Birabresib (formerly OTX-015; MK-8628) is a potent and orally bioavailable inhibitor of BET bromodomain (BRD2/3/4) with antineoplastic activity.

ZL0454 (ZL-0454), an analog of ZL0420, is a novel potent and highly selective inhibitor of BRD4 (Bromodomain-Containing Protein 4) with nanomolar binding affinities to bromodomains (BDs) of BRD4.

PF-CBP1 HCl (also known as PF-06670910 HCl) is a novel, potent and highly selective inhibitor of the CREB binding protein bromodomain (CBP BRD).

CPI-203 (RO6870810, JQ-2, TEN010, RG6146) is a novel, selective, cell permeable and orally bioavailable BET bromodomain inhibitor with anticancer activity.

MI-2 (MI2, Menin-MLL Inhibitor) is a novel, potent and selective inhibitor of menin-MLL interaction with antineoplastic activity.

AZD-5153 HNT salt, the 6-Hydroxy-2-naphthoic acid salt form of AZD5153, is a potent, selective, and orally available BET/BRD4 (bromodomain and extraterminal) bromodomain inhibitor with pKi of 8.3 for BRD4.

Molibresib besylate (GSK-525762C; I-BET-762 besylate) is a novel and potent BET bromodomain inhibitor with IC50 of 32.5-42.5 nM and has immunomodulatory activity.

GSK6853 is a novel, potent and selective benzimidazolone BRPF1 bromodomain inhibitor with pIC50 of 8.1 (TR-FRET) and showed greater than 1600-fold selectivity over all other bromodomains tested.

Y06036 is a potent BET Inhibitors for Potential Treatment of Castration-Resistant Prostate Cancer (CRPC).

dBET57 is a novel BRD4 heterobifunctional small-molecule ligand (PROTAC) which exhibits significant and selective degradation of BRD4 BD1 but is inactive on BRD4 BD2.