Potency assay (off target):
LP-935509 effects on the kinase activity of the two most closely related kinases, BIKE and GAK (77% and 39% amino acid identity versus AAK1 in the kinase domain, respectively). LP-935509 was a potent inhibitor of BIKE (IC50 = 14 nM) and a modest inhibitor of GAK (IC50 = 320 ± 40 nM).
The ability of 1 µM LP-935509 to inhibit the binding of 389 kinases to an ATP-binding probe was measured showing that LP-935509 inhibited more than 70% of probe binding to 13 kinases, including BIKE.
Outside target family:
In functional or binding assays for 43 receptors, transporters, and enzymes, LP-935509 was inactive at up to 10 µM in the vast majority of the assays (42 of 43), with the most potent interaction observed for phosphodiesterase 4 (PDE4) (IC50 = 8.4 µM)
