GPCRs (G protein-coupled receptors) are the largest and most diverse family of membrane proteins that transduce extracellular stimuli into intracellular signals. They regulate a wide variety of physiological processes and are also well-validated drug discovery targets.
Our GPCRs Track Record
Given the significance of GPCRs as key targets, we have developed our in-house expertise in this area. Consequently, Charnwood Discovery’s bioscience team has a strong track record of delivering on multiple GPCR drug discovery projects. As a result, this ensures that you achieve the best possible outcomes for your project.
Assay Development
We have particular expertise in assay development and screening, using Promega’s NanoBRETTM GPCR reagents.
Coupled with our in-house expertise, this format has significant advantages over traditional methods of compound profiling in 2D well plates:
- Cells adhere to scaffolds and thus, can be effectively moved between plates, replacing buffers without washing and providing the ability to use ‘assay ready compound plates’
- Cells can be cryo-preserved on scaffolds, then defrosted and used repeatedly from the same stock or batch, therefore improving data consistency
Applying the Technology to other GPCRs
When applied to other GPCRs this technology provides the benefits of:
- Highly specific detection of binding interactions due to the inherent distance constraints of BRET
- Small and minimally interfering bioluminescent peptide tag
- Selective cell surface detection
- Non-radioactive and homogeneous live cell assay
- High throughput – can be used for compound profiling in HTS formats
