Table 2.
Anti-COVID-19 (anti-SARS-CoV-2/anti-VOC-202012/01) activities (along with human cells toxicities) of Taroxaz-104 (using GS-443902 as the positive control/reference drug, and DMSO as the negative control/placebo drug) against SARS-CoV-2 (VOC-202012/01 strain) in Vero E6 cells.
| Classification | Compound Name |
CC50a (μM) |
Inhibition of SARS-CoV-2in vitro(Anti-VOC-202012/01 Bioactivities) (μM) |
||
|---|---|---|---|---|---|
| 100% CPE Inhibitory Concentration (CPEIC100)b |
50% Reduction in Infectious Virus (EC50)c |
50% Reduction in Viral RNA Copy (EC50)d | |||
| Target Compound | Taroxaz-104 | > 100 | 1.20 ± 0.08 | 0.42 ± 0.02 | 0.46 ± 0.03 |
| Reference Compound | GS-443902 | > 100 | 20.50 ± 0.93 | 18.05 ± 0.88 | 18.67 ± 0.90 |
| Placebo Solvent | DMSO | > 100 | > 100 | > 100 | > 100 |
CC50 or 50% cytotoxic concentration is the concentration of the tested compound that kills half the cells in an uninfected cell culture. CC50 was determined with serially-diluted compounds in Vero E6 cells at 48 h postincubation using CellTiter-Glow Luminescent Cell Viability Assay (Promega).
CPEIC100 or 100% CPE inhibitory concentration is the lowest concentration of the tested compound that causes 100% inhibition of the cytopathic effects (CPE) of SARS-CoV-2 VOC-202012/01 virus in Vero E6 cells under increasing concentrations of the tested compound at 48 h postinfection. Compounds were serially 2-fold or 4-fold diluted from 100 μM concentration.
EC50 or 50% effective concentration is the concentration of the tested compound that is required for 50% reduction in infectious SARS-CoV-2 VOC-202012/01 virus particles in vitro. EC50 is determined by infectious virus yield in culture supernatant at 48 h postinfection (log10 TCID50/mL).
EC50 or 50% effective concentration is the concentration of the tested compound that is required for 50% reduction in SARS-CoV-2 VOC-202012/01 viral RNA copies in vitro. EC50 is determined by viral RNA copies number in culture supernatant at 48 h postinfection (log10 RNA copies/mL).