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. Author manuscript; available in PMC: 2015 Dec 15.
Published in final edited form as: Medchemcomm. 2014 Dec 1;5(12):1879–1886. doi: 10.1039/C4MD00291A

Table 4.

Inhibitory effect of the substituted 4-piperidine series in seven JmjC KDMs

Compound
 pIC50a KDM
21 R 2A 3A 4A 4C 4E 5C 6B
21a Et 5.2 ± 0.14 (2) 4.3 ± 0.13 (2) ND 4.8 ± 0.42 (2) <4.0 (2) 5.3 ± 0.11 (2) 4.2 ± 0.11 (2)
21b nPr 5.1 ± 0.14 (2) <4.0 (2) ND 4.8 ± 0.19 (2) <4.0 (2) 5.2 ± 0.07 (2) <4.0 (2)
21c Ph 5.1 ± 0.13 (2) <4.0 (2) 4.3 ± 0.29 (4) 5.0 ± 0.18 (4) <4.0 (2) 5.4 ± 0.02 (2) 4.4 ± 0.26 (2)
21d Bn 5.4 ± 0.11 (2) 4.5 ± 0.19 (2) 4.4 ± 0.30 (2) 4.5 ± 0.19 (2) <4.0 (2) 5.4 ± 0.06 (2) 4.8 ± 0.09 (2)
21e graphic file with name emss-66085-t0014.jpg 5.6 ± 0.09 (4) <4.0 (2) 4.1 ± 0.18 (2) 4.1 ± 0.15 (2) <4.0 (2) 5.5 ± 0.06 (2) <4.0 (2)
a

Mean pIC50 ± standard error of the mean (number of determinations) as determined by AlphaScreen.