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In Vitro Enzymatic Activity Assay from US Patent US20240101551: "CRYSTAL FORM AND SALT FORM OF BROMINE DOMAIN PROTEIN INHIBITOR AND PREPARATION METHOD THEREFOR"
Assay data:1 Active, 1 Activity ≤ 1 nM, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
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
BRD4 SGC Tm panel (DSF)
Assay data:1 Tested
SummaryRelated BioAssays by Target
Binding affinity to BRD4 bromodomain 2 (unknown origin) assessed as gibbs free energy change by ITC analysis
SummaryPubMed CitationRelated BioAssays by Target
Binding affinity to full length BRD4 short isoform (unknown origin) by BROMOscan assay
Assay data:2 Active, 1 Activity ≤ 1 µM, 4 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
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
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
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
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