Half-life measurement and decay constant by HPLC with glutathione and cysteine.
| Neq ID | pKi | Warhead | Half-life with glutathione | Half-life with cysteine | Decay constant with glutathione | Decay constant with cysteine |
|---|---|---|---|---|---|---|
| 409 | 6.3a | Methylene-nitrile | >6000 min | 74.3 min | — | 9.33 × 10−3 min−1 |
| 570 | 6.6a | Cyclopropane-nitrile | >6000 min | 159.0 min | — | 4.36 × 10−3 min−1 |
| 656 | 5.4 | Aldehyde | 40.0 min | 22.2 min | 1.73 × 10−2 min−1 | 3.12 × 10−2 min−1 |
| 690 b | 8.8 | Aza-nitrile | <5 min | <5 min | — | — |
| Nilvadipine | — | — | >5000 min | 49.5 min | — | 1.41 × 10−2 min−1 |
a
Values retrieved from the recent literature.7
b
When the concentrations of the compound Neq0690 and the thiol are half of the initial values, the kobs is 1.01 × 10−2 min−1 for the glutathione assay and 3.15 × 10−2 min−1 for the cysteine assay (t1/2 = 68.45 and 21.98 min respectively). The standard deviation is lower than 10% for all experiments.