Table 1.
Jak inhibitors and their selectivity profile.
| Compound | Primary target(s) | IC50 in cell free assay (nM) | |||
|---|---|---|---|---|---|
| Jak1 | Jak2 | Jak3 | Tyk2 | ||
| Tofacitinib | Jak3, Jak2, and Jak1 | 112 | 20 | 1 | 34 |
| Ruxolitinib | Jak1 and Jak2 | 3.3 | 2.8 | 428 | 19 |
| Baricitinib | Jak1 and Jak2 | 5.9 | 5.7 | 560 | 53 |
| Delgocitinib | Jak1, Jak2 | 2.8 | 2.6 | 13 | 58 |
| Momelotinib | Jak1, Jak2 | 11 | 18 | 155 | n.a |
| Filgotinib | Jak1 > Jak2 | 10 | 28 | 810 | 116 |
| Solcitinib | Jak1 | 8–9 | 108 | 539 | 225 |
| Upadacitinib | Jak1 | 47 | 120 | 2,300 | 4,700 |
| Itacitinib | Jak1 | 2 | 63 | >2,000 | 795 |
| Abrocitinib | Jak1 | 29 | 803 | >10,000 | 1,253 |
| PF-06651600 | Jak3 | >10,000 | >10,000 | 33,1 | >10,000 |
| PF-06700841 | Tyk2 > Jak1 | n.a | n.a | n.a | n.a |
| BMS986165 | Tyk2 | n.a | n.a | n.a | 2–14 |
| SAR-20347 | Tyk2 | 23 | 26 | 41 | 0.6 |
Obtained from MedChemExpress and Selleckchem. n.a, not available.