Table 2.
Inhibitory activity on mammalian DHODHs
| Cmpd | hDHODH | mDHODH | rDHODH | dDHODH |
|---|---|---|---|---|
| Teriflunomide* | 0.30±0.052 (6) | 0.11, 0.14 | 0.017±0.0046 (3) | 0.20, 0.27 |
| 1 | >50 (10) | 2.1±0.62 (6) | 4.4±2.7 (8) | 14 ± 6.7 (5) |
| 4 | >100 (1) | >100 (1) | >100 (1) | >100 (1) |
| 6 | >100 (1) | >100 (1) | >100 (1) | >100 (1) |
| 9 | >100 (1) | >100 (1) | >100 (1) | >100 (1) |
| 37 | >100 (2) | >100 (2) | >100 (2) | >100 (2) |
| 45 | >100 (3) | >100 (1) | >100 (1) | >100 (1) |
| 60 | >100 (3) | nd | nd | nd |
h, human; m, mouse; r, rat; d, dog. Number of independent experiments in parenthesis. nd, not determined.
*
Human DHODH inhibitor teriflunomide ((Z)-2-cyano-3-hydroxy-N-(4-(trifluoromethyl)phenyl)but-2-enamide) is an approved drug for the treatment of rheumatoid arthritis and multiple sclerosis, data similar to previous reports40.