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. 2011 Sep 1;108(37):15366–15371. doi: 10.1073/pnas.1107906108

Table 1.

Assay data for compounds 1–5

graphic file with name pnas.1107906108unfig01.jpg
graphic file with name pnas.1107906108unfig02.jpg graphic file with name pnas.1107906108unfig03.jpg graphic file with name pnas.1107906108unfig04.jpg
Assay R = Compound 1 (X=H) Compound 2 (X=Cl) Compound 3 (X=OMe) Compound 4 Compound 5
EC50, μM
 H1N1 A/WSN/33 0.17 0.06 0.04 0.07 0.07
 H1N1 A/Solomon Islands/3/2006 4.9 1.0 0.66 3.5 12
 H1N1 A/CA/07/2009 >20 >20 >20 >20 >20
 H3N2 A/Brisbane/10/2007 >20 >20 7.3 >20 >20
 H5N1 A/Gull_PA/4175/83 0.15 0.10 0.07 0.11 0.04
IC50, μM
 H1N1 A/WSN polymerase 2.5 0.61 0.17 0.26 0.90
Aqueous solubility, μMa <5 <5 20 26 29
MLM stability, % remaining at 10 min 20 0 14 18 45

All EC50 and IC50 values are the mean of at least three experiments.

a20 mM phosphate buffer (pH 7.5), 1.0 M NaCl, and 8% DMSO.