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Table 3 Overview of the data for four representative compounds

From: Inhibitors of the integrase–transportin-SR2 interaction block HIV nuclear import

  In vitro MT4 cells HeLaP4 cells
AlphaScreena MTTb Flucc PIC assayd
IC50 (µM) PIN (%) EC50 (µM) CC50 (µM) % Protection PIN (%) p value
MVG010 54.6 37.1 > 100 100 6 34.2 0.1209
MVG030 33.6 71.6 > 97 97 25 23.3 0.0411
MVG036 37.6 105.6 > 55 65 46 0.0011
MVG044 17.1 75.9 > 250 > 250 22 16.3 0.00001
  1. aHIV-1 IN–TRN-SR2 AlphaScreen IC50 values and percentage inhibition (PIN) are presented. All compounds were tested at 50 µM
  2. bEC50 and CC50 values in MT4 cells are given as well as the percentage of protection against the cytopathic effect of HIV
  3. cHeLaP4 cells were infected with a single-round virus expressing the firefly luciferase reporter gene (Fluc) in the presence of one of the compounds (100 µM) and the results are expressed as a percentage inhibition relative to the DMSO control
  4. dFor the PIC assay in HeLaP4 cells, p values (Mann–Whitney U test), compared to the DMSO control, are given