FUNCTIONAL ASSAY (CELL BASED ASSAYS)

Binding assays provide useful information with regard to the ability of compounds to bind to a receptor, essentially no information is provided on the efficacy of the compound, i.e. whether the compound elicits or inhibits a response at that receptor.

In a functional assay, information what we obtain is whether the compound elicits or inhibits a response at that receptor.  Thus, in a this assay functional activity is measured by adding gradually increasing amounts of the drug compound while measuring a particular function of that receptor, for instance.

·         Calcium mobilization assay is the most widely used functional assay for implementation of GPCR HTS. The assay is applicable for GPCRs whose signaling pathway induces the calcium release from its intracellular stores.