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Table 2 Classification of small molecule kinase inhibitors

From: Kinase-targeted cancer therapies: progress, challenges and future directions

Class of Kinase Inhibitor Mechanism of Action Examples
Type I Competes for the substrate and binds in the ATP-binding pocket of the active conformation Bosutinib, Cabozantinib, Ceritinib, Crizotinib, Gefitinib, Pazopanib, Ruxolitinib, Vandetanib
Type II Type II inhibitors bind to the DFG-Asp out protein kinase conformation, which corresponds to an inactive enzyme form Imatinib, Sorafenib, Axitinib, Nilotinib
Type III (Allosteric Inhibitor) Occupy a site next to the ATP-binding pocket so that both ATP and the allosteric inhibitor can bind simultaneously to the protein. Trametinib, GnF2
Type IV (Substrate Directed Inhibitors) Undergo a reversible interaction outside the ATP pocket and offer selectivity against targeted kinases ONO12380
Type V (Covalent Inhibitor) Bind covalently (irreversible)to their protein kinase target Afatinib, Ibrutinib, HK1–272