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. Author manuscript; available in PMC: 2019 Jun 19.
Published in final edited form as: Biochemistry. 2018 Apr 30;57(24):3326–3337. doi: 10.1021/acs.biochem.8b00315

Figure 5.

Figure 5

Classical Affinity Label As a Covalent Inhibitor. The high effective concentration of the acrylamide in afatinib enables selective reaction with a non-catalytic Cys (C797) in EGFR, presumably with the small fraction of ionized thiolate present at the reaction pH.