IndraLab

Statements

Filgotinib inhibits JAK1. 8 / 8
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"JAK1 antagonist filgotinib and STAT3 antagonist S3I-201 reversed the effect of OSM, indicating that it acts on JAK1/STAT3 signaling."
34516050
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"In human whole blood assays, filgotinib dose-dependently inhibited JAK1 associated IL-6-induced STAT1 phosphorylation but had no effect on JAK2 associated GM-CSF induced STAT5 phosphorylation and demonstrated = ~ 30-fold selectivity for inhibition of JAK1- over JAK2 dependent signalling [XREF_BIBR]."
33237566
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"35 However, selective JAK1 inhibition by filgotinib showed increased remission rates in patients with moderate to severe CD."
33158881
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"In biochemical assays, filgotinib selectively inhibited the activity of JAK1 (> 5-fold higher potency) over JAK2, JAK3 and TYK2."
33237566
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"Target specificity In a cell-free enzyme assay , filgotinib inhibited JAK1 [ IC50 = 10 nM ] and , to a lesser extent , JAK2 [ IC50 = 28 nM ] , but with greater potency than JAK3 [ IC50 = 810 muM ] or TYK2 [ IC50 = 116 muM ] .33 In human whole-blood assays , a greater potency [ IC50 = 629 nM ] and a 28-fold selectivity of filgotinib was observed for JAK1 over JAK2 ."
32160283
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"For example, the JAK1 blocker filgotinib was tested in Crohn 's disease, whereas the JAK1/3 inhibitor tofacitinib was tested in clinical trials for both Crohn 's disease and ulcerative colitis."
29051788
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"In human cellular assays , filgotinib preferentially inhibited JAK1 / JAK3-mediated interleukin ( IL ) -2 , IL-4 and IL-15 signalling , JAK1 / 2-mediated IL-6 signalling and JAK1 / TYK2-mediated type I interferon signalling downstream of the heterodimeric cytokine receptors , with functional selectivity over cytokine receptors that signal via pairs of JAK2 or JAK2 / TYK2 [ 3 , 18 ] ."
33237566
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"An example is filgotinib, which preferentially inhibits JAK1."
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