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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