Скачать или смотреть How to optimize the fragment hit rate take protein crystals first

'The application of X-ray crystallography as a primary fragment screening method has been underutilized due to the limited availability of a robust system for soaking experiments and solubility issues of fragments.

The major bottlenecks in the experimental setup for crystal soaking are the sensitivity of protein crystals. CrystalsFirst overcomes this limitation using the SmartSoak® technology, which stabilizes protein crystals and enables direct crystallographic screening without trial-and-error optimization of the soaking system.

With a hit rate up to 30% and numerous case studies, we demonstrate the advantages of crystallographic fragment screening as a primary method to access the best possible chemical space.'