Fig. 4. Development of AMG 510 (10). a, Chemical structures of indole lead 1Amgen (9), ARS-1620 scaffold and AMG 510 (10). b, Biochemical and cellular data as well as drug-like properties of compounds shown in Fig. 4a. c, Structural comparison of the KRasG12C:GDP binding modes of ARS-1620 (8) (left, pdb id ; 5v9u) and indole lead 1Amgen (9) (right, pdb id ; 6p8z). d, Co-crystal structure of KRasG12C:GDP bound to AMG 510 (10) (left, pdb id ; 6oim) and key interactions (right).
