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. 2023 Sep 25;9(3):e12412. doi: 10.1002/trc2.12412

TABLE 1.

Potency of well‐known PDE5 inhibitors. Potencies stated are IC50 values unless otherwise stated.

Drug name Potency: PDE5i Potency: other actions References
Sildenafil 1–9 nM PDE6: 10–40 nM 8 , 25 , 26 , 27 , 28
KD 3.1 nM
Tadalafil 1–7 nM

PDE6: Ki 700 Nm

PDE11: 10—300 nM

8 , 25 , 26 , 27 , 29 , 30
KD 1.7 nM
Ki 1.9 nM
Vardenafil 0.1‐1.0 nM PDE1: 300 nM 8 , 25 , 26 , 29
KD 0.32 nM PDE6: Ki 0.3‐11 nM
Ki 2.3 nM PDE9: 680 nM
PDE11: 240 nM
Udenafil 6–8 nM PDE 1: 870 nM 31
PDE 6: 50 nM
Dipyridamole 900–2000 nM PDE6: 380–1000 nM 27 , 28 , 30
PDE7: 1–2 μM
PDE10: 1 μM
PDE11: 800 nM
Zaprinast 50 nM–2.5 μM a PDE6: 150 nM 27 , 28
a

Wide species and tissue dependence of zaprinast potency as a PDE5i.

Abbreviation: PDE, phosphodiesterase; PDE5i, phosphodiesterase‐5 inhibitor.