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p300 and CBP Protein Activity Assay from US Patent US20240109879: "BENZIMIDAZOLE COMPOUND AND APPLICATION THEREOF"
Assay data:10 Active, 2 Activity ≤ 1 nM, 10 Activity ≤ 1 µM, 10 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
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Inhibition of EP300 (unknown origin) at 10 uM by DiscoverX BROMOscan assay
Assay data:1 Active, 1 Tested
Binding affinity to EP300 (unknown origin) assessed as dissociation constant
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
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
SummaryPubMed CitationRelated BioAssays by Target
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
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
Assay data:1 Tested
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
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 p300 (unknown origin) using Histone H3 substrate at 1 uM relative to control
Inhibition of CBP/p300 in human COLO 320HSR cells assessed as reduction of C-myc levels measured after 24 hrs by HTRF assay
Assay data:25 Active, 16 Activity ≤ 1 µM, 27 Tested
Inhibition of full-length P300 (1 to 2414 residues) (unknown origin) using ARTKQTARKSTGGKAPRKQLAGG-K(Biotin)-amide as substrate preincubated for 60 mins followed by substrate addition and measured by scintillation proximity assay
Assay data:2 Active, 2 Activity ≤ 1 nM, 2 Activity ≤ 1 µM, 2 Tested
Inhibition of full-length P300 (unknown origin) using ARTKQTARKSTGGKAPRKQLAGG-K(Biotin)-amide as substrate preincubated for 60 mins followed by substrate addition and measured by RapdiFire-MS/MS analysis
Assay data:28 Active, 14 Activity ≤ 1 nM, 27 Activity ≤ 1 µM, 28 Tested
Inhibition of p300 (unknown origin) using [3H]-Ac-CoA as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by Flashplate assay
Selectivity interaction (BROMOscan? panel (DiscoverX)) EUB0000247b EP300
Selectivity interaction (Bromodomain panel (DSF assay)) EUB0000191c EP300
Selectivity interaction (DSF assay) EUB0000195c EP300
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