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. 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 1.

Initial SAR for mGlu4 PAM VU0219493

graphic file with name nihms334744u1.jpg
Compd R hmGlu4 EC50 (μM)a Efficacy %PHCCC
2a graphic file with name nihms334744t1.jpg 1.4 ± 0.4 79.0 ± 3.1
2b graphic file with name nihms334744t2.jpg Inactive 12.1 ± 3.1
2c graphic file with name nihms334744t3.jpg Inactive 12.2 ± 4.7
2d graphic file with name nihms334744t4.jpg 4.6 ± 1.4 81.9 ± 2.7
2e graphic file with name nihms334744t5.jpg Antagonistb(IC50 = 7.8) %Inhibition 74.4
a

Potentiation EC50 and efficacy (% PHCCC) are the average of at least three independent determinations performed in triplicate (mean ± SEM shown in table). The maximal response generated in mGlu4 CHO cells in the presence of mGlu4 PAMs varies slightly in each experiment; therefore, PAM data are normalized to a control PAM, PHCCC, response obtained in each day’s run.

b

For 2e, potency and efficacy (% inhibition) data are for blockade of an EC80 glutamate response.