Lead Selection & Optimization

Lead Selection & Optimization

Following the identification of potential leads by high-throughput screening, lead selection and optimization efforts are performed. This work involves evaluating promising compounds to determine which are best suited for further development, then iterating on these compounds to improve key qualities (binding affinity, specificity, stability, toxicity, etc.). Our non-covalent and covalent screening assays can also be leveraged for selectivity, competition, and counter-screening, meaning that hit characterization and hit-to-lead experiments can be performed rapidly and without the need for additional assay development. Additional proteomic and chemoproteomic services enable the global identification of on- and off-targets, validation of target engagement, and evaluation of compound pharmacokinetics/pharmacodynamics. These assays provide valuable information to guide the lead selection process and optimize therapeutic potential.