Off target protein and potency:
LRRK2 16 nMPRKD1 35 nMPotency assay (off target):
In a panel of 20 kinases, BIX-02565 inhibited six of them with IC50 < 1 uM.
In an expanded panel of 20 kinases, BIX-02565 inhibited only 4 additional kinases with an IC50 < 1 uM (PRKD2, PRKD3, RET, FLT3).
Overall, with the exceptions of LRRK2 and PRKD1, BIX-02565 is >100-fold selective for RPS6KA3 in vitro.
Probe Selectivity in Vitro:
Outside target family: Tested in a panel of 68 receptors, ion channels, and protein targets for off-target inhibition of radioligand binding @ 10 uM. The compound elicited >50% inhibition at adrenergic a1A-, a1B-, a1D-, a2A-, 2-, and imidazoline I2 receptors (IC50 values ranged between 0.052 and 1.820 uM).
