Ion Channel Hit Discovery

High-throughput identification of a compound’s ion channel efficacy, potency, specificity or potential for off-target effects in early drug discovery is available in fluorescence-based, automated patch clamp and conventional (manual patch) electrophysiology assays conducted against ion channels from a large collection (>120) expressed in mammalian cells. Off-the-shelf or custom assays are available for screening and profiling ion channel targets, including major cardiac, CNS and PNS channels.

Capabilities

  • Assay development and transfer
  • Fluorescence-based screens of up to 700,000 compounds (FLIPR® / Hamamatsu FDSS)
  • IonWorks® Quattro and IonWorks® Barracuda™ screens of up to 125,000 compounds per target (voltage-gated and ligand-gated ion channels)
  • Conventional as well as PatchXpress® and QPatch HT® automated electrophysiology for detailed pharmacological and biophysical follow-up studies
  • Ion channel selectivity profiling
  • Computational chemistry for knowledge-based compound deck selection from our 850,000 diverse compound library
  • Hit-to-lead and lead optimization support using fluorescence-based, automated and conventional electrophysiology
  • Custom cell line generation – single alpha subunits to more complex multi-subunit combinations, constitutive and inducible expression vectors
  • Access to fluorescence-activated cell sorting
  • Large-scale transient expression using MaxCyte® STX™, allowing 40 million to 10 billion cells per transfection

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high-throughput screening (HTS)

Assay Development and Screening

Charles River offers target class and cell biology expertise together with state-of-the-art instrumentation to provide services tailored to your requirements.