Table 1.

Activity of GSK1838705A in kinase-selectivity panel

Graphic

KinaseIC50 (nmol/L)KinaseIC50 (nmol/L)
AKT1>10,000JNK15,000
AKT2>10,000JNK28,000
ALK0.5JNK32,000
ALK5>10,000LCK>25,000
ASK1>25,000MAPKAPK2>25,000
Aurora A>10,000P38a>25,000
Aurora B>10,000PAK1>10,000
B-Raf V600E>2,000PCTAIRE1>10,000
CAMKK2>10,000PDK1>10,000
CDK2/CyclinA>10,000PI3Kα>10,000
EGFR>10,000PI3Kβ>10,000
ErbB2>10,000PI3Kδ>10,000
ErbB4>25,000PI3Kγ>10,000
GSK3β>25,000PKCε>10,000
HGK>10,000PKCq>10,000
IGF-IR1.6ROCK1>10,000
IKK1>25,000RSK11,600
IKK2>25,000SRC1>10,000
IKK3>10,000SYK>25,000
ITK>25,000VEGFR2>10,000
IR2YAK3>10,000
JAK1>25,000ZAP70>25,000
JAK213,000P70S6K>10,000
JAK35,000