A bottleneck in fragment-based lead development is the lack of systematic approaches to elaborate the initial fragment hits, which usually bind with low affinity to their target. Herein, we describe an analysis using X-ray crystallography of a diverse library of compounds prepared using microscale parallel synthesis. This approach yielded an 8-fold increase in affinity and detailed structural information for the resulting complex, providing an efficient and broadly applicable approach to early fragment development.

中文翻译：

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通过并行化学文库（REFiLX）的X射线晶体学筛选将片段快速加工成引线。

基于片段的先导开发的瓶颈是缺乏系统的方法来详细说明最初的片段命中，这些命中通常与目标物的亲和力很低。在这里，我们描述了使用X射线晶体学分析使用微型平行合成制备的化合物的各种库。该方法使所得复合物的亲和力和详细的结构信息增加了8倍，为早期片段开发提供了有效且广泛适用的方法。