The service is the first complete functional cell-based assay platform that provides pharmacological data on hit or lead compounds as well as the screening of focused GPCR libraries.
GPCRs are a protein family of seven transmembrane surface receptors that transduce an extra cellular signal (ligand binding) into an intracellular signal (G protein activation).
Members of the GPCR protein family are involved in all types of stimulus-response pathways.
These range from intercellular communication to physiological senses. Because of the diversity of their functions, GPCRs are an ideal target class that comprise more than 40 per cent of drug screening programs and are targets for more than 50 per cent of today's commercially available pharmaceuticals.
Clients can determine if a compound is functioning as an agonist or antagonist from the first data report. GPCRProfiler screening leverages the advantages of the proprietary ChemiScreen technology, which funnels all GPCR signalling through real time calcium mobilisation.
Utilisation of a common assay platform for all targets simplifies data comparison and can be easily correlated to historical in house data.
Millipore has over 100 validated GPCR targets available for profiling and screening and is rapidly expanding its portfolio.
The GPCRProfiler also includes features such as selectivity screening for off target effects, IC50 dose response analysis and screening of focused libraries against single or multiple targets.
Despite their obvious success as targets, GPCR drug discovery has remained a relatively inefficient process, typically relying on high-throughput screening of large diverse libraries.
G-protein-coupled receptors (GPCRs) are valuable molecular targets for drug discovery. An important aspect of the early drug discovery process is the design and implementation of high-throughput GPCR functional assays that allow the cost-effective screening of large compound libraries to identify novel drug candidates.