Fragment screening is a popular strategy for generating viable chemical starting points for drug targets, however, weak affinity to targets, as well as the exploration of the binding site, remain challenging. Here, the authors develop pharmacophore-optimized photoaffinity fragments that can effectively explore the available binding site and enable a high hit rate and better sensitivity.
- Péter Ábrányi-Balogh
- Dávid Bajusz
- György M. Keserű
