p38α inhibitor 2 是一种高效选择性 p38α MAPK 抑制剂，pIC50 为 9.6。p38α inhibitor 2 抑制 hERG 离子通道 (IC50=27 μM)，在 51 个其他蛋白激酶组 (10 μM 浓度下抑制率 <30%) 和 141 个其他生物靶点组中测试时显示出良好的选择性。
p38α inhibitor 2 is a highly potent and selective p38α MAPK inhibitor, with a pIC50 of 9.6. p38α inhibitor 2 inhibits the hERG ion channel (IC50=27 μM) and shows a promising selectivity profile when tested in a panel of 51 other protein kinases (<30% inhibition at 10 μM concentration) and a panel of 141 other biological targets[1].
[1]. Raubo P, et al. The discovery and evaluation of 3-amino-2(1H)-pyrazinones as a novel series of selective p38α MAP kinase inhibitors [published online ahead of print, 2020 Jul 15]. Bioorg Med Chem Lett. 2020;30(18):127412.
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