Hit to Lead Integrating Fragment Based Drug Discovery with HTS Approaches

ZoBio offers a comprehensive hit to lead service utilizing its extensive knowledge and experience. Integrating fragment based drug discovery approaches with high-throughput screening (HTS) has proven to be very beneficial, especially in the target class of proteases and in the protein-protein interaction field where traditional HTS approaches have failed. The early stages of evolving the weak, often mM, hits derived from fragment screens can be particularly challenging. In many cases drug discovery and development corporations have been structured to efficiently evolve the µM hits typically derived from HTS. However, ZoBio offers a complete turnkey hit-to-lead projects that make the best use of early stage compounds from fragment based drug discovery.

The following output can be achieved from our projects:

• Orthogonally validated fragment hits against the target
• A predetermined number of independent series with bestpotency in the low μM range (lead-like compounds) and complete Structure-Analysis Relationship (SAR) analysis
• Validated biophysical assays
• Where appropriate structural biology enabled (X-ray or NMR)

For more information or to discuss hit to lead please contact us directly.