Table 1: Inhibitor IC50 Values for Direct and Cascade Kinase Assays. Kinase Reactions were Conducted in the Presence of Increasing Inhibitor Concentrations for the FRET Direct, FRET Cascades, and TR-FRET Direct Assays Using 100 μM ATP
|
Inhibitor IC50 (nM) |
| Format |
Assay |
Staur. |
GW5074 |
ZM336372 |
U0126 |
PD98059 |
| FRET Direct |
ERK2 |
4,400 |
>400 |
>50,000 |
>50,000 |
>50,000 |
| FRET Double |
MEK1-ERK2 |
4 |
>400 |
>50,000 |
>10,000 |
>50,000 |
| FRET Triple |
BRAF-MEK1-ERK2 |
56 |
3 |
400 |
65 |
420 |
| FRET Triple |
BRAF V599E-MEK1-ERK2 |
69 |
2 |
32 |
65 |
300 |
| FRET Triple |
CRAF-MEK1-ERK2 |
63 |
9 |
30 |
66 |
380 |
| TR-FRET Direct |
BRAF |
>50,000 |
15 |
580 |
>40,000 |
>50,000 |
| TR-FRET Direct |
BRAF V599E |
>50,000 |
4.9 |
270 |
≥5,000 |
>50,000 |
| TR-FRET Direct |
CRAF |
>50,000 |
24 |
90 |
>50,000 |
>50,000 |