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Target engagement (TE) assay in drug discovery measures compound binding potency (occupancy) at selected target proteins in intact cells or tissues. Understanding target engagement allows research teams to design and interpret quality in vivo experiments, providing a more refined assessment of target validation.
For covalent inhibitors, an essential part of new drug development, a Parallel Reaction Monitoring (PRM) mass-spectrometry based absolute quantification platform was developed for proteome-wide measurement of target engagement at specific sites. In this strategy, PRM-based quantification was performed to quantify the absolute abundance of both drug-bound and unbound forms of targeted binding sequence, which were then used for downstream calculation of target engagement. PRM-based absolute assay enables a more accurate and sensitive quantification of targeted sequences and can be performed at complex proteome level in a high-throughput way.
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