High quality ion channel screening services using a variety of electrophysiology, label free and fluorescence-based platforms are offered by Metrion Biosciences. Our assay technologies include QPatch and Patchliner automated electrophysiology, conventional electrophysiology, impedance/microelectrode array techniques and FlexStation.
Cell Line Optimisation for Ion Channel Screening
The Metrion team has extensive experience of developing, optimising and validating stable cell lines expressing recombinant and endogenous ion channels to help develop robust screening assays. As an illustration of this, we developed a Nav1.8 assay on the Patchliner (Nanion). Initially, one of the major limiting factors was the poor expression associated with the original Nav1.8 recombinant cell line. Metrion optimised the cell line and tissue culture conditions to increase Nav1.8 expression, allowing the development of a highly efficient SAR profiling assay.
Ion Channel Screening Assay Development
For more than a decade, Metrion’s scientists have been involved in developing, optimising and validating automated and manual patch clamp assays for ion channel targets. We can fully customise ion channel assays at different stages of the screening cascade, from hit finding and medium throughput structure activity studies, through to specialised biophysical and mechanism-of-action studies for hit series or lead compounds. For example, Metrion developed a Kv1.1/(1.2)3 assay on the QPatch that could accurately identify compounds that bind to different channel states. This assay format has been successfully employed for other voltage gated Kv1.x channels, including Kv1.3.
Ion Channel Screening Library
We offer validated ion channel screening services against a wide range of ion channels in our library, such as the Kv1.x panel shown below, and a variety of targets available from commercial vendors. We are always seeking to expand our library of ion channel cell lines, please contact us to determine if we can assist you with an ion channel of interest or any of the above services.
- We provide compound screening in both single concentration point and concentration-response formats using our in house library of stable cell lines, client provided cell lines or transiently transfected cells. We also offer our CiPA-compliant cardiac safety panel and translational neuroscience assays.
- We offer detailed biophysical studies to characterise compound mechanism of action. Metrion’s scientists have routinely investigated state-dependent inhibition of a variety of voltage-gated ion channels over the last 10 years using both manual and automated patch clamp platforms (e.g. Nav, Cav, hERG and other Kv).