. Author manuscript; available in PMC: 2016 Jan 15.

Published in final edited form as: Bioorg Med Chem Lett. 2014 Nov 29;25(2):225–228. doi: 10.1016/j.bmcl.2014.11.066

Table 2.

Inhibitions of [³H]TCP binding at the PCP site of the NMDA receptor (%), binding affinities (K_i), and clogD values for N-aryl-N’-(3-methylthiophenyl)-N’-methylguanidines.


Ligand	R	Inhibition (%)^a	[³H]TCP K_i (nM)^b	cLogD^c
3		3.4		1.86
4		25.3		2.00
5		80.7	>1000	1.92
6		91.2	110	1.82
7		73.8		2.04
8		72.2		2.40
9		91.7	540	2.51
10		8.6		2.31
11		14.4		2.69
12		69.7		2.92
13		23.7		1.87

At 1.0 μM concentration. Mean from two experiments.

Binding affinities were measured for compounds whose inhibitions were ≥ 80%. Mean from two experiments.

Calculated with ACD Labs program.