Table 2.
Radio-TLC assay with [14C]SAG substrate of the inhibition of mDAGLα activity
| Compound Number | Detail of N-formyl-α-amino ester | mDAGLα inhibition at 10 nM (%) | mDAGLagr; inhibition at 100 nM (%) | mDAGLagr; inhibition at 1000 nM (%) | mDAGLagr; inhibition at 10000 nM (%) |
|---|---|---|---|---|---|
| 3 (THL) | L-leucyl | 55 | 72 | 92 | 98 |
| 4 (OMDM-188) | L-isoleucyl | 69 | 80 | 96 | 96 |
| 5 | L-allo-isoleucyl | 60 | 61 | 88 | 100 |
| 6 | D-isoleucylA | 33 | 29 | 69 | 85 |
| 7 | D-allo-isoleucyl | 19 | 51 | 75 | 90 |
| 8 | (S)-α-aminobutyryl | 50 | 68 | 96 | 100 |
| 9 | NA | ND | ND | ND | <0 |
| JZL184 | NA | ND | ND | ND | 3 |
| URB597 | NA | ND | ND | ND | <0 |
| n-C16H33SO2F | NA | ND | ND | 18 | 64 |
| JZL195 | NA | ND | ND | ND | 10 |
NA, not applicable; ND, not done
A
5% impurity in D-isoleucyl analog due to D-allo-isoleucyl analog