CHK1-IN-3是一种高效的检测点激酶 1 (CHK1) 抑制剂，IC₅₀ 为 0.4 nM。CHK1-IN-3 可通过阻断 DNA 损伤应答途径，在癌症治疗中表现出潜在的应用价值。

GDC-0575 is a potent and selective CHK1 inhibitor.

SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC (50) of 13.3 nmol/L on the isolated human enzyme. This compound abrogates an etoposide-induced G (2) arrest with an IC (50) of 55 nmol/L in HT29 cells, and significantly enhances the cell killing of gemcitabine and SN38 by 3.0- to 29-fold in several colon tumor lines in vitro and in a p53-dependent fashion.

ANI-7是一种 AhR 通路激活剂，能够通过激活 AhR 途径抑制多种癌细胞的生长，尤其对 MCF-7 乳腺癌细胞具有选择性抑制作用，GI50 为 0.56 μM，适用于乳腺癌和其他癌症的研究。

SCH-900776 is the S-isomer form of SCH900776, which is a potent, selective and orally bioavailable inhibitor of checkpoint kinase Chk1 (IC50 = 3 nM), highly selective against Chk2 (IC50 = 1500 nM) and cyclin-dependent kinase CDK2 (IC50 = 160 nM).

AZD-7762是一种强效的 ATP 竞争性检查点激酶 (Chk) 抑制剂，对 Chk1 的 IC50 为 5 nM。

LY2606368 is a potent and selective ATP competitive inhibitor (IC50=1.5 nM in SW1990 cell) of the Chk1 protein kinase.

Rabusertib(LY2603618) 是一种高效且选择性的 Chk1 抑制剂，IC50 为 7 nM。

LY2606368 (Prexasertib) is a selective Chk1 inhibitor with IC50 value <1nM, modest to Chk2 and Rsk with IC50 values of 8nM and <10nM.

PF-477736 is a selective, potent and ATP-competitive Chk1 inhibitor with Ki of 0.49 nM and also inhibits VEGFR2, Aurora-A, FGFR3, Flt3, Fms (CSF1R), Ret and Yes and shows ~100-fold selectivity for Chk1 than Chk2.

CCT241533 HCl is a potent serine/threonine checkpoint kinase (Chk2) inhibitor with IC50 of 3 nM and shows minimal cross-reactivity against a panel of kinases at 1 μM.

BML-277 is a selective Chk2 (checkpoint kinase 2) inhibitor with IC50 of 15 nM.

CCT245737 is a potent, ATP-competitive CHK1 inhibitor with an IC50 of 30-220 nM.

SCH 900776 (MK-8776) is a selective and highly potent CHK1 inhibitor with IC50 value of 3nM, modest to CDK2 and Chk2 with much higher IC50 values of 160nM and 1.5uM, respectively.

CHIR-124 is a potent Chk1 inhibitor with IC50 of 0.3 nM with 2,000-fold selectivity against Chk2, 500- to 5,000-fold less activity against CDK2/4 and Cdc2.

Prexasertib, also known as LY2606368, is a potent and selective Chk1/Chk2 inhibitor. Prexasertib increases the effectiveness of conventional therapy in B-/T- cell progenitor acute lymphoblastic leukemia. LY2606368 Causes Replication Catastrophe and Antitumor Effects through CHK1-Dependent Mechanisms. Treatment of cells with LY2606368 results in the rapid appearance of TUNEL and pH2AX-positive double-stranded DNA breaks in the S-phase cell population.

Inhibitor of checkpoint kinase 1 (Chk1) that displays selectivity over other protein kinases (IC50 values are 15, 250 and 1000 nM for Chk1, cdc2 and PKC respectively). Abrogates G2 cell cycle arrest caused by γ-irradiation and topoisomerase I inhibition. Potentiates cytotoxicity of DNA-damaging drugs, enhancing the efficacy of some chemotherapeutics.