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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
BRD4 SGC Tm panel (DSF)
Assay data:1 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
Displacement of biotinylated small-molecule ligand from recombinant His-tagged BRD4 bromodomain 2 (unknown origin) measured after 10 mins by TR-FRET assay
Assay data:4 Active, 11 Tested
Displacement of biotinylated small-molecule ligand from recombinant His-tagged BRD4 bromodomain 1 (unknown origin) measured after 10 mins by TR-FRET assay
Assay data:9 Active, 1 Activity ≤ 1 µM, 11 Tested
Protac activity at IAP/BRD4 in human SK-MEL-28 cells assessed as induction of BRD4 degradation at 0.1 to 10 uM measured after 24 hrs by Western blotting analysis
Assay data:2 Active, 2 Tested
Protac activity at VHL/BRD4 in human MCF7 cells assessed as induction of BRD4 degradation at 10 uM measured after 24 hrs by Western blotting analysis
Assay data:1 Active, 2 Tested
Inhibition of BRD4 bromodomain 1/2 (unknown origin) assessed as dissociation constant by DiscoveRx BROMOscan assay
Assay data:19 Active, 16 Activity ≤ 1 µM, 21 Tested
Inhibition of BRD4 bromodomain 1/2 (unknown origin) by Alphascreen assay
Assay data:4 Active, 6 Tested
Inhibition of human N-terminal His6-tagged BRD4 (44 to 168 residues) expressed in Escherichia coli BL21 (DE3) incubated for 1 hr by chromatography method
Assay data:1 Active, 1 Tested
Inhibition of BRD4 (unknown origin) using pre-acetylated Biotin-Histone 4 Peptide as substrate by alpha screen assay
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