Table 1 Antiviral activity of HAP or SBA against HBV core mutants determined in the HepG2 HBV transient transfection assay.

From: Heteroaryldihydropyrimidine (HAP) and Sulfamoylbenzamide (SBA) Inhibit Hepatitis B Virus Replication by Different Molecular Mechanisms

 

HAP_R01

Bay 41-4109

SBA_R01

ETV

Mean EC50 (nM) ± SD

FC

Mean EC50 (nM) ± SD

FC

Mean EC50 (nM) ± SD

FC

Mean EC50 (nM) ± SD

FC

WT

91 ± 10

1

149 ± 25

1

390 ± 44

1

1.40 ± 0.20

1

Core T33N

3471 ± 2065

38.1

>10000

>67

>5000

>13

1.16 ± 0.01

0.8

Core T33Q

1972 ± 607

21.7

3722 ± 890

25.0

>5000

>13

2.09 ± 0.73

1.5

Core T33S

162 ± 46

1.8

451 ± 205

3.0

878 ± 112

2.3

1.35 ± 0.25

1.0

Core P25G

1384 ± 62

15.2

>10000

>67

4749 ± 337

12.2

2.23 ± 0.52

1.6

Core P25A

735 ± 118

8.1

3452 ± 1438

23.2

895 ± 71

2.3

1.34 ± 0.12

1.0

Core P25S

902 ± 86

9.9

4278 ± 461

28.7

930 ± 168

2.4

1.10 ± 0.46

0.8

Core V124I

9 ± 1

0.1

13 ± 3

0.09

42 ± 2

0.1

0.69 ± 0.25

0.5

Core V124F

1086 ± 113

11.9

2332 ± 799

15.7

289 ± 102

0.7

2.53 ± 0.68

1.8

  1. Shown are mean EC50 values ± standard deviation (SD) from three independent experiments. EC50 fold-change values (FC) were calculated by dividing the mutant EC50 value by the wild type EC50 value.
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