Table 2. Inhibition of enzymatic activities of porcine pancreatic group IB (pGIB) and human group IIA (hGIIA) PLA2s by compounds C1 to C8 and their corresponding log P values.
Cpd | Log P * | IC50 (µM) | |
hGIIAPLA2 | pGIBPLA2 | ||
C1 | 3.81 | 5.0±0.7 | >100 |
C2 | 5.59 | 10.0±1.5 | >100 |
C3 | 2.88 | 5.0±1.2 | >100 |
C4 | 4.57 | 6.5±1.8 | >100 |
C5 | 3.91 | 2.5±0.5 | >100 |
C6 | 5.59 | 3.0±0.2 | >100 |
C7 | 3.64 | 35±1.8 | >100 |
C8 | 7.13 | 0.62±0.15 | >100 |
*: calculated using the Rekker's hydrophobic fragmental constants