Temuterkib (formerly LY3214996; LY-3214996) is a selective, ATP-competitive and orally bioavailable inhibitor of the ERK1 (extracellular signal-regulated kinase) and ERK2 with potential anticancer activity.
ASN007 (ASN-007) is a novel, potent, orally bioavailable and selective inhibitor of ERK1/2 with robust antitumor activity.
AG126 is a tyrosine kinase inhibitor which can prevent the activation of mitogen-activated protein kinase p42MAPK (ERK2).
CC-90003 is a novel, potent, selective, orally bioavailable, and irreversible (covalent) inhibitor of ERK1/2 (extracellular signal-regulated kinase) with IC50s in the 10-20 nM range, and displays good kinase selectivity in a 258-kinase biochemical assay.
Ulixertinib (formerly also known as BVD-523 and VRT752271) is a novel, potent, orally bioactive, highly selective, ATP-competitive and reversible ERK1/ERK2 inhibitor with IC50 of<0.3 nM for ERK2.
KO-947 is a novel, potent and selective inhibitor of ERK1/2 kinases with potential usefulness in MAPK pathway dysregulated tumors.
Alobresib (GS-5829) is a novel and potent BET bromodomain inhibitor with anticancer activity.
ERK5-IN-2 is a novel, potent, orally bioavailable, sub-micromolar, and selective ERK5 inhibitor with selectivity over p38α and BRD4.
Ravoxertinib (formerly known as GDC0994; RG7842) is a novel, potent, orally bioavailable inhibitor of extracellular signal-regulated kinase (ERK1/2) with potential antineoplastic activity.
DEL-22379 is a novel, potent, selective, and water-soluble ERK (extracellular signal-related kinase 2) dimerization inhibitor with potential antitumor activity.