https://www.pnas.org/doi/10.1073/pnas.2122506119

Discovery of potent BET bromodomain 1 stereoselective inhibitors using DNA-encoded chemical library selections

From abstract:

The compound RVX-208 was an early BD2-specific compound; however, it exhibited only moderate BD2 potency (>100 nM, IC50 [the concentration that inhibits response by 50%] = 2 µM in our BRDT-BD2 AlphaScreen assay) and selectivity over BD1 domains (∼10-fold) (21). More recent efforts from other laboratories and ours have reported the synthesis of pan-BD2 inhibitors with significantly enhanced potency and selectivity [e.g., GSK046 (12), ABBV-744 (22), and our CDD-1302 compound (23)].