High-throughput PARK7
inhibitor screen on a covalent fragment library
using the FP assay. (A) Screening results at 100 μM compound
concentration. Colors represent three different compound groups with
the highest hit rate. (B) Structures of representative hits. Colors
correspond to those in Figure A. (C) Heatmap displaying the validation
of the screening hits at 12.5, 37.5, and 100 μM using the FP
assay. (D) Heatmap displaying the validation of the representative
hits at 12.5, 37.5, and 100 μM using the DiFMUAc assay. (E)
Validation of representative hits in a cell lysate. The prepared cell
lysate was incubated with a dilution series of each compound, followed
by incubation with JYQ-92 (1 μM).