TABLE 1.
Biochemical selectivity testing of ADAMs inhibitors against a panel of zinc metalloproteinases.
| Compound | MMP1 | MMP2 | MMP8 | MMP9 | MMP14 | ADAM10 | ADAM17 |
| LT4a | 346 | 5.4 | NT | 24 | 100 | 0.04 | 1.5 |
| CID3117694b | >100 | >100 | >100 | >100 | >100 | 1.1 | >100 |
| GI254023Xa | 0.125 | 0.0021a | NT | 0.0051 | 0.088 | 0.027 | 0.86 |
| INCB8765c | >5.0 | >5.0 | NT | >5.0 | >5.0 | 0.097 | 2.05 |
| ADAM10 pro-domaind | NT | NT | NT | NT | NT | 0.048 | >10.0 |
Synthetic substrates were used for all assays. All results are IC50, μM. Bold numbers indicate the potency against the main target. NT, not tested; afrom Camodeca et al. (2016); bfrom Madoux et al. (2016); cfrom Zhou et al. (2006); dfrom Moss et al. (2007).