Affinities of crisaborole, compd2, compd3, compd4, apremilast, and roflumilast for other PDE isozymes
| PDE Isozyme | IC50 Value | |||||
|---|---|---|---|---|---|---|
| Crisaborole | Compd2 | Compd3 | Compd4 | Apremilastc | Roflumilastc | |
| nM | ||||||
| PDE1A1 | a | 260 | 1500 | 6400 | ||
| PDE1B | 3700 | 90 | 800 | 5500 | ||
| PDE1C | b | 81 | 520 | 5700 | ||
| PDE2A1 | 6700 | 400 | 970 | 580 | ||
| PDE3A | 5100 | 130 | 1200 | 1400 | ||
| PDE3B | 4500 | 310 | 1700 | 1400 | ||
| PDE5A1 | c | 1700 | 1100 | 3100 | ||
| PDE6C | 6700 | 5000 | 7500 | 2700 | ||
| PDE7A1 | c | 24 | 260 | 470 | ||
| PDE7B | 9400 | 330 | 650 | 710 | ||
| PDE8A1 | c | 140 | 910 | 1500 | ||
| PDE9A2 | c | c | c | c | ||
| PDE10A1 | c | 450 | 580 | 1800 | ||
| PDE10A2 | c | 380 | 480 | 1600 | ||
| PDE11A4 | c | 2700 | 2400 | 3200 | ||
A fluorescent polarization assay was performed using full-length human PDE enzymes and 0.1 μM FAM-cAMP or FAM-cGMP as a substrate. FAM, 5-(and-6)-carboxyfluorescein.
↵a 54% inhibition at 10 μM.
↵b 80% inhibition at 10 μM.
↵c Less than 50% inhibition at 10 μM. For apremilast and roflumilast, inhibition was < 50% at 10 μM for all PDE isozymes.