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Matches in SemOpenAlex for { <https://semopenalex.org/work/W2234787003> ?p ?o ?g. }

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• W2234787003 abstract "High throughput screening of our corporate compound library followed by hit-to-lead development resulted in a 4-aryl-3-arylsulfonyl-quinoline derivative lead (2) with mGluR5 negative allosteric modulator activity. During the lead optimization process, our objective was to improve affinity and metabolic stability. Modifications at the three targeted regions of the lead structure resulted in compounds with nanomolar affinity and acceptable metabolic stability. One of the most promising compounds (3), showing excellent in vivo efficacy, was selected for preclinical development and subsequent phase I clinical studies." @default.
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• W2234787003 date "2016-02-01" @default.
• W2234787003 modified "2023-10-18" @default.
• W2234787003 title "4-Aryl-3-arylsulfonyl-quinolines as negative allosteric modulators of metabotropic GluR5 receptors: From HTS hit to development candidate" @default.
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• W2234787003 doi "https://doi.org/10.1016/j.bmcl.2016.01.024" @default.
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