TABLE 1.
Radioligand binding affinities for human S1P1 and S1P5.
| Compound | Human S1P1 Ki (nM) | Human S1P5 Ki (nM) |
|---|---|---|
| Ozanimod | 0.5 ± 0.03 | 1.93 ± 0.07 |
| S1P | 2.33 ± 0.17 | 2.69 ± 0.31 |
| FTY720-p | 0.1 ± 0.01 | 0.26 ± 0.03 |
| Amiselimod-p | 0.13 ± 0.02 | 0.25 ± 0.04 |
| Ponesimod | 9.37 ± 1.31 | 17.43 ± 4.32 |
| Siponimod | 0.74 ± 0.09 | 0.43 ± 0.08 |
| KRP-203-p | 0.22 ± 0.02 | 0.24 ± 0.04 |
| Etrasimod | 6.73 ± 0.62 | 16.3 ± 0.71 |
[3H]-ozanimod was competitively displaced with increasing concentration of test compound using Chinese hamster ovary cell membranes stable expressing recombinant human S1P1 or human S1P5. Data shown are the mean ± standard error of the mean of the binding affinities calculated for 3–5 replicate experiments run in duplicate wells.
S1P, sphingosine 1-phosphate; S1P1, sphingosine 1-phosphate receptor subtype 1; S1P5, sphingosine 1-phosphate receptor subtype 5.