Table 4. IC50 values of selected compounds in the NHLF myofibroblast reversal assay.
| Compound name | Nuclear count IC50 [nM] |
Impedance IC50 [nM]1 |
MS / MS α–SMA IC50 [nM] |
MS / MS COL1 IC50 [nM] |
HCA IC50 [nM] |
|---|---|---|---|---|---|
| EW–7197 | >25,000 (n = 1) | >10,000 (n = 2) | 73 ± 31 (n = 2) | 82 ± 30 (n = 2) | 18,000 (n = 1) |
| Nintedanib | 16,000 (n = 1) | >10,000 (n = 1) | >10,000 (n = 1) | 626 (n = 1) | 6,900 (n = 1) |
| Halofuginone | 1,400 (n = 1) | >1000 (n = 2) | 102 ± 87 (n = 2) | 116 ± 81 (n = 2) | 120 (n = 1) |
| GSK–269962 | n.a. | >10,000 (n = 1) | 35 (n = 1) | 537 (n = 1) | n.a. |
| Alprostadil | >25,000 (n = 1) | 0.9 ± 0.2 (n = 2) | 1 ± 0.0 (n = 2) | 1.5 ± 0.7 (n = 2) | 280 (n = 1) |
| PGE2 | >25,000 (n = 1) | 0.7 (n = 1) | 0.8 (n = 1) | 0.4 (n = 1) | 145 (n = 1) |
| ONO–18c | >25,000 (n = 1) | 0.1 ± 0.02 (n = 2) | 0.14 ± 0.09 (n = 2) | 0.2 ± 0.14 (n = 2) | 20 (n = 1) |
| ONO–18k | >25,000 (n = 1) | 2 (n = 1) | 3 (n = 1) | 2 (n = 1) | 5,500 (n = 1) |
| Evatanepag | >25,000 (n = 1) | 14 (n = 1) | 16 (n = 1) | 24 (n = 1) | 2,300 (n = 1) |
| Digoxigenin | 2,700 (n = 1) | 140 (n = 1) | 48 (n = 1) | 54 (n = 1) | 76 (n = 1) |
n.a.: not assessed. Mean ± SD of n independent experiments are shown.
1Impedance data were extracted at t = 20 h post TGF–β1 addition.