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. Author manuscript; available in PMC: 2020 Nov 21.
Published in final edited form as: Cell Chem Biol. 2019 Oct 17;26(11):1486–1500. doi: 10.1016/j.chembiol.2019.09.012

Figure 1. Selective covalent ligand validation workflow.

Figure 1.

Structured process for irreversible covalent inhibitors validation is based on using in vitro and cell-based strategies to assess compound potency, covalent mode of binding, target selectivity, and link observed phenotype to direct covalent engagement between the compound and the target. Although no single experiment is sufficient to validate a molecule as a selective covalent tool compound, collective evidence accumulated through this validation process can be used to judge a quality of a tool compound.