Identification of Ion Channel Modulators
Creative Bioarray is committed to providing clients with lead identification and characterization services by combining high-throughput analysis technology with classic drug development technology, accelerating the discovery and optimization of the activity of potential ion channel drug candidates. Our experts in the field of drug discovery will deeply communicate with you and specify the best strategy to meet your specific scientific research needs.
Introduction
Identifying appropriate small molecule drug leads with ideal chemical properties is one of the most challenging tasks in ion channel drug development. The identification and characterization of leads is a key factor in the successful development of ion channel drugs. Scientists have traditionally considered ion channels to be targets that are difficult to engage in a form of high-throughput functional screening, and large-scale screening campaigns often fail to achieve potent and selective hits. The pharmaceutical industry's long-standing focus on targeting G protein-coupled receptors, kinases, and other enzymes has led to a scarcity of acceptable ion channel leads.
The successful targeting of ion channels requires sensitive and powerful technologies that can detect a small number of active substances in large compound libraries. Counter-screening for possible off-target activities has also proved to be important for hit assessment and lead prioritization. Recently, the development of cell-based fluorescence screening technology has provided the possibility for efficient screening of libraries composed of millions of compounds to detect the true lead structures with sufficient initial potency and defined mechanisms of action.
Fig. 1 High-throughput biochemical and computational screening to support lead compound identification with respect to validation. (Sawyer, 2005)
Our Services
Characterization of screen hits using manual voltage clamping techniques has the disadvantage of being low-throughput, slow, and tedious. Our researchers are working on secondary screening of initial hits using new automated patch-clamp techniques. These techniques allow us to help our clients quickly identify the direct functional effects of compounds on the channel and determine their selectivity across the ion channel superfamilies. We have several different platforms dedicated to providing high-throughput analysis and quantitative measurement of channel activity, combining biophysical and biochemical methods to efficiently identify useful lead structures. Our lead identification and characterization services are available for virtually any member of the various ion channel superfamilies. Our services include but not limited to:
- Identification of sodium or potassium channel modulators
- Screening of ligand-gated ion channel modulators
- Detection of voltage-gated calcium channel effectors
- Identification of voltage-gated sodium channel effectors
Applications
- Improvement of pharmacodynamic and pharmacokinetic properties of compounds
- Ion channel drug discovery
- Development of target engagement indices
- Detection of the therapeutic potential of agents
With technical advantages in pharmaceutical chemistry and biology, and years of experience in the pharmaceutical R&D industry, Creative Bioarray has the strength to provide clients with professional lead identification and characterization services, which is conducive to the development of new clinical-related compounds. If you need scientific services in target validation, please contact us for more details.
Reference
- Sawyer, T. K. New screening tools for lead compound identification. Nature Chemical Biology, 2005, 1(3): 125-125.
