Fragment-Based Drug Discovery
WuXi AppTec offers a very diverse technology platform that facilitates target validation, enables fast hit finding, hit confirmation, and supports lead series optimization.
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
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
Ability to optimize pharmacokinetics profile simultaneously with potency as fragment hit grows to clinical candidate.