[3H]-A971432 competition radioligand binding affinity assessment for human and mouse wild type S1P5 and mouse S1P5_A120T performed using CHO cell membranes stably expressing the recombinant wild type receptors or transiently expressing mouse S1P5_A120T.
| Receptor | Ozanimod Ki | FTY720-p Ki | Siponimod Ki | A971432 Ki |
|---|---|---|---|---|
| nM | nM | nM | nM | |
| Human S1P5 | 2.0 ± 0.1 | 0.3 ± 0.01 | 0.2 ± 0.02 | 3.8 ± 0.4 |
| Mouse S1P5 | 59.9 ± 8.8 | 0.2 ± 0.01 | 0.3 ± 0.02 | 5.1 ± 0.4 |
| Mouse S1P5_A120T | 5.6 ± 1.2 | 0.3 ± 0.03 | 0.4 ± 0.03 | 6.0 ± 0.5 |
Data shown are means ± S.E.M. for n = 3 independent experiments each performed in duplicate. Ki is the binding affinity defined as the concentration required to elicit a 50% reduction in [3H]-A971432 binding once corrected for the concentration of radioligand used and the dissociation constant of the radioligand.