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Glutamate Receptor Focused Library

Glutamate receptors are proved to play an important role in many neurological disorders. They are localized on neuronal and non-neuronal cells and are capable of mediating rapid excitatory synaptic transmission in the central nervous system. These receptors can regulate a wide range of processes in the brain, spinal cord, retina and peripheral nervous system. There are two major classes of glutamate receptors: ionotropic receptors and metabotropic receptors. Ionic glutamate receptors are ligand-gated channels whose agonists include AMPA, Kainate, and NMDA. Metabotropic glutamate receptors are a family of eight GPCR receptors that are promising drug discovery targets for modulating glutamate action and response.

BOC Sciences has carefully designed its proprietary library of glutamate receptor screening compounds containing more than 4,600 drug-like small molecule compounds to facilitate glutamate drug discovery programs.

Classification of ionotropic glutamate receptors (iGluRs). Figure 1. Classification of ionotropic glutamate receptors (iGluRs). (Hayashi, T. 2021)

Glutamate Receptor Focused Library Design

a. Firstly, we use a reference set of reported compounds showing dose-response activity (IC50, EC50, or Ki, etc.) for a glutamate receptor that are compiled based on relevant authoritative data (activity cut-off 10 uM):

  • Metabotropic glutamate (mGlu) receptors - 7,000 reference compounds
  • Ionic glutamate receptors - 5,000 reference compounds

b. Then, a 2D fingerprint similarity search (Tanimoto cut-off >0.8) is employed to examine the BOC Sciences HTS compound library for analogs of known glutamate receptor inhibitors

c. Finally, the following subset of glutamate receptor-focused libraries is generated:

  • Nearly 3,300 potential ligands of metabotropic glutamate receptors
  • Over 1,300 potential modulators of ionotropic glutamate receptor

Excitatory and inhibitory synapses. Figure 2. Excitatory and inhibitory synapses. (Hayashi, T. 2021)

Glutamate Receptor Focused Library Characteristics

  • No PAINS or toxic substances/unwanted functions: filtered by strict ‘Ro5-like’ physicochemical and most stringent in-house structural filters
  • Bioactivity and safety confirmed by preclinical studies and clinical trials
  • Structural diversity, medicinal activity, and cellular penetration
  • Structural document, IC50, and other chemical and biological data are provided
  • All compounds are continually updated
  • Compound cherry-picking service is available

What We Deliver

  • Delivered within 2 weeks in any customer-preferred format
  • Powders, dry films or DMSO solutions formatted in vials, 96 or 384-well plates
  • All compounds have a minimum purity of 90% assessed by 1H NMR and HPLC
  • Analytical data is provided

BOC Sciences provides professional, rapid and high-quality services of Glutamate Receptor Focused Library design at competitive prices for global customers. Personalized and customized services of Glutamate Receptor Focused Library design can satisfy any innovative scientific study demands. Our clients have direct access to our staff and prompt feedback to their inquiries. If you are interested in our services, please contact us immediately!

Reference

  1. Hayashi, T. Post‐translational palmitoylation of ionotropic glutamate receptors in excitatory synaptic functions. British Journal of Pharmacology. 2021. 178(4): 784-797.
Our mission is to provide clients with a professional chemical library design platform. Empowered by high-quality services and effective research solutions, we are committed to helping customers achieve effective and successful research goals.

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Services Based on the Chemical Library Design Platform

Services Based on the Chemical Library Design Platform

BOC Sciences has rich experience in working with global customers in custom library synthesis of compounds and generating small to medium-sized libraries of target compounds. Our knowledge in generating a large number of target molecules in a remarkably shorter time enables quick biological screenings for affinities. With the target properties in mind, we deliver target molecules, by applying our extensive knowledge in drug discovery.

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