Author: Laura Riva; Shuofeng Yuan; Xin Yin; Laura Martin-Sancho; Naoko Matsunaga; Sebastian Burgstaller-Muehlbacher; Lars Pache; Paul P. De Jesus; Mitchell V. Hull; Max Chang; Jasper Fuk-Woo Chan; Jianli Cao; Vincent Kwok-Man Poon; Kristina Herbert; Tu-Trinh Nguyen; Yuan Pu; Courtney Nguyen; Andrey Rubanov; Luis Martinez-Sobrido; Wen-Chun Liu; Lisa Miorin; Kris M. White; Jeffrey R. Johnson; Christopher Benner; Ren Sun; Peter G. Schultz; Andrew Su; Adolfo Garcia-Sastre; Arnab K. Chatterjee; Kwok-Yung Yuen; Sumit K. Chanda
Title: A Large-scale Drug Repositioning Survey for SARS-CoV-2 Antivirals Document date: 2020_4_17
ID: 1fgnfh62_60
Snippet: Among the 17 compounds validated to show a dose-response relationship in our orthogonal assay, 10 compounds harbored EC 50 antiviral activities >750 nM, suggesting that additional preclinical studies will likely be required to determine whether administration of these compounds can achieve sufficient systemic exposure to enable antiviral activity (Figure S5) . Seven molecules were found to inhibit viral replication at EC 50 concentration <500 nM......
Document: Among the 17 compounds validated to show a dose-response relationship in our orthogonal assay, 10 compounds harbored EC 50 antiviral activities >750 nM, suggesting that additional preclinical studies will likely be required to determine whether administration of these compounds can achieve sufficient systemic exposure to enable antiviral activity (Figure S5) . Seven molecules were found to inhibit viral replication at EC 50 concentration <500 nM. These include Z LVG CHN2, a preclinical tripeptide derivative that displays a broad-spectrum bactericidal activity. Specifically, this molecule has been previously shown to suppress herpes simplex virus (HSV) replication by inhibiting the enzymatic activity of HSV-encoded cysteine protease 68 , which may indicate that the antiviral function of Z LVG CHN2 occurs through inhibition of SARS-COV-2 3CLpro protease. Another preclinical molecule that exhibits strong antiviral activity, MDL 28170, is a potent cell permeable calpain I and II inhibitor. Interestingly, MDL 28170 was previously found to impair infection by SARS-COV-1 and Ebola virus (EBOV) 50, 69 . Additionally, astemizole a registered anti-histamine H1 receptor antagonist author/funder. All rights reserved. No reuse allowed without permission.
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