IndraLab
Statements
eidos
"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 ."
eidos
"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 ] ."