GSK8814 is a potent, selective inhibitor of ATAD2/2B bromodomain binding constant pKd of 8.1 in ITC assays.
GSK8814 displaces acetylated H4 peptide from the ATAD2 bromodomain with pIC50 of 7.3 and is also active in BROMOscan with pKi of 8.9.
GSK8814 displays >100 fold selective over all other bromodomains and >1,000 fold selective over BRD4.
GSK8814 shows cellular target engagement with an EC50 of 2 µM in a NanoBRET assay evaluating the interaction of the NanoLuc-ATAD2 bromodomain with histone H3.3-HaloTag.
