Off target protein and potency:
Tyk2 53 nM, JAK3 560 nM, AAK1 17.2 nM, BIKE 39.8 nM, GAK134.4 nM, MPSK1 68.5 nMPotency assay (off target):
TR-FRET, ITC
Probe Selectivity in Vitro:
JAK3 IC50 ~ 560 nM, ~10-fold selectivity against Tyk2 (IC50 = 53 nM), c-Met (IC50 > 10,000 nM) and Chk2 (IC50 > 1,000 nM). Tested @ 500 nM against a diverse panel of 28 kinases with no significant inhibition observed.
Additional Off Targets are (Kd): AAK1 17.2 nM, BIKE 39.8 nM, GAK134.4 nM , MPSK1 68.5 nM
