Automated high-throughput synthesis and biological evaluation of compound libraries

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High-throughput chemical library screening (HTS) still forms the backbone of modern drug discovery. It can allow the rapid identification of hit compounds towards novel therapeutic candidates and/or chemical probes for the study of biological systems. However, the limitation of this methodology is access to large and chemically diverse libraries with organic synthesis and purification still being a major bottleneck in the process. This project will take an automated approach to both synthesis and screening, avoiding troublesome purification. We will develop a small library of well-designed building blocks capable of assembly into larger entities through iterative coupling chemistries. Combining the advantages of robotically enabled high-throughput synthesis, solid-phase synthesis and on-bead target screening our libraries can be taken from synthesis directly to in vitro biological testing. These approaches will be targeted towards the discovery of inhibitors for protein-protein interaction, aiming to significantly streamline their discovery.