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

Table 2. SAR of 6-Benzyl-Substituted Bicyclic Coresa.

graphic file with name ml-2010-00228m_0004.jpg

compd W X Y Z hS1P1 RI EC50 (μM) (% efficacy) hS1P3 Ca2+ EC50 (μM) (% efficacy)
9 O C CH C 0.013 (110) 0.679 (42)
10 O C N C 0.094 (108) 0.542 (87)
11 N C S C 0.042 (102) 1.21 (24)
12 N C CH N 0.741 (110) 6.09 (50)
13 N N CH C 1.81 (100) 2.71 (48)
a

Data represent an average of at least two determinations. Percent efficacy is reported as in Table 1.