A novel in vitro permeability and efflux classification system for proteolysis targeting chimeras

> 20%. This approach aims to streamline in vitro workflows and minimize the need for extensive in vivo pharmacokinetic studies when evaluating novel PROTACs in preclinical discovery studies. SIGNIFICANT STATEMENT: This work establishes optimized assay conditions to assess permeability and a novel classification strategy that enables more reliable in vitro assessment of proteolysis targeting chimeras oral absorption potential. By streamlining workflows, it reduces the need for extensive in vivo pharmacokinetic studies when evaluating novel proteolysis targeting chimeras in drug discovery.