TABLE 2.
Antiviral activities of anti-HIV drugs that target different stages of HIV replication in the EASY-HIT system
| Phase | Classa | Compoundb | EASY-HIT EC50 (nM)c |
Reference data |
||
|---|---|---|---|---|---|---|
| HIV-1IIIB | Primary isolate | EC50 (nM) | Cell line (reference) | |||
| Early | Entry inhibitor | GRFT | 0.15 ± 0.01 | 0.19 ± 0.03 | 0.043-0.63 | CEM-SS human T4-lymphoblastoid cell line, PBMC (37) |
| Entry inhibitor | T20 | 4.58 ± 0.46 | 14.70 ± 2.34 | 0.4-190 | PBMC (27) | |
| NRTI | AZT | 146.00 ± 22.00 | ND | 15-390 | PBMC (40) | |
| NNRTI | EFV | 0.08 ± 0.01 | 0.03 ± 0.00 | 0.8-1.4 | MT-4 human leukemia T-cell line (22) | |
| Integration | RAL | 134.00 ± 72.80 | ND | 1.2-24 | PBMC (4) | |
| Integration | 118-D-24 | 4.37 ± 1.15 | 5.04 ± 0.5 | 7 | CEM-SS human T4-lymphoblastoid cell (51) | |
| Transcription | FLV | 17.17 ± 1.63 | ND | <12 | PM-1 T-cell lymphoma line (23) | |
| Late | PI | SQV | 2.96 ± 0.10 | 2.79 ± 0.27 | 8.0-220 | PBMC (40) |
| PI | DRV | 3.54 ± 0.10 | ND | 3 | MT-2 cells (29) | |
a
NRTI, nucleoside reverse transcriptase inhibitor; NNRTI, nonnucleoside reverse transcriptase inhibitor; PI, protease inhibitor.
b
GRFT, griffithsin; AZT, azidothymidine; EFV, efavirenz; RAL, raltegravir; FLV, flavopiridol; SQV, saquinavir; DRV, darunavir.
c
Mean values ± SD of three independent experiments are shown. Values for compound 118-D-24 are micromolar (μM). ND, not done.