Potent, selective, and cell active small molecule kinase inhibitors are useful tools to help unravel the complexities of kinase signaling. As the biological functions of individual kinases become better understood, they can become targets of drug discovery efforts. The small molecules used to shed light on function can also then serve as chemical starting points in these drug discovery efforts. The Nek family of kinases has received very little attention, as judged by number of citations in PubMed, yet they appear to play many key roles and have been implicated in disease. Here we present our work to identify high quality chemical starting points that have emerged due to the increased incidence of broad kinome screening. We anticipate that this analysis will allow the community to progress towards the generation of chemical probes and eventually drugs that target members of the Nek family.

中文翻译：

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深入分析激酶交叉筛选数据，以确定抑制 Nek 激酶家族的化学起点†

有效的、选择性的、细胞活性的小分子激酶抑制剂是帮助解开激酶信号传导复杂性的有用工具。随着单个激酶的生物学功能得到更好的了解，它们可以成为药物发现工作的目标。用于阐明功能的小分子也可以作为这些药物发现工作的化学起点。从 PubMed 中的引用数量来看，Nek 激酶家族很少受到关注，但它们似乎发挥着许多关键作用，并且与疾病有关。在这里，我们介绍了我们的工作，以确定由于广泛的激酶组筛查发生率增加而出现的高质量化学起点。我们预计，这项分析将使社区能够朝着化学探针的产生以及最终针对 Nek 家族成员的药物的方向取得进展。