Unique receptor dissociation kinetics of the novel endothelin receptor antagonist, macitentan

Characterizing a drug candidate for Gq coupled GPCR

This Poster summarizes a study from the Actelion Drug Discovery Department, characterizing the inhibitory potency of the drug candidate macitentan on ET_A and ET_B^4,5, two GPCRs involved in pulmonary arterial hypertension (PAH).

Features:

• Methodology followed by the authors
• Key results of the study (antagonist potency and binding kinetics)
• Conclusion suggesting the unique effectiveness of the macitentan compound