Inhibitory activity of selected pyrazolopyrimidine sulfamates in E1 enzyme assays.

Homogeneous Time-Resolved Fluorescence (HTRF) enzyme assays were employed to evaluate the 50% Inhibitory Concentrations (IC50) values for compounds against Atg7 (autophagy-related protein-7), NAE (NEDD8-activating enzyme), UAE (ubiquitin activating enzyme) and SAE (SUMO-activating enzyme) with appropriately tagged ubiquitin-like proteins and E2 conjugating enzymes as described in the Methods. GABARAP = GABAA receptor-associated protein. Data represent mean ± SEM. n = Number of independent experiments.