Table 3. IC50 values of selected compounds in the standard 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) | 47 ± 25 (n = 7) | 51 ± 17 (n = 7) | 110 ± 30 (n = 7) | 82 ± 30 (n = 7) |
Nintedanib | 1,400 (n = 1) | 300 ± 110 (n = 2) | 500± 120 (n = 2) | 1,600 ± 1,300 (n = 3) | 760 ± 130 (n = 3) |
Halofuginone | >46,000 (n = 1) | 96 ± 11 (= 2) | 27 ± 4 (n = 2) | 27 ± 1 (n = 2) | 690 ± 320 (n = 2) |
GSK–269962 | >50,000 (n = 1) | 1,010 ± 300 (n = 3) | 22 ± 1 (n = 2) | 3,100 ± 92 (n = 2) | 240 ± 270 (n = 2) |
Alprostadil | >50,000 (n = 2) | 0.6 ± 0.1 (n = 3) | 1.9 ± 1.6 (n = 3) | 5.0 ± 1.4 (n = 3) | 8.6 ± 10 (n = 2) |
PGE2 | >2,500 (n = 1) | 0.5 ± 0.1 (n = 2) | 1.2 ± 1.2 (n = 2) | 4.9 ± 4.4 (n = 2) | n.a. |
ONO–18c | >50,000 (n = 1) | 0.04 ± 0.01 (n = 3) | 0.05 ± 0.01 (n = 2) | 0.9 ± 0.5 (n = 3) | < 2.5 (n = 2) |
ONO–18k | >50,000 (n = 2) | 1.3 ± 1.1 (n = 4) | 2.6 ± 2.9 (n = 3) | 7.6 ± 5.7 (n = 4) | 110 ± 150 (n = 2) |
Evatanepag | >50,000 (n = 2) | 6.7 ± 3 (n = 3) | 26 ± 29 (n = 2) | 11 (n = 1) | 82 ± 110 (n = 2) |
Merck–19a | n.a. | 10.4 ± 1.1 (n = 2) | 108 ± 87 (n = 2) | 17.7 ± 7.0 (n = 2) | n.a. |
Digoxigenin | 19,000 (n = 1) | 250 ± 140 (n = 2) | 38 ± 6 (n = 2) | 85 ± 8 (n = 2) | 220 (n = 1) |
n.a.: not assessed. Values represent mean ± SD of n independent experiments.
1 Impedance data were extracted at t = 20 h post TGF–β1 addition.