GPCR

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 ‘druggable’ targets.

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Our track record

Charnwood Molecular has delivered on multiple GPCR projects. We have particular expertise in assay development and screening, using Promega’s NanoBRET TM GPCR reagents.

Assay development

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

This technology can be applied to other GPCR’s with the benefits of:

  • Highly specific detection of binding interactions due to the inherent distance constrains 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

GPCR blog

Take a look at our blog  to learn more about GPCRs and their role in drug discovery:

Our success stories

View all case studies