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Table 1.

BRAF, MEK, and ERK inhibitors with their binding modes defined with structures shown below

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.