Table 4. S1P1-5–Rs selectivity counter screen of selected compounds.
| cpd | EC50 nM α | ||||
|---|---|---|---|---|---|
| S1P4 | S1P1 | S1P2 | S1P3 | S1P5 | |
| 4 | 205 | 819 | NA | NA | 721 (70%) β |
| 15g | 250 | NA | NA | NA | NA |
| 15h | 306 | 20% (8.3μM) χ | NA | NA | 60% (8.3μM) χ |
| 19e | 433 | 1800 (70%) β | NA | NA | 652 (50%) β |
| 19i | 210 | 4470 | NA | NA | NA |
| 19k | 440 | 3010 | NA | NA | 3400 |
| 19l | 602 | 68 | NA | NA | 237 |
| 19r | 262 | 720 | 3650 | NA | 144 |
| 19s | 72 | 250 | 60% (25μM) χ | 25%(25μM) χ | 51 |
| 19t | 92 | 34 | 120% (25μM) χ | 70%(25μM) χ | 34 |
| 19u | 314 | 18 | NA | NA | 22 |
| 19v | 147 | 287 | NA | NA | 37 |
α
Data are reported as mean of n = 3 determinations.
β
Percentage of response.
χ
Concentration producing the reported percentage of response.
NA = not active at concentrations up to 25 μM.