Kinetic analysis of BVDU and TK inhibitors against TK-2 and HSV-1 TK using ATP as the varying substrate
| Compound | TK-2 | HSV-1 TK | ||||
|---|---|---|---|---|---|---|
| Ki | Ki/Km | Nature of Inhibition | Ki | Ki/Km | Nature of Inhibition | |
| μM | μM | |||||
| KIN-12 | 17 ± 0.2 | 0.81 | U.C. | 33 | 6.4 | U.C. |
| KIN-52 | 24 ± 4.5 | 1.1 | U.C. | N.A. | N.A. | N.A. |
| BVDU | 5.3 ± 0.6 | 0.21 | N.C. | 14 ± 1.0 | 1.7 | N.C. |
Ki values are derived from Lineweaver-Burk plots. Km values for ATP are 23 μM (TK-2) and 6.8 μM (HSV-1 TK).
U.C., uncompetitive; N.C., noncompetitive; N.A., not applicable: no measurable inhibition.