sars-cov-2-in-11

SARS-CoV-2-IN-11 is a highly potent and non-toxic inhibitor of the 3C-like protease (3CLpro) of SARS-CoV-2, with IC50 and EC50 values of 0.17 nM and 1.45 nM, respectively. This compound targets the essential viral replication enzyme (3CLpro), making it an attractive candidate for intervention strategies and holds significant promise in the development of specific antivirals against SARS-CoV-2.

SARS-CoV-2 3CLpro-IN-11(11d) is a broad-spectrum antiviral compound that inhibits the SARS-CoV-2 3CL protease with an IC50 of 140 nM, and also exhibits inhibitory activity against SARS-CoV-1 and MERS-CoV with IC50 values of 240 nM and 70 nM, respectively.

SARS-CoV-2-IN-110 (compound Bb1) is an inhibitor of SARS-CoV-2, demonstrating antiviral efficacy with an EC50 of 1.10 μM, and significantly reduced toxicity compared to Lapatinib. The compound exhibits a CC50 of greater than 100 μM against SARS-CoV-2, with a selectivity index (SI) exceeding 91.

SARS-CoV-2-IN-92 (compound 11) effectively inhibits variants of SARS-CoV-2 (EC50= 0.48 μM), as well as SARS-CoV and MERS-CoV. Additionally, this compound robustly and selectively blocks ERα-Glu II.

SARS-CoV-2-IN-15 (compound 11) is a niclosamide analogue exhibiting greater stability in human plasma and liver S9 enzyme assays compared to niclosamide. It enhances bioavailability and half-life upon oral administration and is a potent SARS-CoV-2 inhibitor with an IC50 of 0.49 μM [1].

Covidcil-19 binds to the revised attenuator hairpin structure of the SARS-CoV-2 frameshifting element (FSE) with high affinity (Kd = 11 nM). It stabilizes the hairpin's folded state and reduces frameshifting efficiency in cells. Covidcil-19 inhibits viral propagation and reduces viral infectivity by > 3.5 orders of magnitude.

SARS-CoV-2 Mpro-IN-31 (Compound 18) is an inhibitor of SARS-CoV-2 MPro with an IC50 of 11 nM. Additionally, this compound effectively inhibits the enzymatic activity of the cysteine proteases cathepsin B and cathepsin L, with IC50 values of 24 nM and 1.8 nM, respectively.

Bamlanivimab, an Anti-Human SARS-CoV-2 monoclonal antibody (mAb), was the first of its kind to receive Emergency Use Authorization (EUA) from the U.S. Food and Drug Administration (FDA) in November 2020 for COVID-19 treatment. However, its authorization was withdrawn in April 2021 due to emerging SARS-CoV-2 variants resistant to the antibody [1].

Mpro inhibitor N3 hemihydrate is a potent antagonist of the SARS-CoV-2 main protease (Mpro), with an EC50 of 16.77 μM against SARS-CoV-2. It specifically inhibits Mpro in various coronaviruses, including SARS-CoV, MERS-CoV, HCoV-229E (IC50 4.0 μM), FIPV (IC50 8.8 μM), and MHV-A59 (IC50 2.7 μM) [1][2].