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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 1.

Comparison of activity of (2-benzyl)-Pip-heterocyclic urea derivatives.

graphic file with name nihms534552u1.jpg
Structure Compound DAGLβ % inhibition (100 nM) Off-targets (10 μM)
X1 = N, X2 = N, R = 4-OCF3 5 52 FAAH, ABHD6, ABHD11, PLA2G7
X1 = N, X2 = C, R = 4-OCF3 8 0 none
X1 = C, X2 = N, R = 4-OCF3 9 0 none
X1 = N, X2 = N, R = 3-5 diF 10 55.4 FAAH, KIAA1363, ABHD6, LYPLA1, LYPLA2, PLA2G7, ABHD11
X1 = N, X2 = N, R = 4-Ph 11 (KT109) 60.8 ABHD6, PLA2G7
X1 = N, X2 = N, R = 3-Ph 14 27.4 FAAH, MGLL, ABHD6, 80 kDa SH, ABHD11
X1 = N, X2 = N, R = 2-Ph 15 17.6 FAAH, MGLL, ABHD6, ABHD11
X1 = N, X2 = N, R = 4-piperidineamide 19 40.9 FAAH, ABHD6, ABHD11
HHS Vulnerability Disclosure