Efficient sampling of chemical space

A diverse set of 1000 fragments represents its chemical space about as effectively as would 10 trillion diverse drug-sized molecules

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Ideally suited for targeting PPIs

They can bind to small pockets available on the protein surface

Predictor of protein druggability

Obtaining high hit rates is an excellent predictor that high-affinity, small molecule ligands can be identified.

Low hit rates (< 0.1%) strongly suggest an undruggable pocket.

Often unique binding profiles

High-quality interactions between fragment and target

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Chemical optimization

Ability to optimize pharmacokinetics profile simultaneously with potency as fragment hit grows to clinical candidate.