Table 1. S1P4–R agonist activity of compounds 15a-15n (EC50 nM).
cpd | R2 | R1 | X | EC50 (nm)α |
---|---|---|---|---|
15a | NMe | H | S | 3600 |
15b | NH | H | S | NA |
15c | NPh | Me | S | 2800 |
15d | NPh | H | S | NA |
15e | N(pyridin-2-yl) | H | S | 2100 (70%) β |
15f | O | Me | S | NA |
15g | NEt | Et | S | 250 |
15h | NCH2CH2OH | Me | S | 306 |
15i | NMe | Me | O | NA |
15j | NCH2CH2CH2 | S | NA | |
15k | NCH2CH2 | S | NA | |
15l | NiPr | iPr | S | NA |
15m | NnPr | nPr | S | NA |
15n | NnBu | nBu | S | NA |
Data are reported as mean of n = 3 determinations.
Percentage of response.
NA = not active at concentrations up to 25 μM.