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Table 1 In vitro potency of upadacitinib

From: In vitro and in vivo characterization of the JAK1 selectivity of upadacitinib (ABT-494)

Recombinant Human Kinase

IC50 nM

Fold selectivity vs. JAK1

in Biochemical AssaysA

 JAK1

47 +/−  6.1

1

 JAK2

120 +/−  29.6

2.5

 JAK3

2304 +/−  380.3

49

 TYK2

4690

100

Engineered Cellular Assays

Ba/F3 Cellular

IC50 nM

Fold selectivity vs. JAK1

 JAK1

14

1

 JAK2

593 +/−  118.7

42

 JAK3

1860 +/−207.2

133

 TYK2

2715 +/−  548.7

194

Cytokine Signaling in Human Cells

Cytokine

JAK

pSTAT

Cells

Human IC50 nM

 IL-6

1

3

TF-1

11 +/− 1.3

 IL-6

1

3

CD14+ whole blood

78 +/− 0.3

 IL-6

1

3

CD3+ whole blood

207 +/− 9

 OSM

1

3

TF-1

1.6 N = 2

 Epo

2

5

UT7

649 +/−  41.2

 IL-2

1/3

5

T-blasts

10 +/− 1.1

 IL-15

1/3

5

T-blasts

22 +/−6.7

 IFNγ

1/2

1

CD14+ monocytes

19

 IL-4

1/3

6

HEKa B

2

 IL-13

1/TYK2

6

HEKa

4

 IL-31

1/2

3

HEKa

3

  1. aEnzyme reactions were conducted at 0.1 mM ATP. IC50 values represent the mean +/− SEM from at least three independent studies except where noted. B HEKa = human epithelial keratinocytes, adult