Specialist, cost efficient, ion channel high-throughput screening

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Assays to support hit finding, hit-to-lead, lead optimisation and selectivity profiling

The high-throughput screening of vast numbers of compounds is pivotal to the drug discovery process. It is often an expensive, timely, process which can return false positive results. What sets us apart is our specific high-throughput screening knowledge and experience across multiple ion channel targets.

By working with our ion channel high-throughput screening specialists you will have access to a dedicated and highly experienced team, with experience including high-throughput ion channel screening to support HTS campaigns, hit finding, hit-to-lead, lead optimisation and follow-up selectivity profiling. Custom cell line generation, assay development and optimisation is also provided in-house.

Once we have run your project, we will interpret the data, communicate the results and support your decision making to best inform your screening strategy.

Our complementary phenotypic and translational assays enable further detailed characterisation of your lead compounds. Read about our small molecule library and modular screening decks to suit your project and budget.

Screening against V434L KCNC1 using thallium flux assay. Read the drug repurposing high-throughput screeningcase study about a recent project researching a rare de novo variant in the KCNC1 gene.

Access to Enamine and Assay.Works compound libraries

To support your medicinal chemistry programmes and structure-activity relationship (SAR) studies, we offer access to commercially available compound libraries from Enamine and Assay.Works.

Case study: Multi-assay High-throughput drug repurposing screen: KCNC1

Our approach enabled a long-term Kv1.3 screening project to expand medicinal chemistry SAR and successfully identify selective small molecule modulators by accessing high quality APC and ion channel expertise. Through this long-term collaboration with a pharmaceutical company, Metrion delivered: exceptional long-term reliability of the optimised primary target screen and counter-screen assays over the course of two years, bespoke development of cell lines, including support of complete gene family selectivity and species selectivity studies, wider selectivity studies including extended cardiac (CiPA) panel screening, and exploration of mechanism of action (e.g. closed, open or inactivated state block).

Read the full Case Study

Small molecule library and modular screening decks 
to suit your project and budget

Figure 1: Physico-chemical property profile according to Lipinski’s Rule of 5 (left); Prediction of compound properties and drug-like features: Colloidal Aggregation, Permeability, Bioavailability, Solubility, PAINS.

Figure 2: Compound sets and diversity metrics based on Bemis-Murcko clusters.

A combined, flexible, approach for your high-throughput ion channel screening project

By screening across multiple platforms we offer flexibility and use technology and automated processes in synergy to progress your project as efficiently and cost-effectively as possible.

Ion Channel Screening Resource Library
Using high-throughput automated patch clamp electrophysiology to identify novel TREK-1 modulators in an animal venom library

We developed a high-throughput, electrophysiological assay of TREK-1 function to identify novel modulators. The assay was optimized to identify both activators and inhibitors, providing comprehensive mechanistic data for high value, limited supply screening libraries, such as the venom fraction library used in this study (Targeted Venom Discovery Array, T-VDA, Venomtech, UK).

Ion channel and HTS services

Specialist ion channel screening to accelerate early-stage screening and lead optimisation.

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Metrion Biosciences

Let’s work together

If you have any questions or would like to discuss your specific assay requirements, we will put you directly in touch with a member of our scientific team. Contact us today to discover more.
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Metrion Biosciences is a contract research organisation (CRO) specialising in high-quality preclinical drug discovery services.
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