Focused Pseudostatic Hydrazone Libraries Screened by Mass Spectrometry Binding Assay: Optimizing Affinities toward γ-Aminobutyric Acid Transporter 1

M Sindelar, TA Lutz, M Petrera…

Index: Sindelar, Miriam; Lutz, Toni A.; Petrera, Marilena; Wanner, Klaus T. Journal of Medicinal Chemistry, 2013 , vol. 56, # 3 p. 1323 - 1340

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Citation Number: 23

Abstract

Mass spectrometric (MS) binding assays, a powerful tool to determine affinities of single drug candidates toward chosen targets, were recently demonstrated to be suitable for the screening of compound libraries generated with reactions of dynamic combinatorial chemistry when rendering libraries pseudostatic. Screening of small hydrazone libraries targeting γ-aminobutyric acid transporter 1 (GAT1), the most abundant γ-aminobutyric acid ...