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Distinct ET_A Receptor Binding Mode of Macitentan As Determined by Site Directed Mutagenesis

Figure 7

Confirmation of characteristic IC₅₀ shifts using macitentan and bosentan analogs.

Graphical representation of the potency loss (IC₅₀ shift) of macitentan analogs (A) or bosentan analogs (B) on the three ET_A mutants L322A, R326Q, I355A compared to the wildtype receptor. Shifts were calculated from the mean IC₅₀ values generated in at least 3 independent experiments.

doi: https://doi.org/10.1371/journal.pone.0107809.g007