Ready for Growth: A New Generation of Highly Versatile Fragment Libraries

Careful design and maintenance of our fragment library is of great importance to the ZoBio lead discovery process. Continuous improvement of our collection relies both on commercial acquisition of new fragments and gaining access to unique and novel compounds. We are keen to engage in partnerships with industrial and academic partners to explore new fragment bioactive space and therefore we accepted the invitation to join the consortium of Radboud University (RU), Vrije Universiteit Amsterdam (VU) and Symeres whose goal is to generate novel 3D fragment libraries.

The project is led by the research groups of Prof. Iwan de Esch at the VU and Prof. Floris Rutjes at the RU with funding from the TTW program of the Dutch Research Council (NWO). The teams will focus on the synthesis of 3D shaped, small-sized rings utilizing nonclassical synthetic techniques such as high pressure cycloaddition and flow-photochemistry. Subsequently the performance of the compounds will be evaluated in fragment screening campaigns. The unique compounds will be carefully designed based on desired physicochemical properties. Regular triaging during the synthesis campaign will ensure only high-quality fragments enter the final library that will be screened against multiple protein targets. Since these targets have all previously been subjected to fragment screening, it will be of great interest to see the further value provided by this previously unexplored part of fragment chemical space. Naturally the well behaved fragments will be used to enhance the ZoBio fragment library.

ZoBio is delighted to collaborate with these top Dutch researchers and contribute to this great program!