Towards a RIOK2 chemical probe: cellular potency improvement of a selective 2-(acylamino)pyridine series

RIOK2 is an understudied kinase associated with a variety of human cancers including non-small cell lung cancer and glioblastoma. No potent, selective, and cell-active chemical probe currently exists for RIOK2. Such a reagent would expedite re-search into the biological functions of RIOK2 and validate it as a therapeutic target. Herein, we describe the synthesis of naphthyl-pyridine based compounds that have improved cellular activity while maintaining selectivity for RIOK2. While our compounds do not represent RIOK2 chemical probes, they are the best available tool molecules to begin to characterize RIOK2 function in vitro.

Automated summary

The study describes a synthesis method for preparing compounds with improved cellular activity while maintaining selectivity for RIOK2. Although these compounds are not RIOK2 chemical probes, they serve as the best tool molecules to begin characterizing RIOK2 function in vitro.