Table 2 IC50 values [nM] for different N-phosphono-(S)−3-aminopiperidine-2-one compounds inhibiting DPP4/8/9
From: Sulphostin-inspired N-phosphonopiperidones as selective covalent DPP8 and DPP9 inhibitors
IC50 [nM] | ||||
|---|---|---|---|---|
| R | DPP4 | DPP8 | DPP9 |
5 C6-alkyl |
| 46,671 ± 6534 | 13,662 ± 735 | 42,669 ± 2551 |
6 C8-alkyl |
| 25,903 ± 5307 | 664 ± 115 | 6994 ± 1279 |
7 C10-alkyl |
| 19,961 ± 4300 | 231 ± 15 | 2125 ± 1236 |
8 C12-alkyl |
| 28,219 ± 3709 | 96 ± 8 | 486 ± 49 |
9 C5-alkyne |
| 2989 ± 970 | 668 ± 43 | 1573 ± 92 |
10 C8-alkyne |
| >100,000 | 11,418 ± 1033 | 32,686 ± 4630 |
11 |
| 952 ± 40 | 370 ± 23 | 1909 ± 158 |
12 |
| 243 ± 8 | 65 ± 3 | 179 ± 14 |
13 |
| 942 ± 55 | 199 ± 18 | 630 ± 14 |
14 |
| 4451 ± 174 | 2016 ± 118 | 13,250 ± 886 |
15 |
| 4713 ± 201 | 5864 ± 584 | 15,888 ± 652 |
16 |
| 16,150 ± 1350 | 14 ± 1 | 298 ± 21 |
