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. Author manuscript; available in PMC: 2022 Jan 12.
Published in final edited form as: ACS Chem Neurosci. 2019 Oct 28;10(11):4558–4570. doi: 10.1021/acschemneuro.9b00415

Table 4.

Summary of Lipophilic Ligand Efficiency (LLE) Values of Tested mGlu5 NAMs in mGlu5/HEK Cells and Striatal, Hippocampal, and Cortical Culturesa

LLE
mGlu5 HEK striatal hippocampal cortical
MPEP 4.22 2.80 4.23 3.77
Fenobam 5.50 2.38 3.20 2.94
AFQ056 4.57 1.88 3.44 3.42
RG7090 4.59 4.06 4.90 3.95
AZD2066 4.29 2.30 3.87 3.27
a

LLE = pIC50 − log P.4246 Consensus log Po/w of each drug listed in Table 1 and IC50 listed on Table 3 were used to calculate the LLE for each NAM.