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Ataxia telangiectasia mutated and Rad3-related (ATR) kinase is an important regulator of the DNA damage response, especially in response to replication stress. SKLB-197 is a potent and highly selective ATR inhibitor with an IC50 value of 13 nM. SKLB-197, exhibits good pharmacokinetic properties, could be a promising lead compound for drug discovery targeting ATR. The pharmacokinetic (PK) studies were performed by Medicilon.

Reference

Huachao Bin, et al. Discovery of a potent and highly selective inhibitor of ataxia telangiectasia mutated and Rad3-Related (ATR) kinase: Structural activity relationship and antitumor activity both in vitro and in vivo. Eur J Med Chem. 2022 Mar 15;232:114187. doi: 10.1016/j.ejmech.2022.114187.