Table 1.

Inhibition of G312V and A204E variants by TAK779

CloneResidue change% inhibitiona
Q23-17G312V100 ± 0
A204E98 ± 1
QF495.A3G312V99 ± 1
A204E100 ± 0
MG505.H3G312V100 ± 0
A204E100 ± 0
BG505.B1G312V100 ± 0
A204E99 ± 0
Q259.D2.26G312V100 ± 0
A204E100 ± 0
SF162P3100 ± 0
NL-DT5R15 ± 21
  • a Percent inhibition of luciferase activity in cells treated with 1 μM TAK779, compared to untreated cells (averages ± standard deviations from two independent experiments).