High-throughput assay for measuring target occupancy of covalent compounds: a case study with MK2

Key Points

• This research investigates techniques to measure how effectively covalent compounds bind to their targets.
• Developed two plate-based assays to assess target occupancy.
• Utilized covalent tracers for indirect measurement of target engagement.
• Focused on the specific application of these methods with MK2.
• Both assays successfully measured the target occupancy of MK2 by covalent compounds.
• Assays demonstrated improved throughput compared to traditional methods.

Abstract