Fig 1: In vitro potency of sartans at blocking AT1R-induced G protein or βarr activation.(A) Dose-response curves for inhibition of AngII-induced AT1R-βarr binding or for inhibition of AngII-induced AT1R-G protein coupling (early response, ER) for each compound, as derived from the CellKey assay. (B) Dose-response curves of each drug for βarr activation at the AngII-bound AT1R, based on the DiscoveRx PathHunterTM β-Arrestin assay system. (C) AngII-induced G protein inhibition potencies based on the FLIPR calcium assay (Molecular Devices). Los: Losartan; Exp: EXP3174; Tel: Telmisartan; Epr: Eprosartan; Azi: Azilsartan; Olm: Olmesartan; Can: Candesartan; Val: Valsartan; Irb: Irbesartan.
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