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. Author manuscript; available in PMC: 2017 Jul 14.
Published in final edited form as: J Med Chem. 2016 Jun 17;59(13):6136–6148. doi: 10.1021/acs.jmedchem.6b00040

Table 6.

Biochemical inhibition of RT-associated RNase H and the antiviral correlation

Compound RNase H INST CPE MAGI
IC50 (μM)a IC50 (μM)a EC50 (μM)b EC50 (μM)c
26 0.061 ± 0.004 0.080 ± 0.007 0.83 3.7 ± 0.3
30 0.042 ± 0.012 0.033 ± 0.004 0.061 0.30 ± 0.01
38 0.011 ± 0.003 0.049 ± 0.004 0.033 0.09 ± 0.02
40 0.010 ± 0.006 0.068 ± 0.011 0.032 0.07 ± 0.02
42 0.026 ± 0.009 0.077 ± 0.011 0.049 0.30 ± 0.06
44 0.022 ± 0.009 0.12 ± 0.021 0.19 0.80 ± 0.2
45 0.029 ± 0.015 0.021 ± 0.002 0.015 0.30 ± 0.09
46 0.020 ± 0.010 0.051 ± 0.013 0.15 1.3 ± 0.2
3 >10 0.068 ± 0.01 -- 0.020 ± 0.002
1 >10 0.65 ± 0.14 0.023 0.030 ± 0.008
a

Concentration with 50% enzyme inhibition, expressed as mean ± standard deviation from three independent experiments.

b

Concentration of a compound inhibiting virus replication by 50%.

c

Concentration of a compound inhibiting virus replication by 50%, expressed as mean ± standard deviation from three independent experiments.