Table 5.
Condition | VMAX (Percent of Control) | Apparent KM (nM) |
---|---|---|
A. SoRI-20040 | ||
Control | 100±7 | 36.8±1.4 |
0.8 μM | 74±7* | 50.7±2.2* |
3.2 μM | 39±2* | 48.6±3.0* |
12.8 μM | 22±2* | 50.4±5.0* |
B. SORI-20041 | ||
Control | 100±5 | 52.9±3.0 |
0.8 μM | 30±2* | 65.7±5.1* |
3.2 μM | 22±4* | 78.5±8.9* |
12.8 μM | 16±2* | 87.4±9.0* |
C. SORI-2827 | ||
Control | 100±7* | 41.7±2.1 |
0.8 μM | 98±7 | 72.1±2.3* |
3.2 μM | 92±6 | 89.8±3.5* |
12.8 μM | 68±4* | 84.6±5.6* |
Uptake binding surfaces were generated as described in Methods in the absence and presence of the indicated concentrations of test drugs. The data of 3 experiments (132 data points) were pooled and fit to the one component uptake equation for the best-fit estimates of the Vmax and Km. Each value is ±SD, n=3.
p<0.01 (F-test).