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Chem Pharm Bull (Tokyo) ; 70(3): 199-201, 2022 Mar 01.
Article in English | MEDLINE | ID: covidwho-1714684

ABSTRACT

MS is a powerful methodology for chemical screening to directly quantify substrates and products of enzymes, but its low throughput has been an issue. Recently, an acoustic liquid-handling apparatus (Echo®) used for rapid nano-dispensing has been coupled to a high-sensitivity mass spectrometer to create the Echo® MS system, and we applied this system to screening of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) 3CL protease inhibitors. Primary screening of 32033 chemical samples was completed in 12 h. Among the hits showing selective, dose-dependent 3CL-inhibitory activity, 8 compounds showed antiviral activity in cell-based assay.


Subject(s)
COVID-19 , Protease Inhibitors , Acoustics , COVID-19/drug therapy , High-Throughput Screening Assays/methods , Humans , Protease Inhibitors/chemistry , Protease Inhibitors/pharmacology , SARS-CoV-2
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