GPCR cAMP Product Solutions

Homogeneous cAMP Detection Assay Solutions for Small Molecules and Biologics

cAMP cell-based assays measure cAMP levels in cells as a direct indication of GPCR functional status (activation or inhibition). This direct measurement is obtained by quantifying cellular cAMP accumulation levels in a dose-dependent manner with cell-based assays that are homogeneous and scalable.

Eurofins DiscoverX® provides robust, easy-to-use, and high throughput screening (HTS) HitHunter® cAMP cell-based assays that accurately detect cellular cAMP levels in a variety of applications without the need for wash steps, optimization, or specialized equipment. These versatile assays provide a simple, validated detection system in two different modes – adherent and suspension. The adherent-mode protocol has been validated across 125+ cAMP Hunter™ cell lines and is applicable to ChemiSCREEN™ and non-Eurofins DiscoverX cell lines. The suspension-mode protocol is faster and is currently validated for select Gs targets (GCGR, GLP-1R, GIPR) with cAMP Hunter cell lines, with ongoing phased expansion planned. Both formats deliver robust signal-to-background and consistent gain-of-signal responses. Easily obtain reproducible results with high sensitivity, rank order ligands based on molecular potency, or determine pharmacological profiles of your ligands.

Used in the screening of millions of data points and referenced in hundreds of peer reviewed publications ranging from basic research to clinical applications, these assays provide accurate pharmacology of your ligand or small molecules and biologics while giving you the flexibility to work with multiple cell lines and assay formats.

Product Highlights
  • Optional Formats – Select from hundreds of cell line assay kits, stable cell lines, frozen ready-to-assay cells, and assay ready eXpress and bioassay kits for chemiluminescent or fluorescent assay detection
  • Assay Ready Kits – Complete, ultra-convenient kits with optimized reagents for over 125 cAMP Hunter cell lines for monitoring GPCR activation using small molecules or biologics
  • High Throughput – Simple, rapid, and scalable assays that accurately detect cellular cAMP levels in 96-well through 3456-well formats
  • Validated Applications – Referenced products in over 400 peer reviewed publications ranging from basic research to clinical applications

Consider Eurofins DiscoverX’s custom development capabilities for custom cell lines, assays, & enzyme development.

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Products

Product Types

  • HitHunter cAMP Assays – Accurately detect cellular cAMP levels using biologics or small molecules ligands in a variety of applications. These Enzyme Fragment Complementation (EFC) based assays monitor GPCR activation through chemiluminescent detection of cAMP production in cAMP Hunter cell lines as well as non Eurofins DiscoverX cell lines.
  • GPCR cAMP Accumulation Bioassay Kits – Ready-to-use cell-based assay kits with a simple, homogenous protocol and are provided as qualified or target-based. These physiologically relevant, robust bioassays are fit-for-purpose for use in screening and characterization applications to potency testing in quality control lot-release programs. Learn more about Bioassay Kits.
  • GPCR cAMP Accumulation eXpress Assay Kits – Ready-to-use cell-based assay kits for quick analysis and implementation in early discovery phases for screening applications, proof-of-concept, mechanism of action confirmation, and rank-ordering studies. Learn more about eXpress Assay Kits.
  • GPCR cAMP Hunter Cell Line Assays – Complete cell-based assays (kits) that include a naturally coupled, stable cell line, chemiluminescent EFC-based HitHunter® cAMP reagents, and AssayComplete™ cell culture reagents. Learn more about Cell Line Assays.
  • ChemiSCREEN Cell Lines and Ready-to-assay Frozen Cells – Cells based on our proprietary Chem-1 and related host cell backgrounds that contain an endogenous expression of Gα15. Gα15 is a promiscuous G protein to help funnel signaling to a common calcium readout, regardless of G protein coupling status. Use cell lines or frozen cells with chemiluminescent or fluorescent assays, and parental cell lines to generate your own GPCR stable cell lines. Additional second messenger signaling, e.g. calcium mobilization, and ERK phosphorylation, for most targets can be used to perform orthogonal assay confirmation.
  • ChemiBRITE Cell Lines and Ready-to-assay Frozen Cells – Cells engineered to flash with added brightness upon GPCR activation and developed to provide the greatest readout flexibility, including luminescent and fluorescent calcium flux as well as cAMP. These cells express a proprietary mutant version of clytin, a calcium activated photoprotein.

Application Related Assays

  • β-Arrestin Assays – Universal G-protein independent cell-based assays to quantify GPCR activation based on the recruitment of β-arrestin. Ideal for ligand bias analysis, antagonist mode screening, and studying virtually any GPCR including orphan receptors.
  • Calcium Assays – Fluorescent dye-based assays to measure calcium mobilization in cell lines as a direct indication of GPCR or ion channel activation or inhibition.
  • GPCR Internalization Assays – Secondary, orthogonal screening cell-based assays for measuring GPCR desensitization and recycling as well as uncovering novel classes of compound pharmacologies and identifying safer drugs without imaging or antibodies.
  • Pharmacotrafficking Assays – Quantitative cell-based assays to identify small molecule pharmacochaperones that act as therapeutic agents to stabilize and correct disease-relevant mutant GPCRs, ion channels, or transporters.
  • Membrane Preparations – Purified membrane preps for obtaining GPCR and ion channel ligand binding affinities and evaluating GPCR activity through GTPγS functional studies in response to the addition of a ligand or therapeutic.
  • Obesity/Diabetes Assays – Accelerate the development of GPCR peptide therapeutics like GLP-1, GIP and glucagon for obesity and diabetes with MOA-reflective assays.