Cell Lines GPCRs

GPCRs in Drug Discovery and Safety Pharmacology


A Single Platform Solution for In-House Studies with ChemiSreen™ GPCR Cell Lines

To meet the demands of HTS and selectivity profiling, our ChemiScreen™ stable cell lines were designed to provide robust data on a uniform platform. Most of our ChemiScreen™ cell lines were created in our proprietary host background, Chem-1, which contains endogenous expression of Gα15, a promiscuous G protein, to help funnel signaling to a common calcium readout, regardless of G protein coupling status. Additional second messenger signaling, e.g., cAMP and ERK phosphorylation, has been found for many targets, which can be used to perform orthogonal assay confirmation.

Advantages of ChemiScreen™ GPCR cell lines:

  • One of the largest GPCR stable cell line portfolios in the industry
  • Ability to assay both agonist and antagonist in a single well
  • High functional expression of receptors at the cell surface
  • Stable cell lines, tested for ≥6 weeks of continuous culture, for increased reliability and reproducibility
  • Single and simple functional readout
  • Signaling to calcium, regardless of G protein coupling status, for identical assay conditions and data analysis for straightforward comparative studies


ChemiBrite™ GPCR Cell Lines for Luminescent Assays

Engineered to flash with brilliance upon GPCR activation, our ChemiBrite™ stable cell lines were developed to provide the greatest readout flexibility, including luminescent and fluorescent calcium flux as well as cAMP. The ChemiBrite™ cells express a proprietary mutant version of clytin, a calcium activated photoprotein. These cells are available as either "tool box" reagents (parental line) to develop your own GPCR cell lines or as fully tested cell lines stably overexpressing a GPCR of interest.

Advantages of ChemiBrite™ GPCR cell lines:

  • High assay signal with exceptionally high signal-to-background ratio
  • No assay interference with autofluorescent compounds
  • Non-toxic substrate enables greater flexibility in scheduling assays
  • "Tool box" capabilities allows you to generate your own stable cell lines

Review our ChemiScreen™ and ChemiBrite™ cell lines here. 

For additional GPCR cell lines, visit Eurofins DiscoverX.