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Table 4 Antiviral activities in single-round and multiple-round infection assays

From: Dual inhibition of HIV-1 replication by integrase-LEDGF allosteric inhibitors is predominant at the post-integration stage

Drug

NL4-3 EC50(μM)

SR/MR ratio

Single-round

Multiple-round

EFV

0.0012 ± 0.0004

0.0013 ± 0.0002

0.9

RAL

0.0025 ± 0.0003

0.0024 ± 0.0006

1

EVG

0.00042 ± 0.00005

0.00086 ± 0.0004

0.5

NVP

0.041 ± 0.008

0.086 ± 0.012

0.5

AZT

0.0025 ± 0.0003

0.0024 ± 0.0006

0.6

IDV

Inactive

0.036

NA

SQV

Inactive

0.013

NA

Mut029

30 ± 4

3.8 ± 1.6

8

Mut047

37 ± 2

16 ± 7

2.3

Mut049

41 ± 2

2.0 ± 0.1

21

Mut062

30% @50

3.3 ± 1.5

>25

Mut075

23% @50

3.4 ± 1.0

>25

Mut101

9.0 ± 1.5

0.49 ± 0.04

18

  1. EC50 for the ARV activity of Mut101 compound series (tested in SR and MR assays) and the SR/MR ratio compared to the indicated drugs. Data represent the mean of six independent experiments.
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Retrovirology

ISSN: 1742-4690

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