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The identification and SAR studies of glumetinib (9) are presented. The essential amino acid residues that mediate interactions between the small molecule and the MET protein are depicted. Mauve dashed lines represent hydrogen bonds with key amino acids, and faint gray dashed lines indicate π-π interactions. The chemical structures of candidate molecules SAR125844 (4) and bozitinib (5), currently undergoing clinical phase I/II studies, are presented.
