Table 1.
Inhibition results for thiophene carboxamide series against JNK-1.
| Compd. | Kinase activity assay IC50a(μM) | Compd. | Kinase activity assay IC50a(μM) | Compd. | Kinase activity assay IC50a(μM) |
|---|---|---|---|---|---|
| 1 | 26.0 | 24 | >25 | 50 | >25 |
| 3 | >100 | 25 | 1.3 | 51 | 1.9 |
| 5a | >100 | 26 | 1.4 | 52 | 8.2 |
| 5b | >100 | 27 | 2.6 | 53 | 10.2 |
| 5c | >100 | 28 | 18.7 | 54 | 9.7 |
| 5d | >25 | 29 | 8.3 | 55 | 7.4 |
| 5e | >25 | 30 | 9.4 | 56 | 5.8 |
| 5f | >100 | 31 | 5.1 | 57 | 12.5 |
| 5g | 5.4 | 32 | 2.9 | 58 | >25 |
| 7 | 3.6 | 33 | 1.8 | 59 | 3.1 |
| 8 | 5.9 | 34 | >25 | 60 | >50 |
| 9 | >100 | 35 | 3.4 | 61 | 8.1 |
| 10 | >100 | 36 | 1.8 | 62 | >50 |
| 11 | >25 | 37 | 11.9 | 63 | 9.4 |
| 12 | >25 | 38 | 2.6 | 64 | >50 |
| 13 | >25 | 39 | 5.7 | 65 | 65.3 |
| 14 | 3.2 | 40 | 6.0 | 66 | 7.6 |
| 15 | 2.7 | 41 | 5.4 | 67 | 83.5 |
| 16 | >50 | 42 | 4.3 | 68 | 75.1 |
| 17 | >25 | 43 | >25 | 69 | 3.6 |
| 18 | 2.7 | 44 | 2.9 | 70 | 2.5 |
| 19 | 1.8 | 45 | 7.6 | 71 | 4.9 |
| 20 | >25 | 46 | 6.4 | 72 | 2.5 |
| 21 | >25 | 47 | 5.8 | 73 | 1.9 |
| 22 | 2.30 | 48 | 20.9 | 74 | 2.5 |
| 23 | >25 | 49 | 3.4 |
a
Values are means of at least three or more experiments. Standard deviation generally within ±25%