%0 Journal Article %T Identification of SARS-CoV-2 entry inhibitors among already approved drugs %A Yang Li %A Pei Rong-juan %A Li Heng %A Ma Xin-na %A Zhou Yu %A Zhu Feng-hua %A He Pei-lan %A Tang Wei %A Zhang Ye-cheng %A Xiong Jin %A Xiao Shu-qi %A Tong Xian-kun %A Zhang Bo %A Zuo Jian-ping %J Acta Pharmacologica Sinica %D 2021 %B 2021 %9 %! Identification of SARS-CoV-2 entry inhibitors among already approved drugs %K %X 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. %U http://www.chinaphar.com/article/view/10376 %V 42 %N 8 %P 1347-1353 %@ 1745-7254