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Drug-target interactions

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The ability to vary a drug's residence time on a target is important for drug optimization. A series of reversible covalent inhibitors of select kinases demonstrates the feasibility of tuning residence time from minutes to days through modification of noncovalent features of the molecules.

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Figure 1: The basis of the drug-target residence time model.

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Correspondence to Robert A Copeland.

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Copeland, R. Stay tuned. Nat Chem Biol 11, 451–452 (2015). https://doi.org/10.1038/nchembio.1831

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