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. 2022 Jun 17;13:892097. doi: 10.3389/fphar.2022.892097

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.