GPCR Screening and Profiling Services

Choose the Best Molecules for Preclinical and Clinical Study

Developing and validating cell-based assays during drug discovery is expensive and can take months to complete. However, data is needed in days or weeks instead of months. To help meet aggressive timelines, GPCR Screening and Profiling Services from DiscoverX provide the most comprehensive cell-based assay offering along with the fastest turnaround time in the industry for rapid efficacy, potency, and selectivity determination during SAR and Lead Optimization.

With over 600 cell-based assays for human and orphan GPCRs, available in multiple direct functional readouts, including second messenger signaling, arrestin recruitment, and receptor internalization, these services provide you ultimate flexibility to choose the ideal screening platform to meet your project needs. Whether your focus is hit identification, selectivity profiling, or lead optimization, these services can reduce the time and cost of GPCR drug discovery.

Learn more about DiscoverX GPCR Screening and Profiling Services and view available readouts.

 

Unlocking GPCRs for Oncology

G protein-coupled receptors (GPCRs) are the most commonly exploited drug target in modern medicine. In recent years, researchers have increasingly implicated specific GPCRs as promising therapeutic targets for oncology, resulting in an increased focus on targeting these receptors. Watch this webinar to see the power of GPCR profiling in identifying the target for a candidate molecule.

Watch Webinar

Target ID & Selectivity Determination with Broad Panel Profiling


gpcrMAX Screening and Profiling

Validate new targets or identify off-target liabilities early to rapidly move your best drug candidates into clinical trials. gpcrMAX offers the largest commercial panel of functional cell-based assays with a coverage of 60 distinct receptor families including Adrenergic, Dopamine, P2Y, Serotonin and many others.

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Deorphanize Orphan GPCR Programs


orphanMAX Screening and Profiling

Uncover novel ligand and receptor pairings during any ligand fishing or de-orphanization campaign using G-protein independent readout. orphanMAX provides the largest collection of functional cell-based assays for liganded and non-liganded orphan GPCR receptors. The panel includes a collection of 73 human orphan GPCRs that utilize PathHunter® Arrestin recruitment technology.

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Easily Determine Compound Potency & Rank Ordering


gpcrE/IC50ELECTsm Screening and Profiling

Quantitate compound potency against any GPCR functional cell-based assay. EC50s and IC50s are calculated from duplicate 10-point dose-response curves.  Measurements are made under optimized conditions to generate consistent and reproducible data that reliably reflects the drug’s potency. gpcrE/IC50ELECT is an ideal follow-up study tool to quantify the potency of interactions identified in primary screens, supplement existing data, or support lead optimization and SAR activity.

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Economical Custom GPCR Assay Screens


gpcrELECT Personalized Screening and Profiling

gpcrELECT provides you access to the world's largest menu of naturally coupled known, orphan, and ortholog GPCR cell lines. Select your target in any one of our convenient assay formats – Arrestin recruitment, 2nd messenger signaling (cAMP or calcium) or receptor internalization. This simple, fast, and cost-effective alternative to in-house profiling and screening is ideal for any size compound collection.


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Quantitate Ligand Bias


gpcrBIASsm Screening and Profiling

DiscoverX offers the largest portfolio of GPCR assays and a novel service that utilizes state of the art tools for characterization of ligand bias. With the appropriate β-arrestin, internalization, and second messenger assays to quantify selective response and statistical tools to scale these effects, harnessing bias to produce selective ligands is now made simple.

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Screen Multiple Biological Targets Simultaneously


GPCR scanLibrarysm Screening and Profiling 

In contrast to the traditional drug discovery model where a target is nominated on the basis of biology and screened against a compound library for putative hits in a single-target high-throughput screening (HTS) campaign, GPCR scanLIBRARY affords researchers the ability to screen an entire compound library against multiple biological targets of interest simultaneously.


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Screen Molecules Against Focused Therapeutic Area Panels


gpcrPanels Therapeutic Disease Panels

gpcrPanels offers focused therapeutic area assay panels for CNS, Metabolic, Ocular, and other panels that may be used to broadly screen for new leads or profile compounds of interest. These panels are organized based on current scientific understanding and are updated regularly.

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Validate GPCRs In-House


Cell Lines and Ready-to-Use Kits for In-House Validation

Choose from over 600 naturally-coupled GPCR cell lines designed to detect GPCR signaling through second messenger activation, β-arrestin recruitment, receptor internalization, and pharmacotrafficking. Offered in stable clonal cell lines and cryopreserved ready-to-use cells. With human and ortholog GPCR assays in a wide variety of functional readouts, you have flexibility to choose the ideal platform for your specific needs.


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Custom Assay Development Services

Can't find your assay on the menu? We can develop it for you. Learn More
 

GPCR Screening & Profiling Resources

gpcrMAX Sample Report Download
Panel Profiling Dates
Panels are run on scheduled dates throughout the year. Compounds, paperwork, and PO must be received by the compound submission dates found in the links above.

Webinars

Understand Safety and Selectivity of Drug Candidates Before Expensive Animal Studies Watch Webinar
Building Relevant Cell-Based Assays for Co-Stimulatory & Co-Inhibitory Checkpoint Receptors Watch Webinar
 

Drug Discovery Educational Insights

Allosteric Modulators of GPCR: PAM and NAM Curves  Watch Recording
 

Case Study

gpcrMAX and orphanMAX Panel Case Study  Ready Case Study
 

Brochures and Flyers

PathHunter Screening and Profiling Services Brochure Download
Integrated In Vitro Pharmacology Services Brochure Download