Drug discovery is a challenging activity. Identification of the right starting points is a key step in each and every successful drug discovery project.
The starting point might be a natural ligand or a molecule described in the literature, however it is more likely to be derived from a (ultra) high-throughput screening (HTS) campaign. HTS is a process of screening and assaying a large number of biological modulators against selected and specific targets. Using state-of-the-art robotics, data processing/control software, liquid handling devices, and sensitive detectors, HTS allows a quick and thorough test of millions of small molecules.
Pivot Park Screening Center (PPSC) is the leading European screening center, providing the expertise and capabilities to identify novel small molecule starting points for COILED’s Trained Immunity program. PPSC’s assay development services will provide the appropriate HTS assays in 1536-well are being developed and subsequently screened in a fully automated fashion. Potential screening hits will undergo rigorous and critical validation. The degree of validation may depend on the screening technology but will include:
- Confirmation of activity with a fresh sample with confirmed structure and purity
- No obvious undesirable chemical motifs or known toxicophores
- Selectivity against key undesired targets
- Structure-activity relationships and activity of close analogs
- Synthetic tractability and potential for IP