Fragment-based drug discovery (FBDD) is a powerful tool for the discovery of new drug leads. Screening of low-molecular ‘fragments’ (MW < 300) affords a series of key advantages over the traditional high-throughput screening (HTS) including higher hit rates and superior sampling of chemical space.
We are involved in the design, synthesis and screening of fragment libraries, as well as hit-to-lead medicinal chemistry. We are interesting in a range of protein target and more recently also RNA targets. Thus, new efforts are focused on the synthetic expansion of our fragment library to include molecules directed towards RNA targets, based on our established screening platform for 19F-NMR fragment screening with hit validation by 1H-NMR.
Output: Angew. Chem. Int. Ed., Chem. Eur. J., ChemMedChem