BET BD2-IN-3 (compound I-58) 作为针对 BET BD2 结构域的抑制剂,有能力在小鼠身上展示外周器官和组织中的适宜生物分布。此化合物可通过 [11C] 进行放射性标记,并利用于正电子发射断层扫描 (PET) 成像技术。其在 PET 成像中的应用证明了其在生物学分布方面的有效性。
GNE-987 is a highly active chimeric BET degrader. GNE-987 binds equipotently to the BD1 and BD2 bromodomains of BRD4 with low nanomolar affinities (IC50: 4.7 and 4.4 nM, respectively). GNE-987 exhibits picomolar cell BRD4 degradation activity (DC50: 0.03
CD161 is a potent, selective, and orally bioavailable BET bromodomain inhibitor (IC50s: 28.2 nM and 7.2 nM for BRD4 BD1 and BRD4 BD2) with good anticancer activity.