Table 2.
Kinetic Parameters of the Selected Inhibitors
|
|
|
Inhibitor Concentrations, μM |
||||||
---|---|---|---|---|---|---|---|---|---|
ID | NSC | Kinetic Parameters | 0 | 0.156 | 0.3125 | 0.625 | 1.25 | 2.5 | 5 |
1 |
NSC86314 |
VM, RFU/s |
35.84 ± 0.26 |
— |
34.65 ± 0.50 |
32.46 ± 0.59 |
28.77 ± 0.49 |
21.87 ± 0.70 |
13.10 ± 0.61 |
|
|
KM, μM |
57.38 ± 1.02 |
— |
51.79 ± 1.92 |
51.45 ± 2.40 |
46.38 ± 2.08 |
40.95 ± 3.59 |
25.02 ± 3.64 |
2 |
NSC716898 |
VM, RFU/s |
34.24 ± 0.28 |
— |
35.25 ± 0.24 |
35.94 ± 0.67 |
32.34 ± 0.26 |
27.27 ± 0.34 |
21.78 ± 0.66 |
|
|
KM, μM |
48.84 ± 1.02 |
— |
49.37 ± 0.86 |
54.75 ± 2.56 |
43.29 ± 0.92 |
36.83 ± 1.29 |
28.26 ± 2.60 |
3 |
NSC157058 |
VM, RFU/s |
32.27 ± 0.59 |
32.87 ± 0.53 |
31.90 ± 0.50 |
30.18 ± 0.50 |
26.46 ± 0.68 |
24.08 ± 0.49 |
— |
KM, μM | 44.17 ± 2.17 | 45.69 ± 1.97 | 45.93 ± 1.90 | 45.35 ± 2.01 | 40.87 ± 2.86 | 40.55 ± 2.26 | — |
The KM and Vmax values were determined using the purified WNV NS2B-NS2pro samples and the pyroglutamic acid-Arg-Thr-Lys-Arg-7-amino-4-methylcoumarin fluorescence-quenched peptide substrate in the presence of the indicated concentrations of the inhibitors.
RFU, relative fluorescence unit.