Table 1.
IC50 values of h12/15-LOX inhibitors selected for the structure-activity relationship study, errors are in parentheses when available. Experiments were conducted in the presence of 10 µM AA and 0.01% TritonX-100. Each experiment was performed in duplicate with at least four different inhibitor concentrations.
| Compound | Structure | %Inhibition (20 µM) |
IC50 (±SD) (µM) |
HT-22 Survival % (5 µM) |
|---|---|---|---|---|
| 99089 |  |
94% | 3.4 (0.5) | 20 |
| 1MLS000068545 |  |
80 | 10 (1) | 49 |
| 2MLS000856489 |  |
75 | 9.1 (2) | 18 |
| 3MLS000551826 |  |
0% | >50 | |
| 4MLS0001163892 |  |
15% | >50 | |
| 5MLS000066802 |  |
92 | 7.0 (0.4) | 76 |
| 6MLS000060847 |  |
74 | 4.0 (0.4) | |
| 7MLS000551030 |  |
75 | 10 (1) | 7 |
| 8MLS000122998 |  |
66 | 7.0 (2) | 34 |
| 9MLS002473404 |  |
59 | 20 (4) |