sarscov2in10

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-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-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-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.

SARS-CoV-2-IN-105 (Compound 4a) is an inhibitor of SARS-CoV-2, with an EC50 value of 0.69 μM.