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up to 1 uM
1H NMR (300 MHz, DMSO-d6) d 9.78 (s, 1 H), 9.20 (s, 1 H), 7.89 (d, 2 H, J = 8.4 Hz), 7.66 (s, 1 H), 7.28-7.32 (m, 3 H), 7.18 (s, 1 H), 7.14 (d, 2 H, J = 8.4 Hz), 3.93 (s, 1 H), 3.57 (m, 1 H), 3.53 (s, 3 H), 3.20 (d, 1 H, J = 11.7 Hz), 2.93 (d, 1 H, J = 11. 1 Hz), 2.80 (s, 3 H), 2.73 (m, 2 H), 2.59 (m, 2 H), 2.54 (m, 1 H), 2.26 (s, 3 H), 2.01 (s, 3 H), 1.75 (m, 4 H)
excellent biochemical selectivity against a panel of 331 kinases, except for TEC-family kinase Bmx where a 3-fold difference was observed.
Minimal to no off-target receptor activity when screened against a panel of 30 targets (all <35% at 10 μM), minimal inhibition of the hERG channel (27% at 10 μM), and was negative in a gene-tox profile Ames (TA98/100 strains; +/− S9) and micronucleus tests (+/− S9). Known to bind six AO substrates with IC50 values ranging from 0.86 to 1.87 μM.
