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。

Volasertib（BI 6727）是一种口服活性、高效和ATP竞争性的Polo样激酶1（PLK1）抑制剂，IC50为0.87 nM。它抑制PLK2和PLK3，IC50值分别为5 nM和56 nM，诱导有丝分裂停滞和凋亡。Volasertib是一种二氢蝶啶酮衍生物，在多种癌症模型中表现出显著的抗肿瘤活性。

Rigosertib Sodium (Random Configuration) is a non-ATP-competitive inhibitor of PLK1 with IC50 of 9 nM in a cell-free assay. It shows 30-fold greater selectivity against Plk2 and no activity to Plk3.

GSK461364 is a potent small molecule Polo-like kinase 1 (PLK1) inhibitor with a Ki of 2.2 nM.

MLN0905 is a small-molecule and potent inhibitor of PLK1 with IC50 of 2 nM.

RO3280 is a potent, highly selective inhibitor of Polo-like kinase 1 (PLK1) with IC50 of 3 nM.

SBE13 HCl is a potent and selective PLK1 inhibitor with IC50 of 0.2 nM while 875 nM and 66 μM for PLK3 and PLK2. SBE 13 could also induce cell cycle arrest, reduce cell proliferation with EC50 of 5-60 µM, and induce apoptosis in a broad range of human cancer cell lines.

NMS-1286937 is an orally bioavailable, small-molecule Polo-like kinase 1 (PLK1) inhibitor (IC50=2 nM) with potential antineoplastic activity and no inhibition on PLK2 and PLK3.

HMN-214 is a potent PLK1 inhibitor an average IC50 of 0.12 μM, and a prodrug of HMN-176, which alters the cellular spatial orientation of Plk1.