Table 1.
Steady-state kinetic parameters and inhibition constants.a
| KM (μM) | kcat × 10−3 (s−1) | Ki (μM) | |
|---|---|---|---|
| 3 | 1.8 ± 0.2 | 28 ± 0.2 | - |
| 2F-3 | 1.6 ± 0.2 | 0.2 ± 0.1 | 1.3 ± 0.1 |
| 3CH2F-3 | - | - | 2.3 ± 0.2 |
| 3CF3-3 | - | - | 1.6 ± 0.2 |
| (±)-12 | 25.0 ± 4.2 | 23 ± 0.1 | - |
a
Assays were carried out according to the standard, linear range, microassay procedure (see Supporting Info and Refs 16b and 20). Reported values are the average of 3 (Michaelis-Menten) or 2 (inhibition) measurements; all values were within 5% of the average. Errors are standard deviations for one sigma.