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A) Covalent inhibitors of KRas G12C. B) Binding mode of 9 to KRas G12C (blue, PDB 5F2E) compared to the apo KRas (grey, PDB 4OBE). The binding of 9 caused the α2 helix and Met72 of switch II to move. The carbonyl of the acrylamide is situated where the γ‐phosphate of GTP would be situated. These changes result in the GDP‐state of KRas being favored and prevent nucleotide exchange.
