Table 1 Biochemical potency of tofacitinib15 and PF-06673518 across wild type human TYK2 and mouse wild type TYK2; Compounds were assayed at least three times, and the IC50 reported as the geometric mean along with ± standard deviation.

From: Demonstration of In Vitro to In Vivo Translation of a TYK2 Inhibitor That Shows Cross Species Potency Differences

Compound

Human WT

Mouse WT

JAK1 IC50 (nM)

JAK2 IC50 (nM)

JAK3 IC50 (nM)

TYK2 IC50 (nM)

TYK2 IC50 (nM)

Tofacitinib

15

77

55

489

966 ± 157

PF-06673518

41 ± 15

652 ± 175

4,267 ± 1,060

29 ± 11

1,407 ± 472

  1. ATP concentration = 1 mM.
Back to article page