Table 1. Racemic 7-Benzyloxy SAR (human S1P₁, HTRF cAMP).

compd	R1	R2	R3	EC50, nM (%)a
7	CN		OCF3	16.0 (90%)
8	CF3		CF3	26.0 (98%)
9	CN	OCF3		1.7 (109%)
10	CN	OCH3		120 (136%)
11	CF3	CN		141 (104%)
12	CF3	Cl		159 (117%)
13	CN	cyclohexyl		0.087 (98%)
14	CF3	cyclohexyl		0.077 (96%)
15	CF3	cyclopentyl		0.073(104%)
16	CF3	cyclobutyl		0.45 (109%)
17	CF3	cyclopropyl		3.68 (118%)
18	CF3	n-propyl		0.49 (107%)
19	CF3	neopentyl		55.8 (112%)
20	CF3	iso-butyl		0.44 (103%)
21	CF3	methylcyclohexyl		4.58 (111%)

^aEC₅₀ values are the mean of three or more replicates. Value in parentheses is the % agonism relative to S1P. S1P EC₅₀ = 0.062 nM; 2 EC₅₀ = 0.006 nM (101%).