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Evaluation of the synthesized compounds for affinity against nucleoside kinases.
| Compound | Conc. Unit | IC50 a | ||
|---|---|---|---|---|
| Human TK-1 | Human TK-2 | HSV-1 TK | ||
| 2a | µg/mL | >200 | >200 | 150 ± 15 |
| 2b | µg/mL | >200 | 93 ± 7 | 1.6 ± 0.1 |
| 2c | µg/mL | >200 | >200 | >200 |
| 2d | µg/mL | >200 | >200 | 52 ± 28 |
| 2e | µg/mL | >100 | >100 | >100 |
a 50% inhibitory concentration, or compound concentration required to inhibit TK-catalyzed conversion of [3H]dThd to its 5′-monophosphate derivative.
