The solute carrier proteins (SLCs) comprise a superfamily of transporters controlling the import and export of

G protein-coupled receptors (GPCRs) represent, to date, the most successful drug targets, due to their substantial involvement in human pathophysiology and their pharmacological tractability.
GPCRs can be considered a primary target for drug discovery, where over 30% of FDA approved drugs target GPCRs, as well as key players regarding taste and olfactory sensation. Despite a very successful drug discovery history so far, very important new aspects about GPCR biology are still emerging and paving completely new avenues for finding highly innovative drugs acting on GPCRs.
Experimental high-throughput screening (HTS) approaches of clinically relevant GPCRs are a first-line drug discovery approach in biomedical research. For the identification of valid hits in an HTS campaign the assay employed plays a fundamental role. Based on many different parameters, such as correct receptor pharmacology, GPCR coupling, the screening goal (identification of agonists, antagonists, inverse agonists, or allosteric modulators), the most appropriate assay protocol and readout system needs to be selected and developed.
Having developed more than 100 different GPCR assays for HTS campaigns, in this webinar, we will share our experience and “lessons learned” and illustrate of some of the different technologies and tools applied case by case, including the use of cAMP and Ca2+ biosensors, fast and glow luminescence, fluorescent dyes, G protein coupling shift, HTRF-based detection. Critical points and future directions will also be addressed.

SLCs, assay development, HTS, functional assays, optogenetics, genetically encoded sensors, radiometric, FLIPR, GPCRs, 7TM structure, receptor activation, assay development, HTS, functional cell-based assays, inverse agonist, allosteric modulators, constitutive activity, desensitization, genetically encoded Ca2+ and cAMP sensors, G alpha protein coupling, FLIPR, Hamamatsu FDSS