A customer perspective on hit validation in fragment based drug discovery

Guest Presenter: Dr. Martin Andersson, Director Protein Science, Sprint Bioscience, Stockholm, Sweden

Sprint Bioscience have established a fragment-based drug discovery (FBDD) platform with disciplines ranging from protein production, fragment screening, biophysics and x-ray crystallography to computational and medicinal chemistry. In order to drive projects in an efficient manner they identified the need for a set of screening technologies that were generic, could be rapidly established for new targets and efficiently could identify fragment hits from their fragment library. Furthermore, technologies for follow-up after primary screening are important to allow for elimination of false positives and fragments with undesirable modes of action. 

In this webinar, learn how:

• Orthogonal use of biophysical techniques and combination of target-based and phenotypic approaches enables selection of most promising fragment series and leads.
• Isothermal Titration Calorimetry (ITC) can be used as a secondary screening tool in hit validation for proteins demonstrating limited stability in other orthogonal assays
• ITC is a good predictor of successful determination of protein-ligand co-crystal structures