Products & Applications / Assay Ready Kits / Assay Ready Kit Format Selection Guide

Assay Ready Kit Format Selection Guide

Ready-to-use eXpress™, Profiler™, eXplorer™ and Ab Hunter™ Kits

DiscoveRx offers a comprehensive menu of ready-to-use, functional cell-based assays for GPCRs, Kinases, NHRs and novel signaling pathways. These kits contain validated cells, detection reagents, cell plating reagents and plates and do not require expensive instrumentation to run. Eliminate lengthy, expensive and time consuming cell culture. Simply thaw, plate and run the assay!

Ready-to-use complete kits for:

  • Compound profiling 
  • Selectivity and specificity panels
  • Functional antibody screening
  • Biomarker detection in blood or plasma
  • Compound dosing prior to animal studies

Select one of the tabs below to learn more about these different assay ready formats

  PathHunter® and cAMP Hunter™ eXpress kits provide a fast and simple method for detection of receptor activation, receptor internalization and other novel cell signaling events. All assay-ready eXpress kits are formatted for 96-well plate analysis and are available in 3 convenient sizes: 100 dp (1 plate), 200 dp (2 plates), and 1,000 dp (10 plates).

View List of Assay Ready eXpress Kits »

Features & Advantages

  • Choose from over 400 assays - GPCRs, Kinases, NHRs and signaling pathways
  • Functionally validated frozen cells and reagents
  • Single assay format - detect agonists, antagonists, allosteric modulators
  • Optimized step-by-step protocol
  • Chemiluminescent detection for fast and reliable results
  • Utility for both small molecule and biologics screening
  • Compatible with any standard bench top luminometer
 How PathHunter Works

Robust and Reliable Assay-Ready Format

SSTR2

Measurement of β-Arrestin recruitment by the Somatostatin 2 (SSTR2) receptor in response to increasing concentrations of Somatostatin-28 (SST-28) using frozen, assay ready eXpress cells and live PathHunter cell lines. PathHunter eXpress cells have EC50 values equivalent to dividing cells.

Highly Reproducible

I
Individual vials of PathHunter eXpress  GIPR cells were thawed and plated into 96-well dishes on 3 separate days and assay performance was compared. Similar signal to background (S:B) and EC50 values were obtained demonstrating  that the assay ready eXpress format results in robust, reliable and reproducible results  every time.

Adaptable to 96- and 384-well Formats


U2OS PathHunter® eXpress cells expressing the Bradykinin BDKRB1 receptor were plated at 10,000 cells/well in a 96-well plate (left panel) or 2,000 cell/well in a 384-well plate (right panel) and stimulated with a control agonist Lys-des-Arg9 Bradykinin for 90 minutes. Signal was detected using PathHunter® Detection Reagents according to the protocol. Similar pharmacology and signal-to-background was obtained in both formats [click to enlarge].

The PathHunter® eXpress GPCR Profiler Kit allows you to mix-and-match up to 10 different GPCR targets. Select from over 350 targets available in β-Arrestin recruitment, cAMP accumulation, or GPCR internalization readouts. Build a unique panel of assays to compare human and ortholog pharmacology or jump start your deoprhanization campaign by testing your compounds with a unique combination of Orphan GPCR receptors. Profiler kits contain everything needed to perform functional assays on 10 unique targets including frozen pre-validated cells, detection reagents, cell plating reagents and assay plates. Perform compound selectivity profiling on your bench top with our simple and easy to use Profiler kit.

