Table I.
Average IC50 values in µmol/L for CCI activity against a panel of Ser/Thr kinases in vitro
| Gene symbol | Description | IC50(µM) |
|---|---|---|
| CDK4 | Cyclin-dependent kinase 4 | 0.0027 |
| CDK6 | Cyclin-dependent kinase 6 | 0.0063 |
| Mps1 | TTK protein kinase | 0.5 |
| PIM1 | Pim-1 oncogene | 1.6 |
| FLT3 | Fms-related tyrosine kinase 3 | 1.7 |
| CDK9 | Cyclin-dependent kinase 9 | 1.8 |
| PKR | Eukaryotic translation initiation factor 2-alpha kinase 2 | 2.1 |
| Stk33 | Serine/threonine kinase 33 | 2.1 |
| JAK3 | Janus kinase 3 | 2.5 |
| ALK | Anaplastic lymphoma receptor tyrosine kinase | 2.6 |
| mTOR | Mechanistic target of rapamycin (serine/threonine kinase) | 3.9 |
| Tyk-2 | Tyrosine kinase 2 | 6.1 |
| PI3K alpha | Phosphatidylinositol-4,5-bisphosphate 3-kinase, catalytic sub-unit alpha | 8.1 |
| CDK2 | Cyclin-dependent kinase 2 | 9.9 |
| JAK2 | Janus kinase 2 | 11.7 |
| JAK1 | Janus kinase 1 | >10 |
| TBK1 | TANK-binding kinase 1 | >10 |
| IKK (3 | Inhibitor of kappa light polypeptide gene enhancer in G cells, kinase beta | >10 |
| IKKE | Inhibitor of kappa light polypeptide gene enhancer inB-cells, kinase epsilon | >10 |
| PKA alpha | Protein kinase, cAMP-dependent, catalytic, alpha | >10 |
| IGF-1R | Insulin-like growth factor 1 receptor | >10 |
| Src | v-Src avian sarcoma (Schmidt-Ruppin A-2) viral oncogene homolog | >10 |