| Assay Method Information | |
| | In Vitro FTase/GGTase-1 Inhibition Assay |
| Description: | Compounds were tested as inhibitors of FTase or GGTase-1 in vitro using purified recombinant mammalian enzymes to catalyze the reactions between [3H] FPP or [3H]GGPP, and recombinant protein substrates. Incorporation of radiolabeled isoprenoid into Ras protein substrate was quantitated by precipitation of total protein with acid and scintillation counting. The inhibitory activity of the compounds is reported as an IC50 value, the concentration of inhibitor required to reduce radiolabel incorporation by 50% compared with an uninhibited control experiment. |
| Affinity data for this assay | |
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