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 ETA and ETB4,5, two GPCRs involved in pulmonary arterial hypertension (PAH).


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


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Inositol-Phosphate: a new era for Gq couple GPCR signaling

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Ultimate guide to master Gq coupled GPCR assays 

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New to IP-One assays? Or already a user, but wishing to further enhance your experiments? These complete guides feature tips on performing and optimizing such assays for more significant results. Get them now!


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