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up to 100 nM
1H NMR (400 MHz, DMSO) δ 12.78 (s, 1H), 10.05 (s, 1H), 8.08 (s, 1H), 7.66 (s, 1H), 7.37–7.22 (m, 5H), 5.42 (dd, J = 9.3, 5.3, 1H), 2.66 (t, J = 6.0, 2H), 2.38 (s, 2H), 2.25–2.02 (m, 10H), 1.47 (t, J = 6.4, 2H), 0.96 (s, 6H);
Broad kinase selectivity of this molecule was observed: only six of 286 off-target kinases were inhibited >70% when tested at 0.1 μM (>100X ITK Ki).