GPCRProfiler Services
Millipore’s GPCR screening and profiling service, GPCRProfiler, is designed to accelerate successful drug development.
| Technical Publications | |
| GPCRProfiler Services | |
| GPCRProfiler Allosteric Services: AllostericProfiler and AllostericScreener | |
| GPCR Target Panel Q4 2009 Update |
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 155 GPCRs, representing all 3 GPCR classes and over 57 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 (>155) of GPCR for cell-based functional assays
- Flexible screening and profiling and dose response studies
- 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
GPCR-specific compounds or compounds developed for non-GPCR targets may cross-react with other GPCRs
The atypical antipsychotic clozapine, a drug with known GPCR targets, or BIRB0796, developed as a p38 kinase inhibitor, both demonstrate off-target activity at a variety of GPCRs.
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Why functional assays for GPCR selectivity-profiling?
Functional assays (B), like equilibrium radioligand binding assays (A), are capable of detecting antagonists. However, functional assays are more sensitive in their ability to detect agonist as well as allosteric modulators. Data shown is for M1 acetylcholine muscarinic receptor.
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GPCRProfiler service determines both agonist and antagonist activity from a single assay well.
GPCRProfiler service uses Ca2+ flux via a 2-addition protocol to assess receptor activation/inhibition. The first addition can monitor for agonist activity (B), while the second addition can identify antagonist activity (D).
View this PDF for the full size graphic
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.Safety & Disease Panels
Whether you need to profile your lead compounds to evaluate potential side-effects or identify the therapeutic target for a biologically active molecule, GPCRProfiler Service Safety & Disease Panels can help you choose which GPCR targets will best address your research needs.Sonderangebote
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