Pub. Date : 2021 Oct
PMID : 34471993
3 Functional Relationships(s)Download |
Sentence | Compound Name | Protein Name | Organism |
| 1 | Concentrations providing half-maximal inhibition (IC50) in these assays were determined for deucravacitinib and the JAK 1/2/3 inhibitors tofacitinib, upadacitinib, and baricitinib. | upadacitinib | Janus kinase 1 | Homo sapiens |
| 2 | Simulations indicated that tofacitinib, upadacitinib, and baricitinib at steady state exhibited varying degrees of JAK 1/3 (daily average inhibition, 70-94%) and JAK 2/2 (23%-67%) inhibition at therapeutic concentrations, with Cmax values 17- to 33-fold lower than their TYK2 IC50 levels. | upadacitinib | Janus kinase 1 | Homo sapiens |
| 3 | Tofacitinib, upadacitinib, and baricitinib variably inhibit JAK 1/2/3 but not TYK2. | upadacitinib | Janus kinase 1 | Homo sapiens |