Focused Screening Libraries

The screening collection design described above is aimed at providing a diverse sample collection that can be used to screen against a variety of biological targets. However for some biological targets the nature of the molecular target is well defined and a case can be made for only screening a preselected sub-set of compounds, or even compounds not contained in the screening collection. This may also be important in cases where the assay is not of sufficient throughput to support a large HTS campaign.

Examples might include:-

• Know bioactives
• Kinase targets
• Well known structural motifs
• Protease Inhibitors
• Aspartic Protease Inhibitors
• Cysteine Protease Inhibitors
• Serine Protease Inhibitors
• Metalloprotease Inhibitors
• Ion Channels
• GPCR ligands
• CNS Penetrant Compounds
• Inhaled drugs
• Physicochemical properties will be very different from oral drugs
• Topical targets
• No need for oral activity
• Natural Products
• The structures may not comply with the “rule of five” but they have been a rich source of leads particularly anti-infectives

Updated 10 March 2012