Give your lead generation programme the best possible start
Benefits
Diverse components of chemical space able to interact successfully with a particular binding site can be efficiently identified through screening of well-designed fragment libraries with only a few thousand members. Moreover, fragment-based methods tend to generate more efficient starting points for lead generation than traditional HTS-based methods. This is important since retrospective analyses have shown that ligand efficiency tends to decrease during lead generation and optimization of compound series. The weak interactions of fragments with proteins demand sensitive detection systems. High sensitivity combined with low protein consumption and flexible experimental design therefore makes SPR biosensor-based interaction analysis ideal for fragment screening.
Deliverables
1) High-quality fragment leads amenable for rapid and efficient lead generation
2) Initial SAR around the fragment hits
Technical Details
The fragment screening at Beactica is based on the efficient use of SPR biosensor-based techniques. Beactica’s Sprint™ software for ranking of fragments is used as a tool to prioritize among hits. Customers may chose from screening Beactica´s proprietary 2000-member fragment library, or screening their own internal libraries.
Figure. Examples of initial single-concentration fragment screening data for PKA with detection limits indicated by the red line (top). Dose-response curves shown for a few selected hits (bottom).
