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• W2899207006 abstract "This letter describes the first account of the chemical optimization (SAR and DMPK profiling) of a new series of mGlu4 positive allosteric modulators (PAMs), leading to the identification of VU0652957 (VU2957, Valiglurax), a compound profiled as a preclinical development candidate. Here, we detail the challenges faced in allosteric modulator programs (e.g., steep SAR, as well as subtle structural changes affecting overall physiochemical/DMPK properties and CNS penetration)." @default.
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• W2899207006 date "2019-01-01" @default.
• W2899207006 modified "2023-09-26" @default.
• W2899207006 title "The discovery of VU0652957 (VU2957, Valiglurax): SAR and DMPK challenges en route to an mGlu4 PAM development candidate" @default.
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• W2899207006 doi "https://doi.org/10.1016/j.bmcl.2018.10.050" @default.
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