BI-2536 is a potent Plk1 inhibitor with IC50 of 0.83 nM, BI2536 shows 4- and 11-fold greater selectivity against Plk2 and Plk3 and also is a BRD4 inhibitor (IC50= 25 nM).

(+)-JQ1 is a BET bromodomain inhibitor, with IC50 of 77 nM/33 nM for BRD4(1/2) in cell-free assays, binding to all bromodomains of the BET family, but not to bromodomains outside the BET family.

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.

I-BET 762 is an inhibitor for BET proteins with IC50 of ~35 nM.

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.

OTX-015 is a potent BET bromodomain inhibitor with EC50 ranging from 10 to 19 nM for BRD2, BRD3, and BRD4 in cell-free assays.

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 is a PROTAC with VHL-ligand and targeting on BRD protein, with preferential selectivity to BRD4 (Kd=149nM) over BRD2 and BRD3.

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 is a PROTAC targeting on BRD4, consisting of a BRD4-ligand JQ-1 linked to a cereblon E3 ligase ligand Pomalidomide, with K_ds values of 90nM and 28nM for affinity to BD1 and BD2.

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.