Table 1.

Effects of NVP-BYL719 against PI3K lipid or protein kinases

EnzymePI3KαE545K mutantH1047R mutantPI3KβPI3KδPI3KγPI4KβVps34mTORDNA-PKATR
MethodsKGKGKGKGAdaptaAdaptaKGKGTR-FRETCaliperα-screen
BYL719 IC50 nmol/L4.6 ± 0.44.0 ± 0.64.8 ± 0.41,156 ± 77290 ± 180250 ± 140581 ± 42>9,100>9,100>9,100>15,000

NOTE: In vitro assays were conducted with the indicated recombinant PI3K lipid or protein kinases in the presence of increasing concentrations of NVP-BYL719 as described in ref. 17. The concentration producing 50% inhibition of the enzymatic activity (IC50) in nmol/L as determined in multiple experiments (n = 2–20) is shown as an average ± SD.

Abbreviation: KG, KinaseGlo.