Fragment Screening - The CEfrag screen
Fragment screening has recently evolved to become a widely accepted approach to lead discovery. Selcia has established a proprietary approach using capillary electrophoresis (CE) to detect the weak binding interactions between fragments and therapeutic targets. CE has been used in the past by Cetek Corporation (Massachusetts, USA) as a sensitive and robust screening technology. Selcia has acquired the associated IP and has in addition developed new and proprietary methods tailored for screening fragments - the CEfrag Screen.
- High resolution analytical technique applicaple to charged and neutral molecules
- Compatible with fragments, conventional HTS libraries, natural extracts
- Very low protein consumption
- No need for highly pure protein
- Applicable to wide range of targets
- Solution based, involving a separation step: insensitive to aggregation phenomena
- No protein size limit
- Highly flexible: detection/monitoring of target, ligand, or target-ligand complex
- Detects wide range of affinities – from millimolar to picomolar
- Generates IC50 data
- Very low false positive rate
- Rapid assay development
Selcia’s approach offers an innovative and unique approach to identify low molecular weight compounds acting on your therapeutic target in a biologically relevant context. The CEfragTM Screen is particularly powerful to identify hits on traditionally difficult biological targets such as protein-protein interactions in a very short time. Leveraging our expertise in medicinal chemistry in combination with our fragment optimisation technology we can rapidly progress fragment programmes to identify novel lead structures and preclinical development candidates.
We have validated the CEfragTM Screen against a number of biologically relevant targets including peptidyl-prolyl isomerases, HSP90, and protein-protein interactions for therapeutic applications including inflammatory diseases, oncology, viral, fungal, and bacterial infections, metabolic and cardiovascular disorders, and CNS.
Selcia offers the CEfrag ScreenTM as a standalone service or in combination with our integrated discovery service. For the standalone service we can use the Selcia Fragment Library, the customer’s fragment library, or the microbial extract collections of our partners.