AMG 548 is an inhibitor of p38α MAPK (Ki = 0.5 nM).1 It is selective for p38α over p38γ, p38δ, JNK1, JNK2, and JNK3 (Kis = 2,600, 4,100, 11,480, 39, and 61 nM, respectively) and is greater than 1,000-fold selective over a panel of 36 additional kinases but also inhibits p38β (Ki = 3.6 nM). AMG 548 inhibits LPS-induced production of TNF-α and IL-1β in isolated human whole blood (IC50s = 3 and 7 nM, respectively).
1.Lee, M.R., and Dominguez, C.MAP kinase p38 inhibitors: Clinical results and an intimate look at their interactions with p38α proteinCurr. Med. Chem.12(25)2979-2994(2005)