MK-5046 is a novel BRS-3 agonist, binding to BRS-3 with high affinity (mouse Ki = 1.6 nM, human Ki = 25 nM).

BRS3 (mouse):1.6 nM (ki), BRS3 (human):25 nM(ki)

Raf-MEK-ERK cascade kinase assay: Non-phosphorylated myelin basic protein (MBP) is coated onto an ELISA plate, and the active form of B-Raf/c-Raf is mixed with unphosphorylated MEK1/MEK2 and ERERK2 in 10 μM ATP and 12.5 mM MgCl2 containing MOPS buffer in the presence of various concentrations of GSK1120212. The phosphorylation of MBP is detected by the anti-phospho-MBP antibody.