Table 4. Extended Profiling of Compound Candidates for Potential In Vivo Study.
| compound 1 | compound 17 | compound 2 | compound 3 | |
|---|---|---|---|---|
| MMP-13 collagen Degradation assay (IC50, nM) | 9.3 | 1.2 | 77 | 140 |
| BNC degradation assay (IC50, nM) | 43 | 25 | 350 | 87 |
| Caco-2 (AB/BA) (×10–6 cm/s) | 0.6/15 | 3.5/9 | NT | NT |
| PAMPA (cm/s) | 3.3 × 10–6 | 2.9 × 10–5 | 3 × 10–7 | 7.1 × 10–5 |
| hPPB (% bound) | 91 | 93 | 98 | 99 |
| MMP (IC50, μM): 1, 2, 3, 7, 8, 9, 10, 12, 14 | 0.72, 18, >20, >20, >20, >20, >20, >20, 8.3 | >20, 20, >20, >20, 3.1, >20, >20, 10, >20 | >20, 20, >20, >20, >20, >20, >20, 20, >20 | >20, 10, >20, >20, >20, >20, >20, 10, >20 |
a
In vitro collagen degradation and cartilage degradation IC50 values are represented as nM and averaged from a minimum of two independent determinations; BNC, bovine nasal cartilage.