Table 2.
IC50 values of C1-C8 against Human sEH(HsEH) and Murine sEH (MsEH)a.
|
|||||
|---|---|---|---|---|---|
| Compd. | R | HsEH (nM) | MsEH (nM) | cLogPb | LLEc |
| C1 |
|
183 | 2.0 | 4.466 | 2.272 |
| C2 |
|
16 | 0.53 | 4.141 | 3.655 |
| C3 |
|
0.8 | 0.18 | 2.997 | 6.100 |
| C4 |
|
1.54 | 0.44 | 3.374 | 5.438 |
| C5 |
|
2.94 | 0.23 | 2.663 | 5.869 |
| C6 |
|
0.84 | 0.35 | 3.330 | 5.746 |
| C7 |
|
0.91 | 0.55 | 2.486 | 6.555 |
| C8 |
|
0.35 | 0.12 | 1.803 | 7.653 |
| A | - | 4.6 | 1.3 | 3.358 | 4.979 |
| t-TUCB | - | 0.28 | 2.8 | 5.489 | 4.064 |
IC50 values were recorded on recombinant human sEH (HsEH) and murine sEH (MsEH) using PHOME as substrate at 50 mM concentration.
The cLogP values were predicted by BIOVIA Discovery Studio 2016.
Ligand lipophilicity efficiency (LLE) = pIC50-cLogP.