GPCRs have produced more drugs than any other class of receptors: 26 of the top 100 pharmaceutical products are compounds that target GPCRs, accounting for sales of over $ 30 billion.

Also for Actelion, the GPCRs ET_A and ET_B, the endothelin receptors A and B, respectively, have proven to be optimal for drug discovery, allowing the discovery of Tracleer®, Veletri™ and Clazosentan. This success is due to the ideal localization of GPCRs on the cell surface, making them particularly accessible to therapeutic molecules, and to their specific involvement in most pathophysiological situations. The recent completion of the human genome project, combined with the efforts of the whole scientific community, has significantly increased our understanding of the large GPCR family. New GPCRs have now been identified that will be at the origin of the medicines of tomorrow: this represents a formidable potential.