Novel N-substituted azaindoles have been discovered as PIM1 inhibitors. X-ray structures have played a significant role in orienting the chemistry effort in the initial phase of hit confirmation. Disclosure of an unconventional binding mode for 1 and 2, as demonstrated by X-ray crystallography, is presented and was an important factor in selecting and advancing a lead series.

中文翻译：

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的发现Ñ取代7-氮杂吲哚如PIM1激酶抑制剂-第一部分

已经发现了新型的N-取代的氮杂吲哚作为PIM1抑制剂。X射线结构在命中确认的初始阶段确定化学工作方向方面发挥了重要作用。X射线晶体学表明，公开了1和2的非常规结合模式，这是选择和推进前导序列的重要因素。