View Sample List of Profiler™ Kits »

Features & Advantages

  • Flexible - mix and match over 350 GPCR assays 
  • Multiple readouts - Arrestin recruitment, cAMP accumulation and receptor internalization
  • Convenient - benchtop profiling of lead compounds
  • Customizable - create unique selectivity panels or study off-target effects
  • Compound dosing - compare pharmacology between human and ortholog targets
  • Novel tool for receptor de-oprhanization
     
 How PathHunter Works

Assay Performance

 

Chemokine Receptor Family Profiling
  chemokine agonists
 
A series of known chemokine agonists were tested against select multiple chemokine targets. CCR6, CXCR1, CCR2, and CCR5 maintain agonist selectivity demonstrating that these assays are
uniquely suited for in house profiling and/or target prioritization [click to enlarge].
The PathHunter® GPCR Explorer Kit is a simple and easy-to-use method for building on-demand functional GPCR assays in just 3 simple steps – Clone. Transfect. Read. Whether you have a panel of mutant GPCR cDNAs or a favorite GPCR heterodimer you’d like to functionally test, the simple, optimized transfection protocol combined with PathHunter® EFC-based chemiluminescent detection makes it the ideal platform for exploring novel GPCR receptor biology.

Features & Advantages

  • Based on G-protein independent β-Arrestin read-out
  • Contains highly transfectable, ready-to-assay CHO-K1 cells
  • Choice of vectors optimized for maximal expression in mammalian cells
  • Ideal for GPCR heterodimerization, siRNA knockdown, or mutant receptor studies
  • Chemiluminescent detection used with any standard luminometer
 How PathHunter Works  

Assay Performance

 

Create Customized GPCR Biosensor Lines
  Creation of GPCR Biosensor Cell LinesTRKA, TRKB and TRKC inhibition data using Staurosporine           
 
CHO-K1 GPCR eXplorer cells were plated at 10,000 cells per well and incubated overnight at 37°C. The following day, cells were transfected with 2 µg of pEGFP vector and 48 hr post-transfection, greater than 60% of the GPCR Explorer cells were transfected ([Left panel) [click to enlarge]. In a separate experiment, eXplorer cells were transiently transfected with 2 µg of the pCMV-SSTR2-PK vector (+ SSTR2 DNA) or an empty vector (- SSTR2 DNA). Twenty-four hours later, cells were treated with increasing concentrations of Somatostatin 28, a control agonist. Activation of the SSTR2 receptor stimulates binding of Arrestin resulting in an increase in β-gal enzyme activity that can be measured using chemiluminescent PathHunter Detection Reagents  (Right panel) [click to enlarge].
 
   
  Monoclonal antibodies (MAbs) and their derivatives are currently the fastest growing class of biotherapeutic molecules.  Although many technologies exist for generating and panning large collections of antibody fragments, assays that can reliably detect both the binding and functional activity of a biotherapeutic in a fast, reproducible and cost effective manner are required.

DiscoveRx now offers >240 target-specific Ab Hunter™ Cell-Based Assays in a ready-to-use format to monitor specific, high affinity binding and functional activity of your therapeutic antibodies against G-Protein Coupled Receptors (GPCRs) and Receptor Tyrosine Kinases (RTKs). Expedite your discovery and characterization of potent, selective and high affinity biotherapeutics with these novel cell-based assays.
 

View List of Ab Hunter™ GPCR Binding Kits »
View List of Ab Hunter™ Kinase Binding Kits »
View List of Ab Hunter GPCR Bioassay Kits »
View List of Ab Hunter Kinase Bioassay Kits »

Ab Hunter™ Features & Advantages

  • >240 target-specific GPCR and Kinase assays
  • Full length, native receptors enable flexibility in antibody design
  • Screen for biologically relevant antibodies to any extracellular domain of the target receptor
  • Obtain selectivity, specificity and efficacy of your candidate molecules
  • Understand mechanism of action: Identify blocking, neutralizing or activating antibodies
  • Reliable & reproducible assessment of antibody/large molecule preparations in a 96-well format
  • Results in less than 3 hours

Ab Hunter™ Antibody Binding Kits

A Robust Tool for Antibody Screening
With Ab Hunter™ Binding Kits You Can:

  • Access ready-to-go assays for  > 240 extracellular receptors
  • Screen for antibody candidates specific to GPCRs and Kinases
  • Use full length receptors




G protein coupled receptors (GPCRs) and Kinases remain the most important druggable  classes of targets for small molecule drug discovery. However, many current GPCRs and Kinases are intractable to small molecule drug discovery and elicit greater potential with large molecule therapeutics.  A growing interest in developing therapeutic monoclonal antibodies  that target extracellular epitopes of cell surface proteins requires validated, highly specific and sensitive reagents.

