Ion Channel Assays and Functional Profiling Services

CD Biosynsis offers comprehensive Ion Channel Assays, which are fundamental for drug discovery programs in neuroscience, cardiovascular health, pain management, and oncology. Ion channels are highly validated therapeutic targets, controlling membrane potential, cellular excitability, and signaling. Our platform delivers quantitative measurement of channel function, including activation, inactivation, and block, as well as precise inhibitor potency (IC50) determination. We utilize state-of-the-art technologies, including automated patch clamp (APC), manual patch clamp, and high-throughput fluorescence-based assays (e.g., membrane potential dyes, flux assays). Researchers can select and combine individual channel families and subtypes to build a custom profiling panel, enabling rapid and detailed characterization of compounds against critical voltage-gated, ligand-gated, and mechanosensitive ion channels.

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High-Throughput and High-Fidelity Ion Channel Characterization

Targeting ion channels requires high fidelity assays to accurately capture the complex gating and pharmacological properties of these targets. Our platform is designed to handle the diverse nature of ion channels, providing both rapid screening and detailed mechanistic profiling. We offer selectable panels that allow clients to focus on specific therapeutic areas—for instance, profiling compounds against cardiac channels (hERG, Nav1.5) for safety assessment, or pain-related targets (Nav1.7, TRP channels) for analgesic discovery. By enabling custom selection of subtypes and assay methods (electrophysiology vs. flux), we ensure that your lead compounds are characterized with the specificity and reliability needed for successful preclinical development.

Customizable Ion Channel Target Profiling

Voltage-Gated Channels (VGICs) Ligand-Gated & Other Channels Assay Types and Mechanistic Modules

Selectable Voltage-Gated Ion Channels (VGICs)

Choose Key VGIC Targets for Functional Profiling

Check the box next to the Voltage-Gated Channel subtype you wish to include in your customized assay panel:

Nav1.5 (Cardiac Safety/Arrhythmia)

Nav1.7 (Pain Management)

Kv1.3 (Immunology/Autoimmunity)

Cav1.2 (L-Type Calcium Channel)

hERG (Cardiac Safety Screening)

Kv7.2/7.3 (KCNQ, Epilepsy)

HCN4 (Pacemaker Channel)

Full Nav/Cav/Kv Safety Panel (Inquire)

Selectable Ligand-Gated and Other Channels

Choose Additional Channel Targets for Screening

Select the Ligand-Gated, TRP, or other channel targets for activity and inhibitor screening:

TRPA1 (Transient Receptor Potential A1)

GABAA Receptor (Neurotransmitter Gated)

P2X7 Receptor (ATP-gated)

ASIC1a (Acid-Sensing Ion Channel)

nAChR (Nicotinic Acetylcholine Receptor)

Glycine Receptor

CFTR (Cystic Fibrosis Transmembrane Conductance Regulator)

All available TRP Channels (Inquire)

Available Assay Types and Mechanistic Modules

Select the Quantitative and Mechanistic Services

Automated Patch Clamp (APC)

High-throughput voltage/current clamp assays for accurate IC50, state-dependence, and kinetic analysis.

Manual Patch Clamp (Gold Standard)

Detailed, low-throughput characterization for complex gating properties and advanced mechanistic studies (Ki, MoA).

Flux & Membrane Potential Assays

High-throughput, non-electrophysiological assays using fluorescent dyes or radio-labeled ions for screening campaigns.

Ion Channel Functional Assay Workflow

A rigorous process from cell line validation to detailed mechanistic characterization.

Channel Selection and Cell Line Prep

Assay Optimization and HTS Screening

Electrophysiology Confirmation (APC)

Advanced Kinetics and Reporting

Channel Selection: Finalize the list of ion channels based on client selection and screening needs (e.g., safety or efficacy targets).

Cell Line QC: Ensure stable expression and functional quality of the recombinant channel in validated cell lines.

Assay Choice: Select the appropriate method (APC for speed, Manual for detail, or Flux/Dye for HTS).

Potency Screening: Perform dose-response analysis to calculate preliminary IC50 values using the HTS or APC platform.

