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. 2015 Dec 19;7(2):198–203. doi: 10.1021/acsmedchemlett.5b00463

Table 3. SAR of Substitutions on the Piperidine Ring.

graphic file with name ml-2015-004636_0011.jpg

compd R1,R2 BTK enzymatic assaya IC50 (nM) hPBMC assaya IC50 (nM)
1 H, H 0.27 8.0
37 F, Me 0.17 3.0
38 H, CF2H 0.86 20
39 H, MeOCH2 0.31 4.0
40 F, CF3 3.7 ND
a

The data are average of at least two repeated tests. ND: not determined.