Avoralstat
A benzanilide.
General information
Avoralstat is an experimental drug for the treatment of angioedema (DrugBank).
Avoralstat on PubChem
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Supporting references
| Link | Tested on | Impact factor | Notes | Publication date |
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Structure-based phylogeny identifies Avoralstat as a TMPRSS2 inhibitor that prevents SARS-CoV-2 infection in mice
Small molecule Enzyme assay Peptide Animal model In vitro In silico |
in silico; in vitro enzyme assay; Calu-3 2B4 cells; hACE2-BALB/c mice; (VSV) SARS-CoV-2 Spike pseudovirus; SARS-CoV-2 live virus | 11.86 | Avoralstat inhibited TMPRSS2 in vitro with an IC50 of ca. 2.73 nM. It inhibited pseudoviral entry in Calu-3 cells with an EC50 of ca. 2.8 μM. The compound significantly reduced viral replication in cell culture (more than a ten-fold decrease in viral RNA signal with a 1 μM dose). It significantly reduced lung viral loads in mice after a viral challenge. It also prevented mice from infection-related weight loss. |
Apr/12/2021 |
AI-suggested references
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In silico and in vitro assays reveal potential inhibitors against 3CLpro main protease of SARS-CoV-2.
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Sep/22/2021 |
