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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
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Retrovirology

ISSN: 1742-4690

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