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• W2088780980 abstract "This Letter describes the synthesis and SAR of two mGluR4 positive allosteric modulator leads, 6 and 7. VU001171 (6) represents the most potent (EC(50)=650 nM), efficacious (141% Glu Max) and largest fold shift (36-fold) of any mGluR4 PAM reported to date. However, this work highlights the challenges in hit-to-lead for mGluR4 PAMs, with multiple confirmed HTS hits displaying little or no tractable SAR." @default.
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• W2088780980 date "2009-02-01" @default.
• W2088780980 modified "2023-09-25" @default.
• W2088780980 title "Positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4). Part II: Challenges in hit-to-lead" @default.
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• W2088780980 doi "https://doi.org/10.1016/j.bmcl.2008.11.104" @default.
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