With the apparition of concepts such as allosteric modulation and functional selectivity the
field of G-protein coupled receptors drug discovery has regained its momentum. To better address this
paradigm shift new screening technologies were developed. To identify novel GPCR ligands the
screening method of choice was based upon functional assay for the last decade and is now being complemented
by several innovative binding technologies. An overview of these assays, as well as an
example of a fully integrated platform aiming at identifying novel allosteric modulator with the appropriate
profile are presented in this review.
Keywords: Allosteric ligand, Binding technology, G-protein-coupled receptors, Resonance Energy Transfer.
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