. Author manuscript; available in PMC: 2012 Dec 1.

Published in final edited form as: Bioorg Med Chem Lett. 2011 Oct 8;21(23):6955–6959. doi: 10.1016/j.bmcl.2011.09.131

Table 3.

SAR of substituted pyridine compounds


Compd	R-X	hmGlu₄ IC₅₀ (μM)^a	% Inhibition
2e	cl	8.2 ± 0.4	63.1 ± 6.6
4a		Inactive	−5.4 ± 6.1
4b		Inactive	−7.3 ± 3.9
4c		Inactive	−7.2 ± 4.8
4d		Inactive	−7.2 ± 2.3
4e		Inactive	−9.9 ± 4.9
4f		Inactive	−2.9 ± 5.8
4g		Inactive	−15.8 ± 6.1
4h		Inactive	2.2 ± 6.0
4i		>10	25.5 ± 9.2
4j		Inactive	−4.8 ± 3.0
4k		Inactive	0.9 ± 5.4
4l		Inactive	14.0 ± 15.5
4m		Inactive	4.3 ± 13.9

Antagonist activity at mGlu4 is assessed by measuring the ability of a compound to concentration-dependently inhibit an EC₈₀ glutamate response. IC₅₀ and % inhibition values are the average of at least three independent determinations performed in triplicate (mean ± SEM shown in table). Compounds were ranked as active if they inhibited the EC₈₀ response by at least 20%.