How It Works - PathHunter® Profiler Kit Assay Principle

The PathHunter® eXpress GPCR Profiler Kit let you mix-and-match up to 10 different GPCR targets to build a customized panel of assays. Select from over 350 targets available in β-Arrestin recruitment, cAMP accumulation, or GPCR internalization readouts and generate accurate, precise and reproducible data on a unique group of GPCR targets.


Customize your own kit or choose from our most popular kits.

Build Your Own Kit

The Profiler kit is applicable at various stages of drug discovery whether it be target validation, lead optimization, SAR or pre-clinical study. The ability to mix and match targets and assay platforms  has numerous benefits allowing you to explore the selectivity within a target family, uncover off-target effects, confirm novel receptor:ligand pairings for multiple orphan receptors or determine mechanism of action of by comparing the activation and internalization profiles of your lead compound . Profiler kits also let you compare pharmacology between human and ortholog targets to determine effective compound dosing prior to expensive animal models.

Target Selection Guide

PathHunter eXpress β-Arrestin Assay

cAMP Hunter eXpress Assay

PathHunter GPCR Internalization Assay

Kit Components

  • 10 Assay-ready, frozen eXpress vials
  • 10 Optimized Cell Plating Reagent bottles
  • PathHunter or cAMP HunterTM Detection Reagents
  • 10 X 96-well Tissue Culture Treated Plates

Our Most Popular Kits

Customers have taken advantage of our extensive menu to fuel their drug discovery programs.  Choose from the various kits below to get started today!

 
Chemokine receptors and their associated ligands play a key role in both normal and pathological conditions. Understanding their regulatory roles in various disease states such as allergic reactions, cardiovascular disease, metabolic syndromes, sepsis and cancer is critical to the development of safe and efficacious therapeutics. Our complete panel of chemokine receptors utilizes a single common assay readout to rapidly, reliably and reproducibly screen and profile compounds.

Chemokine Profiler™ Kit 1  Request a Quote

Qty Family GPCR Gene Coupling PathHunter® eXpress β-Arrestin
1 vial Chemokine CCR2 Gi/Go 93-0192E2CP0S
1 vial Chemokine CCR3 Gi/Go 93-0388E2CP0S
1 vial Chemokine CCR4 Gi/Go 93-0193E2CP0S
1 vial Chemokine CCR5 Gi/Go 93-0224E2CP0S
1 vial Chemokine CCR6 Gi/Go 93-0194E2CP0S
1 vial Chemokine CCR7 Gi/Go 93-0195E2CP0S
1 vial Chemokine CCR8 Gi/Go 93-0196E2CP0S
1 vial Chemokine CCR9 Gi/Go 93-0296E2CP0S
1 vial Chemokine CCR10 Gi/Go 93-0276E3CP5S
1 vial Apelin AGTRL1 Gi/Go 93-0250E2CP0S
 

Chemokine Profiler™ Kit 2  Request a Quote

Qty Family GPCR Gene Coupling PathHunter® eXpress β-Arrestin
1 vial Chemokine CMKLR1 Gi/Go 93-0313E2CP0S
1 vial Chemokine CX3CR1 Gi/Go 93-0290E2CP0S
1 vial Chemokine CXCR1 (IL8RA) Gi/Go 93-0226E3CP0S
1 vial Chemokine CXCR2 (IL8RB) Gi/Go 93-0202E1CP0S
93-0202E2CP0S
1 vial Chemokine CXCR3 Gi/Go 93-0271E2CP2S
1 vial Chemokine CXCR5 Gi/Go  93-0514E2CP2S
1 vial Chemokine CXCR5 Gi/Go 93-0204E3CP0S
1 vial Chemokine CXCR6 Gi/Go 93-0205E1CP0S -or-
93-0205E2CP2S
1 vial Chemokine CXCR7 N/A 93-0248E2CP2S
1 vial Apelin AGTRL1 Gi/Go 93-0250E2CP0S
Bioactive lipids cause pain and inflammation and their dysregulation can lead to a variety of diseases including cancer. Our panel of lysophospholipid receptors allows you to explore the interaction of lipids with various members of this important therapeutic class using a simple chemiluminescent homogenous assay platform.
 

LPA & S1P Profiler™ Kit  Request a Quote

Qty Family GPCR Gene Coupling PathHunter® eXpress β-Arrestin PathHunter®  eXpress Internalization
1 vial Lysophospholipid EDG1 Gi/Go 93-0207E2CP4S  
1 vial Lysophospholipid mEDG1 Gi/Go 93-0476E2SCP4S  
1 vial Lysophospholipid EDG1 Gi/Go   93-0784E1CP28S (Total)
1 vial Lysophospholipid EDG3 Gq 93-0217E2CP0S  
1 vial Lysophospholipid EDG4 Gq 93-0255E2CP13S  
1 vial Lysophospholipid EDG5 Gs 93-0256E2CP0S  
1 vial Lysophospholipid EDG7 Gq 93-0636E2CP13S  
1 vial Lysophospholipid GPR92 Gq 93-0372E2CP6S  
1 vial Class A Orphan GPR120 N/A (L) 93-0366E2CP0S  
1 vial Apelin AGTRL1 Gi/Go 93-0250E2CP0S  
Opioid receptor targeted drugs are used to treat pain, addiction and anxiety. However, their clinical effectiveness can be limited by the development of analgesic tolerance, which correlates with the amount of desensitized and internalized receptor. Profiler kits let you explore Opioid receptor activation or internalization in response to compound challenge using a simple, non-radioactive cell-based chemiluminescent readout
 

