. 2011 Apr 15;2(8):411–432. doi: 10.1021/cn2000266

Table 4. mGlu₅ Affinity and Potency in the 1,2,4-Triazole and Tetrazole Series.

entry	series	R¹	X	R²	mGlu₅ IC₅₀ (nM)	mGlu₅K_i (nM)	SILE	LELP
49	I	3-Cl	CH₂CH₂	cyclobutyl	1170	204	3.91	3.80
50	I	3-Me	CH₂CH₂	cyclobutyl	490	126	4.26	3.02
51	I	3-OMe	CH₂CH₂	cyclobutyl	501	182	3.93	3.09
52	I	3-Me	CH₂	-CH₂OMe	30 200	186	4.15	1.77
53	I	3-Cl	CH₂	5-methylthiophen-2-yl	6610	123	3.86	5.05
54	I	3-Cl	S	5-methylthiophen-2-yl	759	83	3.79	5.70
55	II	3-Cl	CH₂CH₂	cyclobutyl	338	78	3.96	3.42
56	II	3-Me	CH₂CH₂	cyclobutyl	224	72	4.17	2.87
57	II	3-Cl	CH₂CH₂	5-bromofuran-2-yl	213	48	3.78	4.31
58	II	3-Cl	CH₂	5-methylthiophen-2-yl	251	89	3.78	4.72

Table 4. mGlu5 Affinity and Potency in the 1,2,4-Triazole and Tetrazole Series.