Mechanism of Block: Determine voltage dependence, frequency dependence, and use-dependence of the compound using automated patch clamp.

Confirmation: Run full dose-response curves via APC to validate IC50 results from HTS or preliminary data.

  • Detailed Kinetics: Perform manual patch clamp (if selected) to obtain precise activation, inactivation, and deactivation parameters.
  • Ki and MoA: Determine the inhibition constant (Ki) and confirm the mode of inhibition (open channel block, closed state block, etc.).
  • Reporting: Deliver comprehensive reports including current traces, voltage protocols, IC50/Ki values, and mechanism analysis.

Precision and Throughput in Ion Channel Screening

Automated Patch Clamp (APC)

           

High-throughput, reliable electrophysiology for rapid IC50 determination and early safety profiling (e.g., hERG).

Gold Standard Manual Patch

           

Detailed characterization of complex ion channel kinetics and state-dependent block for lead optimization.

Target Flexibility

           

Access to a wide array of voltage-gated, ligand-gated, and TRP channels in validated expression systems.

Custom Gating Protocols

           

Development of specific voltage or ligand protocols to accurately mimic physiological or pathological states.

Client Testimonials on Ion Channel Assays

"The hERG screening via Automated Patch Clamp was rapid and reliable, providing the necessary cardiac safety clearance for our preclinical candidates efficiently."

Dr. Samuel Liu, Safety Pharmacology Lead

"The manual patch clamp analysis on our Nav1.7 inhibitor was superb. They confirmed the closed-state dependence, which was key to developing a highly selective analgesic."

Ms. Clara Davis, Neuroscience Drug Discovery

"Profiling our Kv1.3 lead against a panel of 10 off-target ion channels provided a clear selectivity window, validating our approach for autoimmune therapy."

Mr. Julian Chen, Therapeutic Discovery Lead

FAQs about Ion Channel Assays

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What is the difference between APC and Manual Patch Clamp?

Automated Patch Clamp (APC) is a high-throughput method ideal for screening large numbers of compounds and determining IC50 values. Manual Patch Clamp is the gold standard for detailed mechanistic studies, allowing fine control over voltage protocols and solution changes.

Why is hERG screening essential for drug safety?

The hERG (Kv11.1) potassium channel is critical for cardiac repolarization. Inhibition of hERG can prolong the QT interval, leading to a potentially fatal arrhythmia (Torsades de Pointes). Therefore, hERG screening is mandatory for almost all new drug candidates.

What is state-dependent inhibition?

State-dependent inhibition occurs when a compound preferentially binds to and blocks the ion channel in a specific conformational state (e.g., open, closed, or inactivated). This property is crucial for achieving therapeutic selectivity (e.g., blocking only activated pain channels).

Can you perform assays on native cell lines (not recombinant)?

Yes. While recombinant cell lines are preferred for HTS due to stable expression, we perform manual patch clamp and flux assays on native cell lines (e.g., cardiomyocytes, primary neurons) to ensure pharmacological relevance.

How much does Metabolic Engineering services cost?

The cost of Metabolic Engineering services depends on the project scope, complexity of the target compound, the host organism chosen, and the required yield optimization. We provide customized quotes after a detailed discussion of your specific research objectives.

Do your engineered strains meet regulatory standards?

We adhere to high quality control standards in all strain construction and optimization processes. While we do not handle final regulatory approval, our detailed documentation and compliance with best laboratory practices ensure your engineered strains are prepared for necessary regulatory filings (e.g., GRAS, FDA).

What to look for when selecting the best gene editing service?

We provide various gene editing services such as CRISPR-sgRNA library generation, stable transformation cell line generation, gene knockout cell line generation, and gene point mutation cell line generation. Users are free to select the type of service that suits their research.

Does gene editing allow customisability?

Yes, we offer very customised gene editing solutions such as AAV vector capsid directed evolution, mRNA vector gene delivery, library creation, promoter evolution and screening, etc.

What is the process for keeping data private and confidential?

We adhere to the data privacy policy completely, and all customer data and experimental data are kept confidential.

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