Table 3.
Biochemical potency of tofacitinib15 and PF-06673518 TYK2 wild type human TYK2 kinase, mouse wild type TYK2, and human (I960V).
Compound | Human WT TYK2 IC50 (nM) | Mouse WT TYK2 IC50 (nM) | Human I960V TYK2 IC50 (nM) |
---|---|---|---|
Tofacitinib | 489 | 966 ± 157 | 487 ± 89 |
PF-06673518 | 29 ± 11 | 1,407 ± 472 | 846 ± 284 |
Compounds were assayed at least three times, and the IC50 reported as the geometric mean ± standard deviation. ATP concentration = 1 mM.