Table 1 In vitro IC50 values for the covalent JAK3 inhibitors used.

From: Generation of a chemical genetic model for JAK3

 

JAK3

JAK1

JAK2

TYK2

References

TL6-144

4.8 (10)

896 (75)

1050 (25)

> 10,000 (25)

25

TL8-52

1.3 (10)

24.4 (75)

17.6 (25)

320 (25)

25

PF-06651600

0.35 (4)

> 10,000 (40)

> 10,000 (4)

> 10,000 (12)

24

FM-381

0.127 (10)

52 (10)

346 (10)

459 (10)

23

  1. Published IC50 values (in nM) for the covalent JAK3 inhibitors used in this study are shown. ATP concentrations in μM used in the assays are shown in brackets.