Identification of modulators of PI4K for cellular trafficking-related indications

National Center For Advancing Translational Sciences

Investigators

Abstract

During this period, the collaborative team completed primary high-throughput screening and hit validation. Screening hits were identified, cherrypicked and retested to validate their activity. Select compounds with validated activity were advanced for medicinal chemistry optimization, and several series of analogs were synthesized. In the meantime, additional assay development afforded an opportunity to conduct a second high-throughput screen to identify compounds capable of binding to and inhibiting PI4K2a. Medicinal chemistry is currently ongoing to further improve hits of interest.