Fragment Based Drug Discovery

Fragment-based Drug Discovery (FBDD) has become a very popular approach in drug development. Due to the rise in the complexity of Target molecules, there is a need for flexible screening technologies allowing the exploration of more diverse molecules especially from new chemical spaces. With a typical size of < 500 Da and their broad coverage of chemical spaces, fragments are perfectly suited for early-stage drug discovery, and can be utilized as “building blocks” of future lead compounds that usually bind to their target molecule with low affinity. TRIC technology allows for rapid screening of fragment libraries in solution and reliable determination of Kds even in the millimolar range, independent of the molecular mass of the interaction partners, making Dianthus the perfect match for FBDD. An application note describing a fragment screen with Dianthus can be found in the NanoTemper Explorer Community.