Table 1.
Molecule | Target | Binding mode | αC-helix “in” or “out” |
---|---|---|---|
GDC-0879 | BRAF | Type I | “in” |
Vemurafenib | BRAF | Type I.5 | “out” |
Dabrafenib | BRAF | Type I.5 | “out” |
PLX-8394 | BRAF | Type I.5 | “out” |
Sorafenib | BRAF | Type II | “in” |
AZ-628 | BRAF | Type II | “in” |
Trametinib | MEK | Class I | “out” |
Cobimetinib | MEK | Class I | “out” |
GDC-0623 | MEK | Class II | “out” |
G-573 | MEK | Class II | “out” |
CH5126766 | MEK | Class II | “out” |
GDC-0994 | ERK | Type I | “in” |
SCH772984 | ERK | Type I | “in” |
MEK, Mitogen-activated protein kinase; ERK, extracellular signal-related kinase.