- 著者
- Tsukasa Hasegawa Riyo M. Imamura Tateki Suzuki Takao Hashiguchi Takao Nomura Satoko Otsuguro Katsumi Maenaka Michihito Sasaki Yasuko Orba Hirofumi Sawa Akihiko Sato Takayoshi Okabe Tetsuo Nagano Hirotatsu Kojima
- 出版者
- The Pharmaceutical Society of Japan
- 雑誌
- Chemical and Pharmaceutical Bulletin (ISSN:00092363)
- 巻号頁・発行日
- pp.c21-01003, (Released:2021-12-21)
- 参考文献数
- 10
- 被引用文献数
- 6
Mass spectrometry 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 SARS-CoV-2 3CL protease inhibitors. Primary screening of 32,033 chemical samples was completed in 12 hours. Among the hits showing selective, dose-dependent 3CL-inhibitory activity, 8 compounds showed antiviral activity in cell-based assay.