Selected article for: "calpain protease and protease inhibitor"
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_28
    Snippet: In an effort to assess robustness and reproducibility of the optimized assay in a high-throughput screening (HTS) configuration, we initially evaluated the assay utilizing Duplicates of each plate were run in parallel and the value corresponding to each well was normalized to the median of each plate and used to calculate the log base 2 of the fold change (Log2FC). Based on the activity of APY0201, the average Zʹ factor for the 5 plates in dupli.....
    Document: In an effort to assess robustness and reproducibility of the optimized assay in a high-throughput screening (HTS) configuration, we initially evaluated the assay utilizing Duplicates of each plate were run in parallel and the value corresponding to each well was normalized to the median of each plate and used to calculate the log base 2 of the fold change (Log2FC). Based on the activity of APY0201, the average Zʹ factor for the 5 plates in duplicate was 0.4, and the correlation coefficient for the duplicates (R 2 ) was 0.81 ( Figure 1B) , although an usual distribution of the positive controls in the correlation plot was observed. Twenty-eight compounds were selected for further study based on activities in both screens. These included the HIV protease inhibitor nelfinavir mesylate hydrate, the calpain and cathepsin B inhibitor MDL28170 and the antagonist of the serotonin receptors 5-HT1B and 5-HT1D GR 127935 hydrochloride hydrate, which have author/funder. All rights reserved. No reuse allowed without permission.

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