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Until recently, ion channel drug discovery has been restricted by a deficiency of molecular and structural information, sub-optimal screening technologies and a lack of pharmacological tools. New scientific and technological advances have removed a number of these obstacles and revealed ion channels to be a pharmaceutically tractable target class with considerable therapeutic potential. Through BioFocus DPI, you gain access to an unrivalled combination of screening technologies, assay development expertise as well as our proprietary approach to ion channel library design.
Benefits
Expertise, speed and flexibility are the key advantages of BioFocus DPI’s ion channel drug discovery capabilities:
• SoftFocus ion channel libraries combined with electrophysiology based screening gives information-rich data and delivers highly validated hit molecules
• Proprietary Helical Domain Recognition Analysis software enables the design of compounds targeted to defined ion channels
• Cell line generation service that can deliver stable cell lines tailored to your specifications
• Electrophysiology-based ion channel screening capacity which exceeds 30,000 data points per week
• Hit evaluation and follow up with Giga ohm patch-clamp using 16 channel PatchXpress
• Biophysical properties and mechanism of action investigated with conventional patch clamp rigs
Applications
From the establishment of cell lines that stably express ion channels through to validating and performing high throughput screening assays - our scientists have the expertise to fast track your ion channel discovery research. Our screening technology is suited to primary screening campaigns across a broad range of both voltage- and ligand-gated ion channels. Detailed followup of hit molecules is available using conventional and high-throughput electrophysiology.
Technologies
For diverse library screens of 100,000+ compounds, we offer comprehensive expertise in using FLIPR384 and Hamamatsu FDSS6000 based fluoresence assays and microarrayed compound screening (µARCS) technology. When little or no pharmacological or structural information exists for a target, hits are best obtained using this approach. Alternatively, the SoftFocus or targeted library approach when combined with IonWorks Quattro automated electrophysiology gives a powerful and extremely rapid hit finding tool that can accelerate your early stage ion channel discovery research.
Case studies
1. Screening on IonWorks Quattro
Screening on IonWorks Quattro produces high quality electrophysiology data straight from the primary screen and can provide an indication of the mechanism of action of your compounds (e.g. open channel block). Direct screening by electrophysiology can also lead to identification of compounds that might be missed in other screening formats.
2. Cell line generation 
Using IonWorks Quattro it is now possible to screen more than 70 clones in an electrophysiology assay over a single working day, leading to the rapid selection of clones based on expression levels and suitability for electrophysiology.
