TABLE 1

Activity of PS200981 and PS166276 at a panel of kinases A panel of kinases was evaluated for activity of PS200981 and PS166276 at ≤ Km [ATP]. IC50 values are in micromolars.


Kinase

PS200981

PS166276

Kinase

PS200981

PS166276
μM
p38α 1.0 0.028 IGF-1R >50 >50
p38β 1.1 0.014 IKKβ >50 >50
p38γ >100 >100 JNK1α1 >50 >50
Abl 25 >50 JNK2α2 >50 >50
Aurora-A >50 >50 KDR >50 >50
BTK >50 >50 Lck >50 >50
CaMKIV >50 >50 Mapkap K2 >50 >50
CDK1/cyclinB >50 >50 Met >50 >50
CHK1 >50 >50 NEK2 >50 >50
CK1δ >50 >50 PAK4 >50 >50
CK2 >50 >50 PDK1 >50 >50
CSK >50 32 PKA >50 >50
EGFR >50 >50 PKBb >50 >50
EphB4 >50 >50 PKCa >50 >50
ERK1 >50 >50 PKCθ >50 >50
ERK2 >50 >50 ROCK-II >50 >50
FGFR3 >50 >50 Rsk2 >50 >50
Flt3 >50 >50 Src >50 >50
GSK3β >50 >50 Tie2 37 >50
Flt1
>50
>50
Zap-70
>50
>50