- Give your lead generation programme the best possible start
Benefits
Beactica’s Sprint™ fragment library is designed for diversity and has proven to be suitable for SPR biosensor-based screening (Elinder et al., J Biomol Screen. 2010). Sufficient material of all compounds is available for hit follow-up analyses. Commercial availability of analogues to fragments in the library allows for rapid SAR-by-catalogue hit expansion. High hit rates enable a shift in focus from quantity to quality of hits. For example, specificity, binding site location and thermodynamic profile of hits can be included as hit criteria.
Deliverables
A fragment library that is:
- Validated for SPR-based biosensor screening
- Composed of structures well suited for SAR by catalogue
- Amenable for screening against diverse target classes
- Designed to discover the best polar interactions right from the start
Technical Details
The Sprint™ fragment library was compiled from approx. 5 million commercially available building blocks and screening compounds. Application of physico-chemical and structural property filters, followed by diverse subset selection yielded a library of 1946 fragments, which were acquired from 16 different vendors. The Sprint™ fragment library is stored in 96-well plates in 100% DMSO at a stock concentration of 50 mM, ready for dilution and screening. Carboxylic acids and aliphatic amines are plated separately, so that they can be screened as subsets for suitable targets.
Multivariate physico-chemical description of the Sprint™ fragment library illustrating its distribution over property space (left). The possibility for a fast SAR by catalogue follow-up of fragment hits is illustrated by the cumulative availability of commercial analogues to fragments in Sprint™ fragment library indicating (right).
