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Covalent drugs primarily work by forming covalent bonds with specific amino acid residues on target proteins, such as cysteine, lysine, and serine. Aspirin is one of the earliest known covalent drug molecules. Additionally, many natural products exhibit covalent properties, such as oridonin, which has anti-inflammatory bioactivity. In recent years, covalent targeted drugs have gained increasing attention from pharmaceutical companies. To date, at least six covalent drugs targeting kinases have been approved by the FDA, including ibrutinib, which targets the BTK kinase. 

In the discovery of covalent drug targets in cells or tissues, an effective strategy is the chemical modification of active small molecules by introducing reporter groups (such as biotin or bioorthogonal groups). This modification, while maintaining the molecule’s original activity, allows for the direct capture of interacting protein targets in live cells or tissues. However, many active molecules are challenging to modify chemically, or the products formed after reacting with amino acid residues are unstable, making them unsuitable for mass spectrometry detection. To overcome these challenges, ChomiX offers a solution: modification site identification using competitive labeling with amino acid-specific probes.