Using Qube 384, we profiled a panel of NaV inhibitors across species, providing valuable translational insight early in analgesic drug discovery.
Successful ion channel drug discovery depends on robust and reproducible assay performance.
Our scientists specialise in:
Every assay is tailored to the specific target biology and project requirements to ensure generation of high-confidence pharmacology data.
Automated electrophysiology screeningAutomated patch clamp technologies enable medium- to high-throughput ion channel screening while maintaining high-quality electrophysiological data.
Our scientists also have extensive experience applying automated patch clamp to biologics discovery programmes. By optimising experimental parameters such as incubation time, stimulation protocols and channel state, we generate robust functional data to evaluate the potency, efficacy, subtype selectivity and mechanism of action of ion channel biologics.
Our automated electrophysiology services support:
We have extensive experience using the Sophion Qube automated electrophysiology platform to deliver robust and reproducible assays across a wide range of ion channel targets.
Figure 1. Example recording of hASIC1a inward current recorded on the Qube automated electrophysiology platform. Cells are held at -60 mV with ASIC1a activated by the addition of extracellular solution buffered to pH 6.3 (black trace). The effect of inhibitor, diminazene, at 100 nM and 30 µM on the inward current is displayed in the blue and red traces, respectively.
Figure 2. Diminazene concentration-response curve displaying an IC50 of 1.13 µM (pIC50 = 5.95).
Figure 3. The pIC50 values of the reference compound, diminazene, against ASIC1a included in the Qube experiments when supporting Medicinal Chemistry Hit-to-Lead activities.
Manual patch clamp electrophysiologyManual patch clamp remains the gold standard for detailed ion channel characterisation and complex pharmacological investigations.
Our experienced electrophysiologists use manual patch clamp approaches for:
Manual patch clamp is particularly valuable for biologics programmes requiring detailed mechanistic investigation. Our electrophysiologists develop bespoke protocols to characterise complex pharmacology, including state-dependent modulation, slow binding kinetics, partial channel modulation and protocol-dependent activity that may not be captured using standard screening assays.
Fluorescence-based ion channel assaysFluorescence-based assays provide efficient higher-throughput approaches for ion channel screening and profiling.
We develop and optimise assays including:
These platforms can provide effective screening solutions for large compound libraries and complement electrophysiology-based approaches during screening cascades.
We support early-stage screening programmes for small molecules and biologics with robust assays designed to identify and confirm active compounds against ion channel targets.
Our rapid screening workflows generate high-quality SAR data to guide medicinal chemistry decision-making and accelerate progression of promising series.
Detailed electrophysiology and mechanistic pharmacology studies support optimisation of potency, selectivity and developability.
We provide ion channel safety profiling services, including hERG screening and selectivity assessment, to help identify potential liabilities early in development.
Our scientists conduct detailed biophysical and pharmacological investigations to characterise compound behaviour and support translational decision-making.
We support a broad range of ion channel families and therapeutic targets.
If your target is not listed, please contact us to discuss bespoke assay development options.
As a specialist ion channel CRO, Metrion has extensive experience supporting both small molecule and biologics discovery programmes. Our electrophysiologists combine deep expertise in ion channel pharmacology with automated and manual patch clamp to develop assays that generate robust, pharmacologically meaningful data. Rather than applying standard protocols, we tailor assay design to the biology of each target and the characteristics of each therapeutic modality, enabling confident decision-making throughout discovery.
We combine robust assay design with rigorous quality control to generate reliable, reproducible ion channel pharmacology data. Our scientists develop and optimise assays to support consistent performance, reliable compound profiling and confident decision-making throughout drug discovery programmes.
Every programme is tailored to your scientific objectives, target biology, pharmacology and project timelines. We support a wide range of ion channel assay formats, screening strategies and mechanistic pharmacology studies.
We understand the importance of timely data generation during hit identification, hit-to-lead and lead optimisation programmes. Our workflows are designed to support efficient progression of ion channel drug discovery projects.
Our services span ion channel screening including high-throughput screening, neuroscience and cardiac safety to support progression through the discovery pipeline. This includes automated electrophysiology, manual patch clamp and fluorescence-based ion channel assay platforms. We also provide ready-to-go and customised cell lines engineered for reliable, reproducible screening success.
We provide access to commercially available compound libraries, including Assay.Works and Enamine collections, with freedom to operate to support ion channel screening and profiling programmes.
Automated patch clamp is an electrophysiology technique that enables higher-throughput measurement of ion channel activity while maintaining high-quality functional data. It is widely used in drug discovery screening and lead optimisation.
Electrophysiology directly measures ion channel currents and provides detailed functional data. Fluorescence assays are typically higher throughput but provide indirect measurements of ion channel activity.
Common ion channel targets include sodium (Nav), potassium (Kv), calcium (Cav), TRP, ASIC and ligand-gated ion channels such as GABA and NMDA receptors.
hERG screening assesses compound activity against the hERG potassium channel to identify potential cardiac safety liabilities during drug development.
Yes. We specialise in developing customised ion channel assays tailored to specific targets, pharmacology and project requirements.
Yes. Metrion supports both small molecule and biologics drug discovery programmes targeting ion channels. Our experienced electrophysiologists develop tailored automated and manual patch clamp assays to characterise monoclonal antibodies, nanobodies, engineered peptides and other biologic modalities. By optimising assay protocols for each target and therapeutic approach, we generate robust functional data to support hit validation, lead optimisation and mechanistic characterisation.
Using Qube 384, we profiled a panel of NaV inhibitors across species, providing valuable translational insight early in analgesic drug discovery.
We explore hNav1.9's unique fast and slow inactivation properties using Qube 384 and QPatch 48 platforms, helping to build more predictive screening assays for state-dependent inhibitors.