Table 6.
Results of kinase activity screening
| Kinase | ATP Km (μM) | Kinase activity (% control) | SD |
|---|---|---|---|
| Abl | 45 | 96 | 2 |
| ALK | 200 | 112 | 10 |
| AMPKα1 | 45 | 98 | 1 |
| ASK1 | 200 | 101 | 1 |
| Aurora-A | 15 | 92 | 0 |
| CaMKI | 200 | 100 | 4 |
| CDK1/cyclinB | 45 | 97 | 1 |
| CDK2/cyclinA | 45 | 90 | 9 |
| CDK6/cyclinD3 | 200 | 103 | 5 |
| CDK7/cyclinH/MAT1 | 90 | 91 | 0 |
| CDK9/cyclin T1 | 45 | 86 | 3 |
| CHK1 | 90 | 94 | 1 |
| CK1γ1 | 15 | 98 | 5 |
| CK2α2 | 10 | 95 | 9 |
| c-RAF | 120 | 92 | 1 |
| DRAK1 | 10 | 81 | 7 |
| eEF-2K | 15 | 86 | 4 |
| EGFR | 10 | 101 | 3 |
| EphA5 | 10 | 98 | 5 |
| EphB4 | 10 | 83 | 5 |
| Fyn | 70 | 97 | 7 |
| GSK3β | 15 | 88 | 5 |
| IGF-1R | 200 | 89 | 10 |
| IKKα | 10 | 91 | 1 |
| IRAK4 | 200 | 95 | 1 |
| JAK2 | 45 | 111 | 4 |
| KDR | 90 | 83 | 3 |
| LOK | 120 | 101 | 4 |
| Lyn | 70 | 87 | 9 |
| MAPKAP-K2 | 90 | 87 | 6 |
| MEK1 | 10 | 90 | 2 |
| MLK1 | 45 | 84 | 3 |
| Mnk2 | 120 | 90 | 11 |
| MSK2 | 45 | 89 | 1 |
| MST1 | 90 | 87 | 2 |
| mTOR | 70 | 100 | 2 |
| NEK2 | 120 | 106 | 0 |
| p70S6K | 15 | 85 | 4 |
| PAK2 | 90 | 88 | 1 |
| PDGFRβ | 200 | 99 | 1 |
| Pim-1 | 90 | 99 | 0 |
| PKA | 10 | 92 | 0 |
| PKBα | 155 | 98 | 4 |
| PKCα | 45 | 99 | 1 |
| PKCθ | 15 | 96 | 7 |
| PKG1α | 90 | 98 | 11 |
| Plk3 | 70 | 99 | 2 |
| PRAK | 15 | 79 | 4 |
| ROCK-I | 70 | 93 | 4 |
| Rse | 45 | 92 | 3 |
| Rsk1 | 45 | 95 | 5 |
| SAPK2a | 90 | 98 | 2 |
| SRPK1 | 10 | 94 | 4 |
| TAK1 | 45 | 87 | 1 |
| PI3 Kinase (p110b/p85a) | 200 | 97 | 1 |
| PI3 Kinase (p120g) | 100 | 98 | 2 |
| PI3 Kinase (p110d/p85a) | 200 | 100 | 1 |
| PI3 Kinase (p110a/p85a) | 200 | 101 | 1 |
Human kinases were evaluated at the Km for ATP and FX-9 was tested at 2.5 μM. Kinase activities are expressed as a percentage of the mean kinase activity in the positive control samples (=100%) Data interpretation of kinase activity: values <30% means a strong hit; values between 30% and 70% means a partial hit. Values >70% means no hit.