The effects of the S1P1 Leu276Phe, and S1P3 Phe263Leu mutations on affinities of S1P, FTY720-P, compound A, and compound B
Compound affinities (Log IC50) were calculated from [33P]S1P binding dose response curves. Results are expressed as the mean ± S.E. of three experiments performed in triplicate.
Compound | Log IC50 | ||||||
|---|---|---|---|---|---|---|---|
| S1P1 | S1P1 L276F | S1P3 | S1P3 F263L | ||||
| M | |||||||
| S1P | -9.20 ± 0.22 | -9.29 ± 0.16 | -9.35 ± 0.15 | -9.29 ± 0.17 | |||
| FTY720-P | -8.96 ± 0.08 | -8.88 ± 0.04 | -8.57 ± 0.19 | -8.41 ± 0.13 | |||
| Compound A | -8.49 ± 0.19 | -7.37 ± 0.08* | -5.73 ± 0.15 | -6.71 ± 0.03§ | |||
| Compound B | -8.93 ± 0.04 | -7.33 ± 0.05¶ | -5.38 ± 0.15 | -7.56 ± 0.05† | |||