BI 2536是一种PLK1和BRD4的双重抑制剂，对它们的IC50分别为0.83 nM和25 nM。BI-2536还抑制IFNB基因转录。

(+)-JQ1（JQ1）是一种高效、特异性和可逆的BET溴结构域抑制剂，对BRD4（1/2）的第一个和第二个溴结构域的IC50分别为77 nM和33 nM。它还激活自噬。

I-BET-151 is a selective BET inhibitor for BRD2, BRD3 and BRD4 with IC50 of 0.5 μM, 0.25 μM, and 0.79 μM in cell-free assays, respectively.

PFI-1 is a highly selective BET (bromodomain-containing protein) inhibitor for BRD4 with IC50 of 0.22 μM and for BRD2 with IC50 of 98 nM in a cell-free assay.

Molibresib（I-BET762；GSK525762）是一种BET溴结构域抑制剂，其IC50在32.5-42.5 nM之间。

RVX-208 is an inhibitor of BET bromodomain BD2 with IC50 of 0.510 μM.

Bromosporine inhibits various bromodomains including BRD2, BRD4, BRD9 and CECR2 with IC50s of 0.41 μM, 0.29 μM, 0.122 μM and 0.017 μM respectively.

Birabresib (OTX-015) 是一种强效的溴结构域 (BRD2/3/4) 抑制剂，IC50 值范围在 92 至 112 nM 之间。

CFT8634是一种口服活性的BRD9靶向降解剂，用于滑膜肉瘤和SMARCB1缺失实体瘤的研究。

GNE-781 是一种有效、口服活性和选择性的 CBP 抑制剂，在 TR-FRET 测定中的 IC50 为 0.94 nM。GNE-781 还抑制 BRET 和 BRD4 (1)，IC50 值分别为 6.2 nM 和 5100 nM。

GSK046是一种 BET 蛋白 BD2 溴结构域抑制剂，能够有效调节免疫系统。它在免疫调节和癌症研究中具有重要应用前景。

NEO2734 is an orally dual p300/CBP and BET bromodomain inhibitor with IC50 values of <30 nM for both p300/CBP and BET bromodomains.

MZ1是一种高效、选择性的PROTAC分子，能够靶向BRD4和VHL E3泛素连接酶，将BRD4蛋白降解。MZ1通过诱导BRD4降解，在癌症等表观遗传疾病的研究中显示出潜力。

FL-411 selectively inhibits BRD4 with an IC50 of 0.43 ± 0.09 μM.

Y06036 is a potent and selective BET inhibitor with BRD4(1) bromodomain binding Kd value of 82 nM. It has antitumor activity and could be used for Potential Treatment of Castration-Resistant Prostate Cancer (CRPC).

dBET57 is a BRD4 heterobifunctional small-molecule ligand (PROTAC), exhibits significant and selective degradation of BRD4 BD1 (DC50/5h=500 nM), but is inactive on BRD4 BD2.

BI-894999 is a potent and selective BET inhibitor that may treat hematological malignancies by inhibiting super-enhancer-driven oncogenes.

ARV-825是一种PROTAC，连接Cereblon和BRD4的配体，结合BRD4的BD1和BD2，Kd值分别为90 nM和28 nM。

PLX51107 is a potent and selective BRD4 inhibitor or BET inhibitor with novel in vitro and in vivo pharmacologic properties that emulates or exceeds the efficacy of BCR signaling agents in preclinical models of CLL.

dBET1 is a PROTAC, consisting of a BRD4-ligand JQ-1 linkerd to a cereblon E3 ligase ligand, targeting on BET bromodomain BRD4