TABLE 1.
Rate constants related to each model for different substrates in human liver cytosol
| Substrate | Rate Constants | MAM | Dead Model | MM |
|---|---|---|---|---|
| Liters/min | ||||
| O6BG | k3 | 25.444 | 12.954 | 8.691 |
| k4 | 0.057 | 0.006 | — | |
| k5 | 13.708 | — | — | |
| DACA | k3 | 33.004 | 19.449 | 6.209 |
| k4 | 0.044 | 0.024 | — | |
| k5 | 6.086 | — | — | |
| Zaleplon | k3 | 1.238 | 0.853 | 0.46 |
| k4 | 0.028 | 0.011 | — | |
| k5 | 0.604 | — | — | |
| Phthalazine | k3 | 466.834 | 351.727 | 11.086 |
| k4/ | 0.335 | 0.366 | — | |
| k5 | 8.523 | — | — | |
| BIBXa | k3 | 0.279 | 0.253 | 0.125 |
| k4 | 0.012 | 0.012 | — | |
| k5 | 0.097 | — | — | |
| Zoniporidea | k3 | 0.082 | 0.079 | 0.085 |
| k4 | −0.023 | −0.001 | — | |
| k5 | 0.163 | — | — |
DACA, N-(2-dimethylamino)ethyl)acridine-4-carboxamide; MAM, modulated activity model; MM, Michaelis-Menten; O6BG, O6-benzylguanine.
a
Rate constants are based on peak area ratio (PAR).