Table 2.
Compound | Structures |
kinact/KI, M−1s−1 |
Potency ratio |
||
---|---|---|---|---|---|
hFAAH | rFAAH | h/rFAAH | hFAAH/rFAAH | ||
1(PF-750) | 791 ± 34 | 104 ± 14 | 528 ± 53 | 7.6 | |
2(PF-622) | 621 ± 130 | 154 ± 67 | 623 ± 250 | 4.0 | |
3 | 2,110 ± 230 | 322 ± 120 | 1,960 ± 1,100 | 6.6 | |
4 | 468 ± 53 | 18.2 ± 8.2 | 415 ± 65 | 26 | |
5 | 1,520 ± 340 | 362 ± 32 | 1,300 ± 590 | 4.2 |
kinact/KI values were determined as described in Methods and by using Km values shown in Table 1. The concentrations of inhibitors varied from 0.012 to 25 μM. Values are averages ± SD of two independent experiments.