Table 5. Aryl- and cyclohexyl-substituted CAI-1 ester analogs.
Entry | Compound | EC50 (nM)a | % Responseb |
---|---|---|---|
1 | 1,100±270 | 59±22 | |
2 | 231±15 | 93±6 | |
2a | 151±20 | 92±13 | |
3 | 310±51 | 82±10 | |
4 | 84±6 | 97±6 | |
5 | 190±27 | 95±9 | |
6 | 190±19 | 100±6 | |
6a | 117±12 | 94±11 | |
7 | 3,700±580 | 83±13 | |
8 | >50,000 | llc | |
9 | 680±84 | 85±8 | |
10 | 1,600±210 | 79+10 | |
11 | 190±17 | 98±6 | |
12 | 9,400±3,600 | 60±53 | |
13 | >50,000 | 28c |
Values determined using a light-based CqsS agonist bioassay, see Supporting Information. All EC50 values are the mean of triplicate analyses with the range defining the 95% confidence interval.
Percent maximal bioluminescence, with respect to CAI-1, which is set at 100%. The range defining the 95% confidence interval.
The maximal % response at the maximum concentration tested (50,000 nM).