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, demonstrating 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. SARS-CoV-2-IN-11 holds significant promise in the development of specific antivirals against SARS-CoV-2.

SARS-CoV-2-IN-110 (compound Bb1) 是一种SARS-CoV-2抑制剂，对SARS-CoV-2 具有抗病毒活性，EC50为1.10 μM，与Lapatinib相比，毒性明显降低。其对SARS-CoV-2的CC50超过100 μM，选择性指数 (SI) 大于91。

SARS-CoV-2 Mpro-IN-31（Compound 18）作为SARS-CoV-2 MPro的有效抑制剂，展示了11 nM的IC50值。此外，该化合物对半胱氨酸蛋白酶cathepsin B与cathepsin L也显示出强效抑制作用，其IC50值分别达到24 nM和1.8 nM。

Mpro inhibitor N3 hemihydrate is a potent inhibitor of SARS-CoV-2 Mpro with an EC50 of 16.77 μM for SARS-CoV-2. Mpro inhibitor N3 hemihydrate specifically inhibits Mpro from multiple coronaviruses, including SARS-CoV and MERS-CoV. Mpro inhibitor N3 hemihydrate displays inhibition against HCoV-229E, FIPV, and MHV-A59 with individual IC50 of 4.0 μM, 8.8 μM, and 2.7 μM, respectively[1][2]. Mpro inhibitor N3 hemihydrate (0-0.64 μM) is able to penetrate cells to inhibit the replication of IBV viruses, probably at the beginning of infection in embryos[3]. [1]. Jin Z, et al. Structure of Mpro from SARS-CoV-2 and discovery of its inhibitors. Nature. 2020;582(7811):289-293.[2]. Yang H, et al. Design of wide-spectrum inhibitors targeting coronavirus main proteases [published correction appears in PLoS Biol. 2005 Nov;3(11):e428]. PLoS Biol. 2005;3(10):e324.[3]. Wang F, et al. Structure of Main Protease from Human Coronavirus NL63: Insights for Wide Spectrum Anti-Coronavirus Drug Design. Sci Rep. 2016;6:22677. Published 2016 Mar 7.

SARS-CoV-2-IN-15 (compound 11) 是一种氯硝柳胺类似物，其在人血浆和肝 S9 酶测定中比氯硝柳胺具有更高的稳定性。当口服给药时，它可以提高生物利用度和半衰期。SARS-CoV-2-IN-15 是SARS-CoV-2的有效抑制剂，IC50值为 0.49 μM。

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 3CLpro-IN-11(11d)为一种针对SARS-CoV-2 3CL蛋白酶的有效抑制剂，具备IC50值140 nM，并对SARS-CoV-1和MERS-CoV分别展现出IC50值240 nM与70 nM的抑制活性，显示出其广谱的抗病毒能力。

Bamlanivimab (Anti-Human SARS-CoV-2) 是一种针对COVID-19的单克隆抗体(mAb)，于2020年11月获得美国食品药品监督管理局(FDA)的紧急使用授权(EUA)。然而，由于SARS-CoV-2病毒耐药性变体的增多，该授权于2021年4月被撤销。

SARS-CoV-2-IN-92 (compound 11) 以0.48 μM的EC50值抑制SARS-CoV-2变种,同样有效对抗SARS-CoV和MERS-CoV.此外,该化合物还能强效且选择性地阻断ERα-Glu II.