Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB (change energy unit to kcal/mol)
Found 47 hits in this display
BDBM191598(2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-ox...)
BDBM191598(2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-ox...)
BDBM191598(2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-ox...)
BDBM191598(2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-ox...)
IC50: 7nMpH: 7.5Assay Description:The demethylase AlphaScreen assay was performed in 384-well plate format using white proxiplates (PerkinElmer), and transfer of compound (100 nl) was...More data for this Ligand-Target Pair
BDBM191598(2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-ox...)
IC50: 7nMAssay Description:We previously described 4-carboxy-2-triazolopyridines as selective KDM2 inhibitors (England et al., 2014). In efforts to find alternative scaffolds b...More data for this Ligand-Target Pair
BDBM191598(2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-ox...)
IC50: 10nMAssay Description:We previously described 4-carboxy-2-triazolopyridines as selective KDM2 inhibitors (England et al., 2014). In efforts to find alternative scaffolds b...More data for this Ligand-Target Pair
BDBM191598(2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-ox...)
IC50: 13nMpH: 7.5Assay Description:The demethylase AlphaScreen assay was performed in 384-well plate format using white proxiplates (PerkinElmer), and transfer of compound (100 nl) was...More data for this Ligand-Target Pair
BDBM191598(2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-ox...)
IC50: 15nMpH: 7.5Assay Description:The demethylase AlphaScreen assay was performed in 384-well plate format using white proxiplates (PerkinElmer), and transfer of compound (100 nl) was...More data for this Ligand-Target Pair
BDBM191598(2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-ox...)
IC50: 20nMAssay Description:We previously described 4-carboxy-2-triazolopyridines as selective KDM2 inhibitors (England et al., 2014). In efforts to find alternative scaffolds b...More data for this Ligand-Target Pair
BDBM191598(2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-ox...)
IC50: 20nMAssay Description:We previously described 4-carboxy-2-triazolopyridines as selective KDM2 inhibitors (England et al., 2014). In efforts to find alternative scaffolds b...More data for this Ligand-Target Pair
BDBM191598(2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-ox...)
BDBM191598(2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-ox...)
IC50: 25nMAssay Description:Inhibition of N-terminal his6-tagged human KDM5A (1 to 797 residues) expressed in sf9 insect cells incubated for 20 mins by Alphascreen assayMore data for this Ligand-Target Pair
BDBM191598(2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-ox...)
IC50: 30nMpH: 7.2 T: 2°CAssay Description:Reactions were performed in 50 mM HEPES [pH 7.2 for KDM5 or pH 7.5 for KDM4A(1-350)] containing 0.01% BSA and 0.01% Tween-20. To each well, 3 μL...More data for this Ligand-Target Pair
BDBM191598(2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-ox...)
IC50: 30nMAssay Description:Inhibition of N-terminal his6-tagged human KDM5B (1 to 769 residues) expressed in sf9 insect cells incubated for 20 mins by Alphascreen assayMore data for this Ligand-Target Pair
BDBM191598(2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-ox...)
BDBM191598(2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-ox...)
IC50: 59nMpH: 7.2 T: 2°CAssay Description:Reactions were performed in 50 mM HEPES [pH 7.2 for KDM5 or pH 7.5 for KDM4A(1-350)] containing 0.01% BSA and 0.01% Tween-20. To each well, 3 μL...More data for this Ligand-Target Pair
BDBM191598(2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-ox...)
IC50: 59nMAssay Description:Inhibition of N-terminal his6-tagged human KDM5C (1 to 839 residues) expressed in sf9 insect cells incubated for 20 mins by Alphascreen assayMore data for this Ligand-Target Pair
BDBM191598(2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-ox...)
BDBM191598(2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-ox...)
BDBM191598(2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-ox...)
IC50: 100nMAssay Description:Demethylase reactions and AlphaScreen assays were performed as described (Sayegh et al., 2013), with a few exceptions. All demethylase buffers contai...More data for this Ligand-Target Pair
BDBM191598(2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-ox...)
BDBM191598(2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-ox...)
BDBM191598(2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-ox...)
BDBM191598(2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-ox...)
BDBM191598(2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-ox...)
