Functional studies of G-protein coupled receptors (GPCR) are complementary to affinity-based radioligand assays. They provide valuable information about the way a drug interacts with a GPCR receptor. For example, you can determine if a drug is an agonist or an antagonist or what its potency and efficacy are for a given GPCR target. Understanding drug functionality is also an important benefit of functional studies and you can, for example, identify allosteric modulators that are generally difficult to identify using orthosteric ligand-based binding assays.
PerkinElmer's Contract Research Services' GPCRFunctional platform is a comprehensive suite of functional GPCR services for custom assay development, screening, and profiling across a variety of GPCR targets and specific drug activity studies. GPCRFunctional is based on PerkinElmer sourced recombinant cell lines and on optimized second messenger assay protocols developed by PerkinElmer's Contract Research Services. ValiScreen® cell lines express human forms of GPCR targets and preserve the natural coupling of each GPCR target. AequoScreen® cell lines couple human forms of GPCR targets with a calcium response pathway emitting a rapidly decaying flash luminescence.
PerkinElmer's Contract Research Services Molecular and Cell biology groups can assist you with any GPCR target assay development. Whether your project requires the complete creation and validation of a recombinant GPCR expressing cell line model or the optimization of assay conditions for an existing target, we will work closely with you to define the best development strategy (choice of cellular host model, GPCR assay readout)
Our capabilities include:
- Gene cloning
- Clone selection and amplification
- Cell line characterization
- Optimization of assay method(s)
- Assay validation
Our fast growing panel of over 50 functional GPCR assays helps you developing a better understanding of your drug:
- Uncover possible GPCR-mediated toxicity
- Determine your drug selectivity for a given receptor
- Identify potential new agonist or antagonist activities for your drug
- Characterize allosteric GPCR modulation
Review a complete list of PerkinElmer's Contract Research Services' GPCR functional assays.
View a chart of GPCR binding assays and their corresponding functional assays.
- Determine agonist or antagonist compound potency in any assay on the GPCRFunctional™ panel: 10-point or custom duplicate IC50/EC50 curves Choice of dose range
- Quality control: reference compound IC50/EC50 determination with historical data comparison Quick turnaround time of about 2 weeks!
Screen your library of compounds in virtually any assay on the GPCRFunctional™ panel. All screening projects are highly customized to meet our clients' needs of throughput, process & workflow as well as data reporting format.
Please contact us by e-mail: email@example.com to discuss your screening projects.
GPCRFunctional™ Label Free
Label free cell based assays provide an especially attractive representation of GPCR drug pharmacology in a more biologically-relevant context.