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 .
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 firstname.lastname@example.org for any details and quotations.
You may also be interested in the N-methyl-D-aspartate (NMDA) Receptor Screening Library.
- 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.