IC50: 160nMAssay Description:Demethylase reactions and AlphaScreen assays were performed as described (Sayegh et al., 2013), with a few exceptions. All demethylase buffers contai...More data for this Ligand-Target Pair
BDBM191598(2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-ox...)
IC50: 170nMAssay Description:We previously described 4-carboxy-2-triazolopyridines as selective KDM2 inhibitors (England et al., 2014). In efforts to find alternative scaffolds b...More data for this Ligand-Target Pair
BDBM191598(2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-ox...)
IC50: 200nMAssay Description:We previously described 4-carboxy-2-triazolopyridines as selective KDM2 inhibitors (England et al., 2014). In efforts to find alternative scaffolds b...More data for this Ligand-Target Pair
BDBM191598(2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-ox...)
IC50: 210nMpH: 7.5Assay Description:The demethylase AlphaScreen assay was performed in 384-well plate format using white proxiplates (PerkinElmer), and transfer of compound (100 nl) was...More data for this Ligand-Target Pair
BDBM191598(2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-ox...)
IC50: 600nMAssay Description:We previously described 4-carboxy-2-triazolopyridines as selective KDM2 inhibitors (England et al., 2014). In efforts to find alternative scaffolds b...More data for this Ligand-Target Pair
BDBM191598(2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-ox...)
IC50: 780nMpH: 7.5Assay Description:The demethylase AlphaScreen assay was performed in 384-well plate format using white proxiplates (PerkinElmer), and transfer of compound (100 nl) was...More data for this Ligand-Target Pair
BDBM191598(2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-ox...)
IC50: 1.00E+3nMAssay Description:We previously described 4-carboxy-2-triazolopyridines as selective KDM2 inhibitors (England et al., 2014). In efforts to find alternative scaffolds b...More data for this Ligand-Target Pair
BDBM191598(2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-ox...)
IC50: 1.00E+3nMAssay Description:We previously described 4-carboxy-2-triazolopyridines as selective KDM2 inhibitors (England et al., 2014). In efforts to find alternative scaffolds b...More data for this Ligand-Target Pair
BDBM191598(2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-ox...)
BDBM191598(2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-ox...)
BDBM191598(2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-ox...)
BDBM191598(2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-ox...)
BDBM191598(2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-ox...)
BDBM191598(2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-ox...)
IC50: 1.40E+3nMpH: 7.5Assay Description:The demethylase AlphaScreen assay was performed in 384-well plate format using white proxiplates (PerkinElmer), and transfer of compound (100 nl) was...More data for this Ligand-Target Pair
BDBM191598(2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-ox...)
BDBM191598(2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-ox...)
IC50: 2.00E+3nMAssay Description:We previously described 4-carboxy-2-triazolopyridines as selective KDM2 inhibitors (England et al., 2014). In efforts to find alternative scaffolds b...More data for this Ligand-Target Pair
BDBM191598(2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-ox...)
BDBM191598(2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-ox...)
IC50: 2.20E+3nMpH: 7.5Assay Description:The demethylase AlphaScreen assay was performed in 384-well plate format using white proxiplates (PerkinElmer), and transfer of compound (100 nl) was...More data for this Ligand-Target Pair
BDBM191598(2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-ox...)
IC50: 4.80E+3nMT: 2°CAssay Description:For inhibition assays, powders of inhibitor compounds were dissolved in 100% (v/v) DMSO to give a 20 or 50 mM concentration and stored at -20 °C unti...More data for this Ligand-Target Pair
BDBM191598(2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-ox...)
IC50: 1.40E+4nMT: 2°CAssay Description:For inhibition assays, powders of inhibitor compounds were dissolved in 100% (v/v) DMSO to give a 20 or 50 mM concentration and stored at -20 °C unti...More data for this Ligand-Target Pair
BDBM191598(2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-ox...)
IC50: 1.50E+4nMT: 2°CAssay Description:For inhibition assays, powders of inhibitor compounds were dissolved in 100% (v/v) DMSO to give a 20 or 50 mM concentration and stored at -20 °C unti...More data for this Ligand-Target Pair
BDBM191598(2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-ox...)
BDBM191598(2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-ox...)
Kd: 80nMAssay Description:ITC experiments were carried out at an enzyme [E] concentration of 25-50 μM with 0.25-1 mM compound [I] concentration in the KDM5 storage buffer...More data for this Ligand-Target Pair