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Displacement of biotinylated small-molecule ligand from recombinant His-tagged CBP (unknown origin) measured after 10 mins by TR-FRET assay
Assay data:1 Tested
SummaryRelated BioAssays by Target
Binding affinity to human partial length EP300 (A1040 to G1161 residues) expressed in bacterial expression system by BROMOscan assay
Assay data:1 Active, 4 Tested
Binding affinity to human partial length CREBBP (R1081 to G1197 residues) expressed in bacterial expression system by BROMOscan assay
Inhibition of CREBBP (unknown origin) at 10 uM by DiscoverX BROMOscan assay
Assay data:1 Active, 1 Tested
Inhibition of EP300 (unknown origin) at 10 uM by DiscoverX BROMOscan assay
Displacement of biotinylated JQ1 from CBP bromodomain (unknown origin) incubated for 20 mins by AlphaLISA assay
Binding affinity to CBP bromodomain (unknown origin) incubated for 60 mins by TR-FRET assay
Binding affinity to CBP (unknown origin) assessed as dissociation constant
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Binding affinity to EP300 (unknown origin) assessed as dissociation constant
Binding affinity to hypoxia induced HIF-1 alpha/P300 CH1 domain (323 to 423 residues expressed in Escherichia coli (DE3)/CBP (unknown origin) interaction assessed as dissociation constant
Inhibition of hypoxia-induced HIF1alpha/P300 interaction (unknown origin) incubated for 30 mins for fluorescence anisotropy competition assay
Binding affinity to EP300 (unknown origin) assessed as change in melting temperature at 200 uM incubated for 30 to 60 mins by SYPRO orange dye based thermal shift assay
Assay data:2 Tested
Binding affinity to CBP (unknown origin) assessed as change in melting temperature at 200 uM incubated for 30 to 60 mins by SYPRO orange dye based thermal shift assay
Binding affinity to human CBP/p300 bromodomain using H-ALREIRRYQK(ac)STELLIRKLK(biotin)-OH as substrate incubated for 30 mins by AlphaScreen assay
Assay data:3 Active, 2 Activity ≤ 1 µM, 3 Tested
Antagonist activity at CBP/beta-catenin (unknown origin) protein-protein interaction
In Vitro Activity Against CBP from US Patent US20240016795: "BROMODOMAIN INHIBITORS FOR ANDROGEN RECEPTOR-DRIVEN CANCERS"
Assay data:4 Active, 4 Activity ≤ 1 µM, 4 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Inhibition of CBP/p300 in human COLO 320HSR cells assessed as decrease in H3K9 acetylation at 0.3 to 1000 nM measured by western blot analysis
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of CBP/p300 in human COLO 320HSR cells assessed as decrease in H3K27 acetylation at 0.3 to 1000 nM measured by western blot analysis
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Inhibition of CBP/p300 in human COLO 320HSR cells assessed as decrease in H3K18 acetylation at 0.3 to 1000 nM measured by western blot analysis
Inhibition of CBP (unknown origin) using Histone H3 substrate at 1 uM relative to control
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