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. Author manuscript; available in PMC: 2012 Nov 15.
Published in final edited form as: Bioorg Med Chem Lett. 2011 Sep 20;21(22):6739–6745. doi: 10.1016/j.bmcl.2011.09.049

Table 1. S1P4–R agonist activity of compounds 15a-15n (EC50 nM).

cpd R2 R1 X EC50 (nm)α
15a NMe H S 3600
15b NH H S NA
15c NPh Me S 2800
15d NPh H S NA
15e N(pyridin-2-yl) H S 2100 (70%) β
15f O Me S NA
15g NEt Et S 250
15h NCH2CH2OH Me S 306
15i NMe Me O NA
15j NCH2CH2CH2 S NA
15k NCH2CH2 S NA
15l NiPr iPr S NA
15m NnPr nPr S NA
15n NnBu nBu S NA
α

Data are reported as mean of n = 3 determinations.

β

Percentage of response.

NA = not active at concentrations up to 25 μM.