Table 1.
Kinase |
Compound |
||||
---|---|---|---|---|---|
3 | 4 | 5 | 6 | 7 | |
AKT1 (PKB alpha) | 0.78 | 0.02 | 2.6 | >100 | 3.6 |
AKT-2 | 0.72 | 0.02 | 1.9 | >100 | 3.3 |
IKBKB (IKKβ) | 72 | 1.1 | 4 | 15 | 34 |
RPS6K1 | 20 | 1.4 | 6 | >100 | 12 |
AMPK (A1/B1/G1) | 46 | 1.5 | 2.5 | 10 | 26 |
RAF1a | 24 | 1.6 | 6.5 | >100 | 8.5 |
MEK1a | 12.8 | 1.1 | 9 | >100 | 30 |
ERK2b | 13 | 4 | 27 | >100 | 20 |
NEK1 | 77 | 0.5 | 3.5 | 83 | 14 |
KDR (VEGFR2) | 0.77 | 0.66 | 1.3 | >100 | 6.5 |
MAPK14 (p38α) | 92 | 35 | >100 | >100 | >100 |
MAPKAPK2 | >100 | 6.7 | 9.8 | >100 | 16 |
Assays for RAF1 and MEK used the kinase cascade method diagramed in Figure 5 and discussed in the Materials and Methods section.
The IC50 values for ERK2 resulted from large experimental variability and should be regarded as only semiquantitative.