The unique MOA of PROTACs provides promising opportunities in the discovery and development of innovative therapeutics. Synthesis and optimization of PROTACs via traditional iterative synthesis for any drug discovery program can be resource intensive and very time-consuming.
We have developed a highly efficient High-Throughput Chemistry Direct-to-Biology platform to conduct miniaturized reactions in 1536-well plates to make large set of PROTACs and directly assess these crude reactions in a cellular degradation assay. Case studies will be presented to showcase how the platform has impacted timelines for identifying new PROTACs and supported lead optimisation projects.