sars-cov-2-in-10

SARS-CoV-2-IN-10 is a powerful and non-toxic inhibitor of SARS-CoV-2 3CL protease, with IC50 and EC50 values of 0.13 nM and 1.03 nM, respectively. The SARS-CoV-2 3C-like protease (3CLpro) is critical for viral replication and serves as an ideal target for intervention. By targeting the SARS-CoV-2 3CL protease, SARS-CoV-2-IN-10 has the potential to facilitate the development of effective antiviral drugs specific to SARS-CoV-2.

SARS-CoV-2 3CLpro-IN-10(5d) is a potent inhibitor of the SARS-CoV-2 3CL protease with an IC50 value of 190 nM and demonstrates broad-spectrum antiviral activity, exhibiting IC50 values of 790 nM for SARS-CoV-1 and 70 nM for MERS-CoV.

SARS-CoV-2 Mpro-IN-10 (27h) is a potent inhibitor of the Mpro enzyme, with IC50 and EC50 values of 10.9 nM and 43.6 nM, respectively. It is used in research on the SARS-CoV-2 virus [1].

SARS-CoV-2-IN-101 (compound 10O) is an effective orally active inhibitor of SARS-CoV-2 with an EC50 value of 0.64 µM against HCoV-229E. This compound exhibits cytotoxicity and can reduce the expression levels of HCoV-229E N protein and RNA. Additionally, SARS-CoV-2-IN-101 has broad-spectrum antiviral activity against coronaviruses.

SARS-CoV-2-IN-102 (example 58) is an inhibitor of the SARS-CoV papain-like protease (SARS-CoVPLpro), demonstrating an IC50 of less than 100 nM.

SARS-CoV-2-IN-106 (compound 19) is a SARS-CoV-2 papain-like protease inhibitor, displaying IC50 values of 0.44 μM for papain-like proteases and 0.18 μM for viral replication.

SARS-CoV-2-IN-100 (Compound 172) is a broad-spectrum antiviral agent against various SARS-CoV-2 variants. It works synergistically with Nirmatrelvir to reduce the risk of antiviral resistance.

SARS-CoV-2-IN-108 (Compound 29) is an inhibitor of SARSCoV-2 papain-like protease, with an IC50 of 0.14 µM. It can inhibit viral replication, displaying an EC50 of 0.21 µM.

SARS-CoV-2-IN-107 (Compound A7) is an inhibitor of SARS-CoV-2 3CLpro, with an IC50 of 261.3 nM. It inhibits the replication of SARS-CoV-2, exhibiting an EC50 of 11.7 μM. Additionally, SARS-CoV-2-IN-107 demonstrates anti-inflammatory activity in LPS-stimulated RAW264.7 macrophages, with a NO inhibition rate of 68.6%.

SARS-CoV-2-IN-109 (compound 50) is an inhibitor targeting SARS-CoV, demonstrating in vivo anti-infection activity. It interferes with the interaction between the SARS-CoV-2 Spike receptor-binding domain (RBD) and the human receptor angiotensin-converting enzyme 2 (ACE2) with an EC50 of 26.5 μM, effectively blocking SARS-CoV-2 entry into VeroE6 cells (ECS50=17.0 μM). The compound has a CC50 greater than 100 μM in VeroE6 cells.

ZG-10 (JNK-IN-2) is an inhibitor of JNK, blocking JNK1, JNK2, and JNK3, and is used in studies of SARS-CoV-2 virus infection.

Hydroxyethylamine (Compd VII) is a SARS-CoV-2 3CLpro inhibitor with an IC50 of ~10 μM in a transmission assay, demonstrating significant antiviral effects.

SARS-CoV-2-IN-96 (compound 12b) acts as an inhibitor for both HCoV-OC43 (EC50= 97 nM) and SARS-CoV-2 (EC50= 45 nM), while displaying low cytotoxicity in Huh7 cells (CC50=10 μM).

SARS-CoV-2-IN-51 (S-10), a lead compound for Omicron fusion inhibition, demonstrates potent activity against Omicron and other SARS-CoV-2 variants, with EC50 values ranging from 0.82-5.45 μM. It functions by directly interacting with the spike (S) protein in the prefusion state [1], thereby preventing viral entry.

SARS-CoV-2 Mpro-IN-7 (compound 6g) effectively inhibits the SARS-CoV-2 main protease (Mpro) with an IC50 value of 8.8 μM and exhibits a cytotoxic concentration (CC50) of 10 μM [1].

FASN-IN-4 tosylate is a potent fatty acid synthase (FASN) inhibitor with an IC50 of 10 nM and also exhibits inhibitory activity against SARS-CoV-2, with an EC50 of 18.6 nM [2].

SARS-CoV-2-IN-95 (Compound 10) acts as an inhibitor of SARS-CoV-2 PLpro, with an IC50 of 0.39 μM. It demonstrates antiviral activity in a murine SARS-CoV-2 infection model.

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].

Hydroxyaloin A (10-10-Hydroxyaloin A) is a potent inhibitor of SARS-CoV-2, demonstrating significant efficacy in binding to the active site of the SARS-CoV-2 main protease (M^pro) [1].

SARS-CoV-2 nsp14-IN-1 (Compound 3) is a dual-substrate inhibitor of SARS-CoV-2 Nsp14 Mtase with an IC50 of 0.061 μM, targeting substrates such as histone lysine, protein arginine, DNA, and RNA.