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. Author manuscript; available in PMC: 2014 Nov 14.
Published in final edited form as: J Med Chem. 2013 Oct 23;56(21):8257–8269. doi: 10.1021/jm400898x

Table 2.

Activity of biphenyl derivatives of 2-benzyl Pip-1,2,3-TUs.

graphic file with name nihms534552u2.jpg
Structure Compound DAGLβ % Inhibition (100 nM) Off-targets (10 μM)
4-OCF3 20 38.1 KIAA1363, ABHD6, PLA2G7
3,4-dioxole 21 17.8 FAAH, ABHD6
3-EtOH 22 11.4 ABHD6
4-piperidineamide 23 9.8 ABHD6
4-CF3 24 31.1 FAAH, KIAA1363, ABHD6,PLA2G7
3-CF3 25 44.4 FAAH, ABHD6
2-CF3 26 59 ABHD6
2-OMe 27 (KT172) 55.3 MGLL, ABHD6
2-OCF3 28 59 MGLL, ABHD6, PLA2G7
2-EtOH 29 67 FAAH, MGLL, ABHD6
2-Cl 30 66.2 ABHD6, PLA2G7, ABHD11
2-Me 31 63.2 ABHD6, PLA2G7, ABHD11
HHS Vulnerability Disclosure