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Inhibitory Action on Binding of BRD4 Protein and Ligand from US Patent US11890288: "Sulfonamide or sulfinamide compound having effect of inducing BRD4 protein degradation and pharmaceutical use thereof"
Assay data:3 Active, 3 Activity ≤ 1 µM, 3 Tested
SummaryRelated BioAssays by Target
VRK1 SGC Tm panel (DSF)
Assay data:1 Tested
BRD4 SGC Tm panel (DSF)
Inhibition of GST-tagged DCN1 PONY domain (unknown origin)/human N-terminal acetylated UBC12 (1 to 12 residues) protein-protein interaction incubated for 1 hr by HTRF analysis
Assay data:41 Active, 34 Activity ≤ 1 µM, 45 Tested
Reversible inhibition of GST-tagged DCN1 PONY domain (unknown origin)/human N-terminal acetylated UBC12 (1 to 12 residues) protein-protein interaction at 500 nM preincubated for 1 hr followed by Ac-UBC12-biotin addition by HTRF based dilution analysis
Assay data:2 Active, 2 Tested
Reversible inhibition of GST-tagged DCN1 PONY domain (unknown origin)/human N-terminal acetylated UBC12 (1 to 12 residues) protein-protein interaction at 500 nM preincubated for 1 hr followed by Ac-UBC12-biotin addition by HTRF based ultrafiltration analysis
Inhibition of biotinylated DCN1 PONY domain (unknown origin)/human N-terminal acetylated UBC12 (1 to 12 residues) protein-protein interaction incubated for 1 hr by TR-FRET analysis
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
Binding affinity to BRD4 bromodomain 2 (unknown origin) assessed as gibbs free energy change by ITC analysis
Binding affinity to full length BRD4 short isoform (unknown origin) by BROMOscan assay
Assay data:2 Active, 1 Activity ≤ 1 µM, 4 Tested
Binding affinity to human partial length BRD4 bromodomain 2 long isoform (K333 to E460 residues) expressed in bacterial expression system by BROMOscan assay
Assay data:2 Active, 4 Tested
Binding affinity to BRD4 bromodomain 1/2 long isoform (unknown origin) by BROMOscan assay
Binding affinity to human partial length BRD4 bromodomain 1 long isoform (N44 to E168 residues) expressed in bacterial expression system by BROMOscan assay
Assay data:3 Active, 4 Tested
Binding affinity to BRD4 in human PC-9 cell lysate assessed as increase in thermal stabilization at 10 uM at 38 to 71 degreeC measured after 30 mins by CETSA
Binding affinity to BRD4 in human PC-9 cell lysate assessed as increase in thermal stabilization at 2 uM at 38 to 71 degreeC measured after 30 mins by CETSA
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