Chemoproteomics-Based Discovery of CNS-Penetrant Covalent Inhibitors
- Development of a robust live cell chemoproteomics screening platform for covalent hit discovery
- Rapid MS-based proteomics led optimization of covalent screening hits to a brain-penetrant covalent inhibitor of a high-value CNS target
- Highlighting the advantages of developing covalent inhibitors for long-lived protein targets in the brain, while minimizing peripheral target occupancy