Table 1.
Inhibition Patterns of the Three Compounds for TPH1
| Inhibitor | Varied Substrate | Fixed Substrate | Inhibition Patterns | Ki ( mean ± S.E.M, uM)a |
|---|---|---|---|---|
| LP-533401 | Trp | 200 uM 6-MePH4 | Cb | 0.31 ± 0.01 |
| LP-533401 | 6-MePH4 | 50 uM Trp | UCc | 0.81± 0.03 |
| LP-521834 | Trp | 200 uM 6-MePH4 | C | 0.036 ± 0.001 |
| LP-521834 | 6-MePH4 | 50 uM Trp | UC | 0.19 ± 0.01 |
| LP-534193 | Trp | 200 uM 6-MePH4 | C | 0.030 ± 0.001 |
| LP-534193 | 6-MePH4 | 50 uM Trp | UC | 0.17 ± 0.01 |
a
Values are calculated based on two independent experiments with each experiment carried out in triplicates.
b
C, competitive.
c
UC, uncompetitive.