BAY-850 (BAY850) is a potent, isoform selective, cellularly active ATAD2 bromodomain inhibitor with binding IC50 of 166 nM in TR-FRET assay.
BAY-850 shows no inhibitory activity in a panel of 354 kinases and only modest effects on a few GPCRs.
BAY-850 displaces a tetra-acetylated H4 peptide with an IC50 of 22 nM, and the tetra-acetylated peptides with IC50 of 115 nM.
BAY-850 pecifically induces ATAD2 bromodomain dimerization and prevents interactions with acetylated histones in vitro, as well as with chromatin in cells.
