Table 1.
Comp | Model[a] | Activity[b] [%] | IC50[c] [νm] |
---|---|---|---|
1 | – | 74.6±10.7 | >10 |
2 | M2 | 14.9±4.9 | 0.43 |
3 | – | 60.8±10.7 | >10 |
4 | – | 75.5±12.9 | >10 |
5 | – | 73.3±9.7 | >10 |
6 | – | 89.1±12.5 | >10 |
7 | M2 | 53.9±2.7 | >10 |
8 | M1 | 12.8±3.7 | 0.4 |
9 | M2 | 22.1±5.6 | 1.15 |
10 | – | 87.5±13.2 | >10 |
Pharmacophore models: “M1”= retrieved by pharmacophore model M1; “M2”= retrieved by pharmacophore model M2; “–”= not found by M1 or M2.
mPGES-1 % remaining activity at 10 μm. Data represent the mean ±SE of n=3–4 independent experiments.
IC50 against mPGES-1. Values quoted were determined by extrapolation. See the Experimental Section for details.