Fragment/Template Screening Platform

Sareum initiates the discovery of novel chemical matter using a fragment-based approach called template screening. Using this powerful and rapid methodology, our scientists have discovered novel inhibitors of different protein families, including protein kinases (ATP site and allosteric site), proteases and polymerases.

Templates are low molecular weight compounds of high solubility which are ideal starting points for optimisation into drug candidates. Using a multiple feature pharmacophore search, molecules for biochemical screening are computationally selected from Sareum's in-house collection of more than 8000 highly diverse templates and supplemented from our proprietary database of more than 150,000 commercially available templates.

The selected compounds are then biochemically screened using a range of assay types to identify binding hits. Hits are then taken forward into X-ray crystallography for structure solution with the chosen protein target. Only after a molecule has demonstrated biochemical binding and its structure solved in complex with the protein target, is it referred to as a 'Template Hit'. Template Hits are generally low potency inhibitors which have a high degree of novelty, as they are rarely identified using standard high throughput screening methods.

Although Template Hits are generally low potency inhibitors, they are rapidly optimised into high potency inhibitors using Sareum's high throughput medicinal chemistry platform, in combination with our computational and structure-guided drug design expertise.