TABLE 1

Activity of compounds on human S1P receptors

Compounds were tested in [33P]S1P binding assays to determine IC50 values and [35S]GTPγS binding assays to determine EC50 values using membranes prepared from CHO cells expressing human S1P receptors. Values are the mean of two to six measurements performed in duplicate. S1P is subject to extensive metabolism under standard [35S]GTPγS binding assay conditions, and EC50 values are not shown.




S1P

A

C

D

E

F
nM
S1P1
IC50 0.5 0.3 3.2 0.9 2.4 12.0
EC50 ND 0.3 2.9 1.2 1.9 12.8
S1P2
IC50 0.3 >1000 >1000 >1000 >1000 >1000
EC50 ND >1000 >1000 >1000 >1000 >1000
S1P3
IC50 0.2 5.0 125 7.9 1424 9265
EC50 ND 3.0 109 7.3 1145 >10,000
S1P4
IC50 55 5.9 160 114 77 380
EC50 ND 4.3 45 ND 83 ND
S1P5
IC50 0.5 0.6 108 5.0 7.5 6.8
EC50
ND
1.0
171
1.3
4.4
5.6
  • ND, not determined.