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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
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
Assay data:1 Active, 1 Tested
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
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
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Selectivity interaction (BROMOscan? panel (DiscoverX)) EUB0000247b CREBBP
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Selectivity interaction (BROMOscan (DiscoverX)) EUB0000191c CREBBP
SummaryRelated BioAssays by Target
Selectivity interaction (Bromodomain panel (DSF assay)) EUB0000330a CREBBP
Selectivity interaction (Bromoscan (DiscoverX, BromoKdELECT)) EUB0000004c CREBBP
Selectivity interaction (BromoKdELECT (DiscoverX)) EUB0000004c CREBBP
SummaryCompounds, ActiveRelated BioAssays by Target
Selectivity interaction (DSF assay) EUB0000195c CREBBP
Selectivity interaction (Biolayer Interferometry experiment) EUB0000195c CREBBP
Selectivity interaction (AlphaScreen) EUB0000195c CREBBP
Affinity Biochemical interaction (ITC) EUB0000208c CREBBP
Affinity Biochemical interaction (ITC) EUB0000195c CREBBP
Affinity Biochemical interaction (TR-FRET assay (BHC domains)) EUB0000328a CREBBP
Affinity Biochemical interaction (TR-FRET assay (BHC domains)) EUB0000326a CREBBP
Affinity On-target Cellular interaction (NanoBRET assay (HEK293T cells)) EUB0000195c CREBBP
Affinity Phenotypic Cellular interaction (FRAP assay (displacement of the CBP bromodomain from chromatin)) EUB0000208c CREBBP
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