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| | GCN2 Enzyme Inhibition (ATP 300 uM) |
| Description: | The inhibitory activity of the Example compounds towards GCN2 enzyme was measured according to the description below, using a LanthaScreen TR-FRET (Time Resolved Fluorescence Resonance Energy Transfer) Kinase Activity assay distributed by ThermoFisher Scientific. The full-length human GCN2 enzyme (UniProt accession number Q9P2K8) was used for all experiments (Carna Bioscience). The TR-FRET pair was composed of GFP-eIF2α and LanthaScreen Terbium-labeled anti-peIF2α (pSer52) Antibody. Each example compound was dissolved in DMSO (0.15 mM) and dispensed in a 384-well plate by a D300 dispenser (Tecan) to a final concentration range 3000-0.13 nM using the logarithmic dilution mode in 2 replicates. Full inhibition (3000 nM commercial reference inhibitor) and DMSO vehicle control wells were also included on the same plate. All volumes were normalized to the final DMSO concentration of 2% of the reaction volume. Next, 5 μL of H2O was added to each well of the plate. |
| Affinity data for this assay | |
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