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(A) A panel of 17 novel ERK1/2 inhibitors surveyed in this study. Ki measurements were made using kinase assays for phosphorylation of Omnia peptide substrate (Invitrogen). (B) Variations among ERK1/2 inhibitors in their left-side, central scaffold, and a sampling of right-side substituents. (C) Contacts formed by VTX11e and GDC0994 with active site residues in 2P-ERK2, based on published X-ray structures (PDBID:6OPK, PDBID:6OPH).
