Table 1.
Overview of in vitro and cellular activities of 160 kinase inhibitors tested at 10 and 5μM, respectively.
160 kinase inhibitors from a panel of inhibitors known to target kinases in all branches of the kinome were tested for their ability to (i) inhibit LRRK2 at 10 μM in an in vitro kinase assay using the LRRKtide model peptide substrate and (ii) dephosphorylate LRRK2 at phosphoserine 935 in a spotblot assay. Listed are the exact values (expressed as a % relative to the control) obtained in these tests for each compound. A general overview of these tests are given in Figures 1, 3 and the plate and position references given in the first 2 columns correspond to those given in Figures 1B, 3B. Color codes to facilitate identification of compounds from the three selected chemical classes are: (A) 9-methyl-N-phenylpurine-2,8-diamine compounds highlighted in green, (B) N-phenylquinazolin-4-amine analogs given in orange, and (C) 1,3-dihydroindol-2-one analogs in blue. The 20 most potent compounds in the cellular assay are indicated in bold. The 3rd column of the table (labeled “class”) indicates the compound classes (A–C) or the 20 most active compounds in the cellular assay (asterisk), as applicable.