GPCRProfiler™ Screening Service Expedites Lead Optimization

Millipore Corporation today announced the availability of GPCRProfiler screening, an innovative service for selectivity screening, characterization of lead compounds, and screening of focused GPCR libraries.

GPCRProfiler screening more accurately characterizes lead compounds than traditional binding methods by providing comprehensive functional data that enables pharmaceutical and biotechnology companies to accelerate their lead optimization efforts.

The GPCRProfiler package includes:

• Selectivity Screening for off target effects
• IC50 Dose Response Analysis
• Screening of focused libraries against single or multiple targets.

The GPCRProfiler service is the first complete functional cell-based assay platform that provides pharmacological data on hit or lead compounds. 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 signaling through real time calcium mobilization. Utilization 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.

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% of drug screening programs and are targets for more than 50% of today’s commercially available pharmaceuticals.