Literature values of substrate and inhibitor affinities for different PDE families
| PDE family | KmcGMP | Ki Sildenafil | KiZaprinast | Ki Rolipram | KiMilrinone |
|---|---|---|---|---|---|
| μM | |||||
| PDE 1 | 1.2–2.72-a | 0.2812-b | 6.652-b | >10002-c | 482-d |
| PDE 2 | 112-c | >302-b | >1002-b | 1802-d | |
| PDE 3 | 0.02–102-d | 16.22-b | >1002-b | 0.26–2.22-d | |
| PDE 4 | 3102-c | 7.682-b | 77.42-b | 0.062-k–1.07l | 112-d |
| PDE 5 | 0.32-c–5.62-b | 0.00352-b–0.0072-e | 0.132-f–0.8562-b | ∼1472-c | |
| PDE 9 | 0.072-g–0.172-h | 72-g | 292-g | >2002-g | |
| PDE 10 | 2.92-i–7.22-j | >12-i–2.12-j | 7.12-i–10.82-j | 47.32-i | >50.72-j |
Values represent the substrate K m and inhibitorK i for different PDE families; ranges signify lowest to highest values found.
↵2-a Schudt et al., 1996;
↵2-b Ballard et al., 1998;
↵2-c Beavo, 1988;
↵2-d Beavo and Houslay, 1990;
↵2-e Moreland et al., 1998;
↵2-f Turko et al., 1999;
↵2-g Soderling et al., 1998;
↵2-h Fisher et al., 1998;
↵2-i Soderling et al., 1999;
↵2-j Fujishige et al., 1999;
↵2-k Muller et al., 1996;l Shakur et al., 1995.