Fragment-based screening — big impact from small molecules

Fragment-based screening is a powerful approach to early-stage drug discovery, using small, well-soluble organic molecules to efficiently explore chemical space. Thanks to their simplicity and affordability, fragment libraries are accessible even to the smallest biotech companies. Traditionally, fragments are screened using biophysical methods like NMR or SPR. While sensitive, these methods can suffer from false positives, limited structural insight, or insufficient sensitivity for low-affinity binders. That’s where X-ray Fragment Screening (XFS) stands out. XFS offers unmatched sensitivity and can detect fragment binders even when other methods fail. More importantly, it delivers direct structural insight thereby revealing exactly where and how fragments bind to the protein, which accelerates downstream optimization. But there’s a catch: XFS requires hundreds of crystals and is often seen as expensive. At GIOS Biostructures, we’ve implemented a cost-effective XFS platform that preserves all the advantages like high sensitivity, direct visualization, and low false-positive rate while significantly reducing the cost barrier.

Whether you’re a biotech startup or an established discovery team, GIOS makes XFS accessible, enabling rapid identification of structurally validated fragment hits.

Fragment-based screening
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