TABLE 3

Mean ± S.E. human sphingosine-1-phosphate receptor [35S]GTPγS binding data

Data are expressed as means ± S.E., N = 3 to 6 independent experiments. Italic = response achieved at the top test compound concentration of 10,000 nM.

CompoundHuman S1P1Human S1P2Human S1P3Human S1P4Human S1P5
EC50IAEC50IAEC50IAEC50IAEC50IA
nM%nM%nM%nM%nM%
S1P33.18 ± 0.83100213.06 ± 12.211001.56 ± 0.11100550.90 ± 25.241007.32 ± 0.83100
Ozanimod1.03 ± 0.1691.9 ± 1.9>10,00028.1 ± 0.72618 ± 20347.5 ± 2.7>10,00037.1 ± 0.510.66 ± 0.2997.4 ± 5.0
CC1122732.99 ± 0.1785.9 ± 2.9>10,000NR>10,000NR>10,000NR29.32 ± 1.9869.8 ± 5.0
CC10840370.20 ± 0.0185.3 ± 1.6>10,000NR2414 ± 74941.0 ± 13.0>10,000NR3.02 ± 0.1686.5 ± 6.8
RP101124>10,000NR>10,000NR>10,000NR>10,000NR>10,000NR
RP1010750.35 ± 0.0185.6 ± 1.9>10,00036.8 ± 2.1>10,000NR1801 ± 31754.1 ± 4.34.49 ± 0.6774.8 ± 6.4
RP1019880.33 ± 0.0185.8 ± 3.8>10,000NR2773 ± 37944.2 ± 9.0>10,00021.2 ± 1.329.15 ± 1.2579.9 ± 5.3
RP1014423.30 ± 0.2587.0 ± 2.9>10,000NR>10,000NR>10,000NR44.77 ± 5.1069.0 ± 6.8
RP1122899.28 ± 0.7968.2 ± 1.8>10,000NR>10,000NR>10,000NR43.51 ± 3.6638.4 ± 2.0
RP11250910.51 ± 1.5387.6 ± 0.9>10,000NR>10,000NR>10,000NR68.98 ± 5.6754.2 ± 1.4
  • IA, intrinsic activity; NR, no response (mean %Emax <20%, where Emax is the maximal response achieved relative to the internal positive control, sphingosine 1-phosphate).