In vitro screen for inhibitors of the inositol kinases ITPK1 and PPIP5K

National Center For Advancing Translational Sciences

Investigators

Abstract

During this period, the collaborative team conducted a high-throughput screening of NCATS libraries using biochemical activity assays against these two inositol kinase targets. Additionally, a DNA-encoded library screen was implemented. In silico-based screening approaches were also applied to increase the chemical space amenable for screening. Medicinal chemistry campaigns for a few selected chemotypes were initiated. The team is also evaluating the implementation of high-throughput cellular and target engagement assays to support the medicinal chemistry campaigns and further characterize compound activity.