The Target Residence Time of Antihistamines Determines Their Antagonism of the G Protein-Coupled Histamine H1 Receptor

The pharmacodynamics of drug-candidates is often optimized by metrics that describe target binding (Kd or Ki value) or target modulation (IC50). However, these metrics are determined at equilibrium conditions, and consequently information regarding the onset and offset of target engagement and modul...

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Autors principals:	Reggie Bosma, Gesa Witt, Lea A. I. Vaas, Ivana Josimovic, Philip Gribbon, Henry F. Vischer, Sheraz Gul, Rob Leurs
Format:	Artigo
Idioma:	Inglês
Publicat:	Frontiers Media S.A. 2017-09-01
Col·lecció:	Frontiers in Pharmacology
Matèries:	residence time recovery time GPCR histamine H1 receptor calcium mobilization DMR
Accés en línia:	http://journal.frontiersin.org/article/10.3389/fphar.2017.00667/full
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