What question did this study set out to answer?

This research investigates techniques to measure how effectively covalent compounds bind to their targets.

February 6, 2026RSC Chemical Biology0 citationsOpen Access

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

JWJulian L. Wong MMMari Manuia SGSandra Gao

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

Two complementary, plate-based assays that overcome the throughput bottleneck associated with measuring target engagement are presented. These methods utilize covalent tracers to probe indirectly the engagement of a covalent inhibitor with MK2.

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