DiscoveRx’s NEW Ab Hunter™ Antibody Binding Kits are designed to detect specific, high affinity antibodies against GPCRs and Kinases. These kits allow you to screen antibodies against full length cell surface receptors expressed on whole cells with simple, scalable, ready-to-assay kit formats. The amount of membrane bound antibody can be quantified using fluorescently labeled secondary antibody by flow cytometry.

View List of Ab Hunter™ GPCR Binding Kits >
View List of Ab Hunter™ Kinase Binding Kits >

Product Features

  • Large menu of target-specific GPCR and Kinase assays
  • Full length, native receptors enable flexibility of antibody design
  • Screen antibodies to any extracellular domain of the target receptor
  • Compatible with complex biological samples, including human serum and plasma
  • Simple - just thaw, incubate, wash, read - obtain results in less than 3 hours

 		 How PathHunter Works
   

 Assay Performance

Representative Data for Ab Hunter™ CXCR3 Antibody Binding Assay

- CXCR3 Antibody		  
+ CXCR3-PE labeled Antibody
Cells expressing CXCR3 receptor were incubated in the presence or absence of PE-labeled primary antibodies and analyzed by flow cytometry. A right shift in fluorescence is observed for a cell population incubated with anti-CXCR3-PE Antibody (right panel) demonstrating the suitability of the platform to screen for antibodies that bind specifically to CXCR3 receptor. [click to enlarge].
  

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Ab Hunter™ Bioassay Kits

A Fast and Reliable Tool for Antibody Screening and Functional Characterization
With Ab Hunter™ Bioassay Kits You Can:
  • Obtain selectivity and specificity information
  • Detect, quantify and confirm efficacy in a functional cell-based assay
  • Differentiate anti-ligand or anti-receptor neutralizing antibodies
  • Understand the mechanism of action of your biomolecules
  • Profile libraries of antibody candidates







To aid innovative discoveries of targeted antibody therapeutics, DiscoveRx now offers NEW Functional Ab Hunter™ Bioassay kits! These bioassays are cell-based, functional, complete out-of-the box solution that offer the convenience of your antibody screening and characterization. The kits include pre-validated engineered cells, control ligands and reagents to ensure consistent, robust and reliable results every time you run the assay. Unlike traditional ELISAs, these kits allow you to detect, quantify and characterize functional antibodies. Now you can determine efficacy and specificity of your therapeutics with these fast, easy and robust assays.

View List of Ab Hunter GPCR Bioassay Kits >
View List of Ab Hunter Kinase Bioassay Kits >


Product Features
  • Broad menu of target-specific GPCR and Kinase functional bioassays
  • Assay format ideal for detecting functional antibodies
  • Compatible with serum, cell lysates and supernatants
  • Easy, one-step, mix-and-read protocol
  • Quantitative chemiluminescent detection
  • Read on any standard benchtop luminometer
 How PathHunter Works

Functional Assay Performance

Detect anti-GPCR Antibodies

  
 

Differentiate anti-RTK Antibodies
ErbB1 receptor and dose dependent inhibition  
CHO-K1 cells expressing CCR5 receptor were run in antagonist mode by incubating with increasing concentrations of a commercially available anti CCR5 mAb (Left panel).  U2OS cells expressing EGFR were run in antagonist mode with varying concentrations of three known antibodies. Both assays demonstrate the suitability of the platform in obtaining specificity, efficacy and characterization of functional antibodies (Right panel).
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