Opioid Profiler™ Kit  Request a Quote

Qty Family GPCR Gene Coupling PathHunter® eXpress β-Arrestin PathHunter®  eXpress Internalization cAMP HunterTM eXpress
1 vial Opioid OPRD1 Gi/Go 93-0400E2CP2S    
1 vial Opioid OPRD1 Gi/Go   93-0673E3CP0S (Active)  
1 vial Opioid OPRD1 Gi/Go     95-0108E2CP2M
1 vial Opioid mOPRD1 Gi/Go 93-0611E2SCP0S    
1 vial Opioid OPRK1 Gi/Go     95-0088E2CP2M
1 vial Opioid OPRL1 Gi/Go 93-0264E2CP0S    
1 vial Opioid OPRM1 Gi/Go 93-0213E2CP0S or
93-0213E3CP0S
   
1 vial Opioid mOPRM1 or rOPRM1 Gi/Go 93-0524E3MCP5S (mouse)
93-0494E2RCP2S (rat)
   
1 vial Opioid OPRM1 Gi/Go   93-0745E3CP5S (Total)  
1 vial Opioid OPRM1 Gi/Go     95-0107E2CP2M
DiscoveRx offers a comprehensive portfolio of cell-based functional orphan GPCR assays for deorphanization and specificity determination. This panel utilizes DiscoveRx's arrestin recruitment technology to enable identification of GPCR activation regardless of G-protein coupling and is a powerful solution for identifying novel ligand and receptor pairings.
 

Orphan Profiler™ Kit  Request a Quote

Qty Family GPCR Gene Coupling PathHunter® eXpress β-Arrestin
2 vial Class A Orphan GPR12 N/A 93-0329E2ACP1S
2 vial Class A Orphan GPR119 N/A 93-0356E1CP0S
2 vial Class A Orphan GPR18 N/A 93-0560E2ACP1S
2 vial Class A Orphan GPR3 N/A 93-0626E2CP1S
2 vial Class A Orphan GPR6 N/A 93-0634E2CP1S
 
Qty Family GPCR Gene Coupling PathHunter® eXpress β-Arrestin
1 vial Class A Orphan GPR3 N/A 93-0626E2CP1S
1 vial Class A Orphan GPR6 N/A 93-0634E2CP1S
1 vial Class A Orphan GPR12 N/A 93-0329E2ACP1S
1 vial Class A Orphan GPR18 N/A 93-0560E2ACP1S
1 vial Class A Orphan GPR39 N/A 93-0338E2CP1M
1 vial Class A Orphan GPR55 N/A 93-0245E2CP0M
1 vial Class A Orphan GPR119 N/A 93-0356E1CP0S
1 vial Class A Orphan LGR4 N/A 93-0516E2ACP1M
1 vial Class A Orphan LGR5 N/A 93-0526E2ACP1M
1 vial Class A Orphan TAAR5 N/A 93-0718E2CP1M

Neurologics

The rapid expansion of CNS drug discovery efforts are associated with an increase in neurological and psychiatric conditions in the growing geriatric population. While small molecules targeting extracellular receptors represent more than 80% of commercially available CNS-related drugs, considerable advancements have also been made in the development of antibodies, vaccines, aptamers, siRNA, and other biologics for the treatment of Alzheimers, Parkinson's, Multiple Sclerosis and other CNS disorders.

Qty Family GPCR Gene Coupling PathHunter® eXpress β-Arrestin
1 Dopamine DRD1 Gs 93-0590E2CP2S
1 Dopamine DRD2(L) Gi/Go 93-0579E2CP2S
1 Dopamine DRD2(S) Gi/Go 93-0351E2CP0S
1 Dopamine DRD3 Gi/Go 93-0591E3CP0S
1 Dopamine DRD5 Gs 93-0426E2CP0S
1 Serotonin HTR1A Gi/Go 93-0696E2CP0S
1 Serotonin HTR1B Gi/Go 93-0697E3CP6S
1 Serotonin HTR1F Gi/Go 93-0699E3CP0S
1 Serotonin HTR2A Gq 93-0401E3CP19S
1 Serotonin HTR2C Gq 93-0289E3CP3S
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Glucagons

The increased prevalence of obesity, Type II diabetes and associated complications has become an alarming global health problem. G-Protein Coupled Receptors (GPCRs) are important therapeutic drug targets for metabolic research as these receptors play a pivotal role in the regulation of insulin and glucagon secretion. Therefore, novel pharmacologic approaches are required to develop fast acting and efficacious compounds that can modulate the ways in which the body controls metabolism, weight gain and body composition.

 
Qty Family GPCR Gene Coupling PathHunter® eXpress β-Arrestin PathHunter®  eXpress Internalization cAMP HunterTM eXpress
1 Glucagon GCGR Gs 93-0241E2CP0M    
1 Glucagon GHRHR Gs     95-0076E2CP2S
1 Glucagon GIPR Gs 93-0788E2CP2M   95-0146E2CP2M
1 Glucagon GIPR Gs     95-0154E2CP2M (mouse)
1 Glucagon GLP1R Gs 93-0300E2CP0M    
1 Glucagon GLP1R Gs   93-0724E3CP0M
(Active)
 
1 Glucagon GLP1R Gs     95-0062E2CP2M
1 Glucagon GLP2R Gs 93-0425E2CP0M    
1 Glucagon GLP2R Gs     95-0112E2CP2M
1 Glucagon SCTR Gs 93-0237E2CP0M    
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