High affinity BET bromodomain ligand (Kd values are 40 and 800 nM for Brd2(2) and Brd2(1), respectively). Exhibits 20-fold selectively for the second over the first bromodomain.
Baud et al (2016) New synthetic routes to triazolo-benzodiazepine analogues: expanding the scope of the bump-and-hole approach for selective bromo and extra-terminal (BET) bromodomain inhibition. J.Med.Chem. 59 1492 PMID:26367539