Table 4. Summary of Selectivity Testing of Novel ADAM17 Inhibitors against a Panel Zinc of Metalloproteasesa.
ID | Structure | MMP2 | MMP8 | MMP9 | MMP14 | ADAM10 | ADAM17 |
---|---|---|---|---|---|---|---|
16 | >100 | >100 | >100 | >100 | >100 | 5.7 (100) | |
17 | NT | > 100 (13) | NT | > 100 (25) | >100 | 4.2 (95) | |
18 | >100 | > 100 (28) | > 100 (13) | > 100 (27) | >100 | 5.4 (100) | |
19 | >100 | >100 | >100 | >100 | >100 | 4.3 (100) | |
20 | >100 | >100 | >100 | >100 | >100 | 11 (100) | |
21 | >100 | >100 | >100 | >100 | >100 | 8.5 (100) |
All results are IC50, μM (%inhibition at 100 μM). No parentheses indicates 0% inhibition at 100 μM. NT: not tested.