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. Author manuscript; available in PMC: 2014 May 9.
Published in final edited form as: J Med Chem. 2013 Apr 23;56(9):3456–3466. doi: 10.1021/jm4002692

Table 1.

Calculated IC50 values from graphs in Figure 3 (μM)a.

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
a

Assays for RAF1 and MEK used the kinase cascade method diagramed in Figure 5 and discussed in the Materials and Methods section.

b

The IC50 values for ERK2 resulted from large experimental variability and should be regarded as only semiquantitative.