Fragment Libraries

Fragment-based drug discovery (FBDD) is a powerful method to develop potent small-molecule compounds starting from fragments binding weakly to targets. FBDD starts by screening libraries of low-molecular weight compounds (fragments) against the target of interest to identify ‘‘hits.’’ The identified hit is then grown into drug-like molecules through different strategies. Although FBDD cannot replace high-throughput screening (HTS) campaigns in drug discovery, it has some attractive advantages such as saving experimental cost, offering diverse hits, and exhibiting multiple ways to develop novel compounds.