Glutamate Receptor Focused Library

There are two broad categories of glutamate receptors: ionotropic receptors and metabotropic receptors (Figure 1). Ionotropic 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 attractive drug discovery targets to modulate glutamate action and response [1].

Classification of the glutamate receptors

Figure 1. Classification of the glutamate receptors

Life Chemicals has designed its proprietary Glutamate Receptor Screening Compound Library of over 4,600 drug-like small-molecule compounds to facilitate glutamate-based drug discovery projects.

First, a reference set of reported compounds showing dose-response activity (IC50, EC50, or Ki, etc.) on one glutamate receptors was compiled based on relevant publications and patents (activity cut-off 10 uM):

  • Metabotropic glutamate (mGlu) receptors – 7,668 reference compounds
  • Ionotropic glutamate receptors – 5,982 reference compounds

Life Chemicals HTS Compound Collection was checked for analogues of known glutamate receptor inhibitors utilizing a 2D fingerprint similarity search (Tanimoto cut-off > 0.8) on MDL public keys fingerprints. As a result, the following Glutamate Receptors Focused Library subsets were obtained:

  • almost 3,300 potential ligands of metabotropic glutamate receptors
  • over 1,300 potential modulators of ionotropic glutamate receptors

Compound cherry-picking is available. Custom compound selection based on specific parameters can be performed on request.

Please, contact us at orders@lifechemicals.com for any details and quotations.

You may also be interested in the N-methyl-D-aspartate (NMDA) Receptor Screening Library.

References:

  1. Llinas del Torrent, C.; Pérez-Benito, L.; Tresadern, G. Computational Drug Design Applied to the Study of Metabotropic Glutamate Receptors. Molecules 2019, 24 (6), 1098.
This site uses cookies. Some of these cookies are essential, while others help us improve your experience by providing insights into how the site is being used. By using our website, you accept our conditions of use of cookies to track data and create content (including advertising) based on your interest. Accept