ZEN-3862 is a BET inhibitor with IC50 s of 0.16 and 0.13 μM for BRD4 (BD1) and BRD4 (BD2), respectively. ZEN-3862 can be used to form PROTAC s to induce degradation of BRD4 [1].
References:
[1]. Kharenko OA, et al. Design and Characterization of Novel Covalent Bromodomain and Extra-Terminal Domain (BET) Inhibitors Targeting a Methionine. J Med Chem. 2018 Sep 27;61(18):8202-8211.
References:
[1]. Kharenko OA, et al. Design and Characterization of Novel Covalent Bromodomain and Extra-Terminal Domain (BET) Inhibitors Targeting a Methionine. J Med Chem. 2018 Sep 27;61(18):8202-8211.
















