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PathHunter® β-Arrestin Orphan GPCR assays
are whole cell, functional assays that directly measure GPCR
activity by detecting the interaction of β-Arrestin with the activated GPCR. Because Arrestin is known to interact with
the vast majority
of GPCRs in a G-protein independent manner, orphan GPCRs can be rapidly and efficiently screened or
profiled without knowing the second messenger signaling
of the target receptor. This direct measurement provides a system
unaffected by endogenous receptor and virtually eliminates false positive hits associated with other assays making this the
ideal platform to rapidly de-orphanize receptors.
Product Features
Largest menu of more than 90 Orphan GPCR assays available
Universal, G-protein independent β-Arrestin readout
Simple, single addition homogeneous assay
Large assay windows, exceptional Z' making it ideal for HTS
Demonstrated success in identifying novel receptor:ligand pairs
Technology Principle: How The Assay Works
PathHunter® β-Arrestin assays monitor GPCR activity by detecting the interaction of β-Arrestin with the activated GPCR using β-galactosidase (β-gal) enzyme fragment complementation (EFC) technology. Since β-Arrestin recruitment occurs independent of G-protein coupling, the assays provide a direct, universal platform for measuring receptor activation. Learn more»
Performance You Can Trust
For known GPCR targets well-characterized ligands can be used to validate the functional response of the assay. However, more than 100 Class A GPCRs are still classified as Orphans (oGPCRs), most likely due to a lack of second messenger response. Since no putative ligands exist for Orphan GPCR Receptors, DiscoveRx's oGPCRs Assays undergo extensive 3-step validation procedure to consistently ensure optimal, out-of-the box performance. Learn More»
Easily Deorphanize any Orphan GPCR
(Click on figure to enlarge)
Figure 1. Easily deorphanize any orphan GPCR using validated cell lines
(A) Expression of the GPR35 oGPCR receptor was confirmed by EAstern blot, as shown by the
presence of a 34 KD band (lane 3). (B) Dose response curve for Zaprinast, a “surrogate” ligand
for GPR35 showing a robust response to agonist.
For instrument compatibility, please click here.
PathHunter® Certified System
All PathHunter® Certified reagents have been designed, validated and optimized for use with each PathHunter® cell-based assay. Each PathHunter® cell-based assay combines pre-validated cell lines and reagents, providing you a convenient solution to minimize assay development and ensure optimal and reproducible results every time. Learn More»
(Click on figure to enlarge)
Figure 2. The PathHunter® System include engineered clonal cell lines validated for stable GPCR receptor tagged with ProLink™ and a β-Arrestin fused with enzyme acceptor (EA); as well as unique PathHunter® Certified Reagents especially optimized to yield high quality, reproducible results. These system utilize a simple, one-step addition protocol and standard chemiluminescent detection and are ideally suited for 96-, 384-, 1536-well compound screening.
Download the user manual 
Don't see your target?
Click here to explore our Custom Assay Development possibilities.
Don't want to do cell culture?
Bulk cell options are available with the purchase of any PathHunter clone. Package sizes range from 100 million to 3 billion cells. Bulk cells are functional tested for optimal assay performance and are confirmed to be Mycoplasma-free. Combine frozen, assay-ready bulk cells with PathHunter-Approved Cell Plating Reagent and Control Ligand to expedite your screening campaigns and ensure optimal and reproducible results every time. Click here for a quote.
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