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 |
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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).