Table 1SAR of the Western Amide Moiety

Image ml128fu2.jpg
SID (CID)REC50 (μM)a (hmGl uR4)Glu Max (h)aLE
85240633 (CID 308065)
Image ml128fu3.jpg
>5135±50.33
85240633 (CID 836051)
Image ml128fu4.jpg
4.1620.32
85240635 (CID 44191097)
Image ml128fu5.jpg
>10
85240636 (CID 869104)
Image ml128fu6.jpg
>10
85240640 (CID 2318321)
Image ml128fu7.jpg
>10
85240641 (CID 44191098)
Image ml128fu8.jpg
>10
85240639 (CID 30268259)
Image ml128fu9.jpg
>10
85240631 (CID 140002)
Image ml128fu10.jpg
>10
85240632 (CID 82516 )
Image ml128fu11.jpg
>10
85240642 (CID 4644726)
Image ml128fu12.jpg
1.4±0.180±90.34
85240637 (CID 871161)
Image ml128fu13.jpg
>10
85240638 (CID 44191099)
Image ml128fu14.jpg
2.8±0.283±100.33
a

EC50 and GluMax are the average of at least three independent determinations performed in triplicate.

From: Discovery of a potent, selective and in vivo active mGluR4 positive allosteric modulator

Cover of Probe Reports from the NIH Molecular Libraries Program
Probe Reports from the NIH Molecular Libraries Program [Internet].

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