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Representative binding modes of the four classes of kinase inhibitors. Representative binding modes of the four classes of kinase inhibitors with ligand in blue sticks and key polar interactions shown as red dotted lines: (A) gefitinib bound to EGFR (type 1, pdb 2ity); (B) vemurafenib bound to B-Raf (type 1.5, pdb 3og7); (C) imatinib bound to ABL (type 2, pdb 1iep); and (D) afatinib bound covalently to EGFR (pdb 4g5j). Activation states of helix-C and the DFG-motif are annotated.
