TABLE 1

Anti HBV activity and cytotoxicitya

CompoundMean (range) EC50 (nM) in HepG2.2.15 cellsMean (range) CC50 (nM)SI
HepG2.2.15 cellsHepG2 cellsHepG2.2.15cellsHepG2cells
JNJ-632121 (44–191) (n = 8)>25,000 (>25,000–>25,000) (n = 4)>100,000 (>5,000–>100,000) (n = 52)>206>826
AT130127 (<98–207) (n = 4)ND>50,000 (>25,000–>50,000) (n = 11)>394
BAY41-4109101 (25–216) (n = 99)33,900 (21,400–>50,000) (n = 3)35,400 (10,600–120,000) (n = 56)336350
ETV0.07 (0.04–0.10) (n = 2)>100 (>100–>100) (n = 4)>25,000 (>25,000–>25,000) (n = 3)>1,429>357,142
  • a The anti-HBV activity of JNJ-632, AT130, BAY41-4109, and ETV in stable HBV-replicating HepG2.2.15 cells was tested in a dose-response assay. HBV DNA was extracted from the cell culture supernatant, and DNA levels were assessed using qPCR. In each experiment, EC50s were determined on the basis of the mean inhibition from 2 wells per compound concentration. The cytotoxicity for HepG2 cells was assessed using a resazurin readout. EC50, 50% effective concentration; CC50, 50% cytotoxic concentration; n, number of experiments; SI, selectivity index; ND, not done.