Table 4 Biochemical selectivity profile of the most potent derivatives
From: Structure-based design of potent and selective inhibitors of the HECT ligase NEDD4
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|---|---|---|---|---|---|
Compound | 15 | 25 | 30 | 31 | 32 |
IC50 NEDD4 (µM) | 0.69 ± 0.18 | 0.34 ± 0.04 | 0.16 ± 0.06 | 0.33 ± 0.03 | 0.12 ± 0.03 |
NEDD4 11 µM | 83.90 ± 3.6 | 89.6 ± 0.38 | 90.7 ± 0.86 | 87.9 ± 3.56 | 92.3 ± 2.22 |
ITCH 11 µM | 0 | 30.7 ± 0.80 | 13.5 ± 1.70 | 0 | 16.6 ± 1.64 |
NEDD4L 11 µM | 14.40 ± 1.1 | 22.0 ± 1.27 | 16.5 ± 8.32 | 3.3 ± 0.72 | 4.1 ± 1.61 |
HECW2 11 µM | 5.50 ± 0.4 | 6.6 ± 0.98 | 14.8 ± 7.20 | 5.3 ± 0.93 | 3.5 ± 0.99 |
NET 0.1 µM | 5.30 ± 4.5 | 70.8 ± 1.7 | 4.0 ± 2.8 | 2.8 ± 2.2 | 0.2a |
5HT 0.1 µM | 81.66 ± 1.4 | 92.5 ± 0.6 | 7.9 ± 5.6 | 4.4 ± 2.8 | 6.7 ± 1.9 |
