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. Author manuscript; available in PMC: 2010 Oct 28.
Published in final edited form as: J Med Chem. 2008 Jul 8;51(15):4708–4714. doi: 10.1021/jm800422v

Table 1.

IC50 Values of Substituted Indole Inhibitors against Human and Mouse sPLA2sa

graphic file with name nihms241734t1.jpg
IC50(nM)
comp R1 R2 hGIB mGIB hGIIA mGIIA hGIIDc mGIID hGIIE mGIIE hGIIF mGIIF hGV mGV hGX mGX
1b graphic file with name nihms241734t2.jpg graphic file with name nihms241734t3.jpg 750±150 140±75 125±20 70±20 60±10 430±90 50±20 75±20 130±30 >1600 500±50 750±100 75±10 75±10
11c graphic file with name nihms241734t4.jpg graphic file with name nihms241734t5.jpg >1600 950±80 250±20 60±10 170±30 890±45 7±1 12±2 1100±60 >1600 100±20 60±7 15±3 30±7
11d graphic file with name nihms241734t6.jpg graphic file with name nihms241734t7.jpg >1600 >1600 >1600 >1600 700±230 >1600 >1600 >1600 >1600 >1600 >1600 >1600 21±7 >1600
12a graphic file with name nihms241734t8.jpg graphic file with name nihms241734t9.jpg 80±20 100±30 170±40 60±10 120±40 >1600 9±4 140±50 90±30 470±190 44±9 57±20 22±2 20±5
12b graphic file with name nihms241734t10.jpg graphic file with name nihms241734t11.jpg >1600 580±10 >1600 >1600 500±90 >1600 1300±18 >1600 550±100 >1600 >1600 >1600 50±16 >1600
a

IC50 values are reported as the mean of duplicate or triplicate analysis with standard deviations. Each compound was screened at 1660 nM and reported as >1600 nM if the inhibition was <50%.

b

IC50 values for GIB, GIIA, GIIE, GV, and GX from ref 17. Retest of this compound against hGV and mGV gave 110 ± 30 and 160 ± 20 nM, respectively.

c

IC50 values obtained using E. coli membrane assay. Each compound was screened at 1330 nM and reported as >1300 nM if the inhibition was <50%.