expressed in Escherichia coli BL21 (DE3) assessed as dissociatio...More data for this Ligand-Target Pair
Affinity DataKd: 232nMAssay Description:Binding affinity to SETDB1 (unknown origin) assessed as dissociation constant by surface plasmon resonance analysisMore data for this Ligand-Target Pair
Affinity DataKd: 1.60E+3nMAssay Description:Binding affinity N-terminal his tagged wild type human SETDB1 (190 to 410 residues ) expressed in Escherichia coli BL21 (DE3) assessed as dissociatio...More data for this Ligand-Target Pair
Affinity DataIC50: 2.20E+3nMAssay Description:Inhibition of SETDB1 (unknown origin) by HMT assayMore data for this Ligand-Target Pair
Affinity DataKd: 3.26E+3nMAssay Description:Binding affinity to SETDB1 (unknown origin) assessed as dissociation constant by surface plasmon resonance analysisMore data for this Ligand-Target Pair
Affinity DataKd: 4.40E+3nMAssay Description:Binding affinity N-terminal his tagged wild type human SETDB1 (190 to 410 residues ) expressed in Escherichia coli BL21 (DE3) assessed as dissociatio...More data for this Ligand-Target Pair
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of human SETDB1 expressed in sf9 insect cells assessed as reduction in methylated histone H3 full length level using histone H3 full lengt...More data for this Ligand-Target Pair
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of human SETDB1 expressed in sf9 insect cells assessed as reduction in methylated histone H3 full length level using histone H3 full lengt...More data for this Ligand-Target Pair
Affinity DataIC50: 6.50E+4nMAssay Description:Inhibition of SETDB1 (unknown origin) using histone H3 as substrate measured after 1.5 hrs by SpectraMax microplate reader analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 1.00E+5nMAssay Description:All HMT reactions were performed as described previously [Nasveschuk et al., ACS Med. Chem. Lett., 5:378-383].More data for this Ligand-Target Pair
Affinity DataIC50: 1.00E+5nMAssay Description:Displacement of Biotin-p53K381acK382me2 from SETDB1 tandem tudor domain (unknown origin) by TR-FRET assayMore data for this Ligand-Target Pair
Affinity DataIC50: 1.00E+5nMAssay Description:Inhibition of SETDB1 (unknown origin) using [3H-SAM] as substrate incubated for 1 hr by scintillation proximity assayMore data for this Ligand-Target Pair
Affinity DataIC50: 1.00E+5nMAssay Description:Displacement of Biotin-p53K381acK382me2 from SETDB1 tandem tudor domain (unknown origin) by TR-FRET assayMore data for this Ligand-Target Pair
Affinity DataIC50: 1.00E+5nMAssay Description:Inhibition of SETDB1 (unknown origin) assessed as incorporation of tritium-labeled methyl group to lysine or arginine residues of peptide substrate b...More data for this Ligand-Target Pair
Affinity DataIC50: 1.00E+5nMAssay Description:Inhibition of SETDB1 (unknown origin) by HMT assayMore data for this Ligand-Target Pair
Affinity DataIC50: 7.50E+5nMAssay Description:Inhibition of GST tagged human SETDB1 (190 to 410 residues ) expressed in Escherichia coli BL21 (DE3) assessed as inhibition of H3K9me2 measured afte...More data for this Ligand-Target Pair
Affinity DataIC50: 9.30E+5nMAssay Description:Inhibition of GST tagged human SETDB1 (190 to 410 residues ) expressed in Escherichia coli BL21 (DE3) assessed as inhibition of H3K9me3 measured afte...More data for this Ligand-Target Pair
Affinity DataKd: 1.27E+6nMAssay Description:Binding affinity to N-terminally biotinylated human SETDB1 Tudor domain (197 to 403 residues) expressed in Escherichia coli BL21(DE3)-pRARE2 cells by...More data for this Ligand-Target Pair
Affinity DataKd: 2.50E+6nMAssay Description:Binding affinity to N-terminally biotinylated human SETDB1 Tudor domain (197 to 403 residues) expressed in Escherichia coli BL21(DE3)-pRARE2 cells by...More data for this Ligand-Target Pair
Affinity DataKd: 2.70E+6nMAssay Description:Binding affinity to N-terminally biotinylated human SETDB1 Tudor domain (197 to 403 residues) expressed in Escherichia coli BL21(DE3)-pRARE2 cells by...More data for this Ligand-Target Pair
Affinity DataKd: 3.50E+6nMAssay Description:Binding affinity to N-terminal His6-tagged human SETDB1 Tudor domain (197 to 403 residues) expressed in Escherichia coli BL21(DE3)-pRARE2 cells by IT...More data for this Ligand-Target Pair
Affinity DataKd: 3.50E+6nMAssay Description:Binding affinity to N-terminally biotinylated human SETDB1 Tudor domain (197 to 403 residues) expressed in Escherichia coli BL21(DE3)-pRARE2 cells by...More data for this Ligand-Target Pair
Affinity DataKd: 4.00E+6nMAssay Description:Binding affinity to N-terminally biotinylated human SETDB1 Tudor domain (197 to 403 residues) expressed in Escherichia coli BL21(DE3)-pRARE2 cells by...More data for this Ligand-Target Pair
Affinity DataKd: 4.00E+6nMAssay Description:Binding affinity to N-terminal His6-tagged human SETDB1 Tudor domain (197 to 403 residues) expressed in Escherichia coli BL21(DE3)-pRARE2 cells by IT...More data for this Ligand-Target Pair
Affinity DataKd: 7.70E+6nMAssay Description:Binding affinity to N-terminally biotinylated human SETDB1 Tudor domain (197 to 403 residues) expressed in Escherichia coli BL21(DE3)-pRARE2 cells by...More data for this Ligand-Target Pair
Affinity DataKd: 1.00E+7nMAssay Description:Binding affinity to N-terminally biotinylated human SETDB1 Tudor domain (197 to 403 residues) expressed in Escherichia coli BL21(DE3)-pRARE2 cells by...More data for this Ligand-Target Pair

3D Structure (crystal)



















