TY - JOUR AU - Yang Li AU - Pei Rong-juan AU - Li Heng AU - Ma Xin-na AU - Zhou Yu AU - Zhu Feng-hua AU - He Pei-lan AU - Tang Wei AU - Zhang Ye-cheng AU - Xiong Jin AU - Xiao Shu-qi AU - Tong Xian-kun AU - Zhang Bo AU - Zuo Jian-ping PY - 2021 TI - Identification of SARS-CoV-2 entry inhibitors among already approved drugs JF - Acta Pharmacologica Sinica; Vol 42, No 8 (August 2021): Acta Pharmacologica Sinica Y2 - 2021 KW - N2 - To discover effective drugs for COVID-19 treatment amongst already clinically approved drugs, we developed a high throughput screening assay for SARS-CoV-2 virus entry inhibitors using SARS2-S pseudotyped virus. An approved drug library of 1800 small molecular drugs was screened for SARS2 entry inhibitors and 15 active drugs were identified as specific SARS2-S pseudovirus entry inhibitors. Antiviral tests using native SARS-CoV-2 virus in Vero E6 cells confirmed that 7 of these drugs (clemastine, amiodarone, trimeprazine, bosutinib, toremifene, flupenthixol, and azelastine) significantly inhibited SARS2 replication, reducing supernatant viral RNA load with a promising level of activity. Three of the drugs were classified as histamine receptor antagonists with clemastine showing the strongest anti-SARS2 activity (EC50 = 0.95 ± 0.83 μM). Our work suggests that these 7 drugs could enter into further in vivo studies and clinical investigations for COVID-19 treatment. UR - http://www.chinaphar.com/article/view/10376