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Enzyme inhibitory activity of 19a-c, 20a-c, 21a-c
| Inhibitor structure | Ki (nM) | IC50 (nM)a |
|---|---|---|
|
82 ± 2 | >1000 |
|
16 ± 1 | >1000 |
|
6.9 ± 0.2 | >1000 |
|
6.8 ± 0.8 | >1000 |
|
15 ± 3 | 380 |
|
6 ± 1 | 200 |
|
2.8 ± 0.3 | 6.3 |
|
3.7 ± 0.3 | 650 |
|
58 ± 6 | >1000 |
|
0.31 ± 0.03 | 9 |
|
0.15 ± 0.01 | 52 |
|
0.07 ± 0.02 | 170 |
MT-2 human T-lymphoid cells exposed to HIV-1LAI; Saquinavir and amprenavir exhibited IC50 values of 16 nM and 27 nM, respectively.
