GNE-781 (GNE781) is a potent, selective, non-CNS penetrant, orally active CBP/p300 bromodomain inhibitor with IC50 of 0.94/1.2 nM in TR-FRET assays.
GNE-781 exhibits high selectivity over BRD4 (1) (>5 uM) and other BRDs.
GNE-781 suppresses Myc transcript levels in cellular assays with EC50 of 6.6 nM.
GNE-781 displays antitumor activity in an AML tumor model and decreases Foxp3 transcript levels in a dose dependent manner.
