Chemoproteomics Discovery of CNS-Penetrant Covalent Inhibitors
11:30 am - Wednesday 21st October 2026
- Leveraging chemoproteomic screening platforms to identify covalent hits with high selectivity, incorporating orthogonal assays and kinetic profiling (kinact/KI) to distinguish tractable opportunities from liabilities
- Accelerating optimization into brain-penetrant proof-of-concept molecules through integrated assessment of selectivity, reactivity, and exposure
- Exploiting prolonged target residence time in the brain to enhance efficacy, enabling reduced dosing strategies while minimizing safety risks through deeper understanding of protein turnover and covalent engagement
