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GPCRProfiler Services

Millipore’s GPCR screening and profiling service, GPCRProfiler, is designed to accelerate successful drug development.

Technical Publications
 
Detection of Allosteric Potentiators for GPCRs with Millipore’s GPCRProfiler Platform
 
Validation of Millipore’s GPCRProfiler Panel for Selectivity Profiling and Detection of
Off-Target Activity
 

Why Profile?

  • Many of the ~385 “druggable” GPCRs (excluding taste and odorant receptors) share a similar small molecule binding pocket
  • Implications of cross-reactivity:
    - Benefits - many efficacious atypical anti-psychotics are promiscuous drugs
    - Cons - non-specificity of compounds has led to dangerous side-effects and financial liability
  • Maximize drug development success by accessing specificity of lead compounds and metabolites early in development
  • Insight into why a compound failed in clinical trials
  • Jump start new drug discovery campaigns by screening novel chemical scaffolds against a large panel of GPCRs

About GPCRProfiler

The current pace of drug discovery often demands that in-house drug discovery efforts be supplemented. GPCRProfiler can either bolster current screening capacity or jump-starting drug discovery efforts on new targets or therapeutic areas. Beyond lead identification, it is obvious that the successful progression of a lead compound to clinical drug is to have a solid knowledge base surrounding the compound.

Our GPCRProfiler is the first complete cell-based functional platform utilizing a common validated readout for over 130 GPCRs, representing all 3 GPCR classes and over 55 ligand families. The foundation of GPCRProfiler is our proprietary ChemiScreen Stable Calcium Optimized GPCR Cell Lines used for real-time calcium mobilization assays to rapidly, reliably and reproducibly screen and profile compounds. Using one platform allows ligands to be screened with identical buffer conditions and incubation times for the entire spectrum of GPCRs, regardless of native G protein coupling, for easy analysis and comparison.

Benefits of GPCRProfiler Service
    • Universal GPCR readout using Millipore’s ChemiScreen Stable Calcium Optimized GPCR Cell Lines
    • Simple data comparison for profiling studies
    • Largest collection (>130) of GPCR for cell-based functional assays
    • Flexible screening and profiling
    • Testing of one or more drugs at one or more receptors
    • Several user-defined assay parameters
    • Identify hits as full or partial agonists, antagonists or allosteric modulators
    • Reader-friendly reports with data summary and recommendations
    • Consult with knowledgeable scientists to help setup appropriate assay conditions or interpret data

Example of Calcium Flux Response



Single well analysis for agonist (top) and antagonist (bottom) funation at α1A expressed in Chem-1 cells.


Example of GPCRProfiler Screening



Sample traces and positive and negative controls for compound screening against α1A expressed in Chem-1 cells in agonist (upper panel) and antagonist (lower panel) mode.

Example of GPCRProfiler Dose Response







Calcium flux traces for agonist (upper panel) and antagonist (middle panel) dose response and corresponding graphs of data (lower panel) for TP expressed in Chem-1 cells.


Under the Hood of the New St. Charles GPCRProfiler Lab
  • 96 and 384 -well capabilities
  • Integrated Automation
  • FLIPRTETRA Fluorescent Plate Reader
  • Biomek FX automated liquid handling
  • Sample Bar Coding
Receptor List

For a complete list of the targets available through the GPCRProfiler Services, click here


Specials & Promotions

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