Table 1.
In vitro JAK isoform selectivity of the JAK inhibitors based on enzymatic assays
| Classification | IC50 (nM) |
||||
|---|---|---|---|---|---|
| JAK1 | JAK2 | JAK3 | TYK2 | ||
| Abrocitinib [47] | Selective JAK1 inhibitor | 29.2 | 803 | >10 000 | 1250 |
| Baricitinib [68] | Selective JAK1/2 inhibitor | 5.9 | 5.7 | >400 | 53 |
| Filgotinib [49] | JAK1/2 inhibitor | 10–53 | 28–29 | 311–810 | 116–177 |
| Peficitinib [39] | Pan-JAK inhibitor | 3.9 | 5.0 | 0.7 | 4.8 |
| Tofacitinib [72] | JAK1/3 inhibitor | 3.2 | 4.1 | 1.6 | 34 |
| Upadacitinib [54] | Selective JAK1 inhibitor | 43 | 120 | 2300 | 4700 |
IC50: half maximal inhibitory concentration; JAK: Janus kinase; TYK: tyrosine kinase.