. 2010 Nov 9;2(2):102–106. doi: 10.1021/ml100228m

Table 1. SAR of 5-Benzyl-Substituted Bicyclic Cores^a.

graphic file with name ml-2010-00228m_0003.jpg

compd	W	X	Y	Z	hS1P₁ RI EC₅₀ (μM) (% efficacy)	hS1P₃ Ca²⁺ EC₅₀ (μM) (% efficacy)
3	O	C	CH	C	0.057 (96)	1.73 (42)
4	O	C	N	C	0.325 (105)	0.354 (77)
5	N	C	S	C	0.221 (84)	3.47 (50)
6	N	C	NH	C	>6.25	>25
7	N	C	CH	N	6.72 (115)	>25
8	N	N	CH	C	2.89 (53)	1.11 (43)

Data represent an average of at least two determinations. Percent efficacy is reported relative to 1.00 μM 9 and 0.200 μM S1P for hS1P₁ RI and hS1P₃ Ca²⁺ assays, respectively. (S1P demonstrates 91% efficacy relative to 1.00 μM 9 in hS1P₁ RI studies.) >[Highest concentration tested] is reported for compounds that do not achieve >10% of control activity (1.00 μM 9 or 0.200 μM S1P).

Table 1. SAR of 5-Benzyl-Substituted Bicyclic Coresa.

Table 1. SAR of 5-Benzyl-Substituted Bicyclic Cores^a.