sars-cov-2 3cl

SARS-CoV-2 3CLpro-IN-16 is a covalent inhibitor of SARS-CoV-2 3CLpro activity, exerting its effect by forming a covalent bond with Cys145.

SARS-CoV-2 3CLpro-IN-20 is a covalent inhibitor of SARS-CoV-2 3CLpro with an IC50 of 0.43 μM and potential antiviral activity.

SARS-CoV-2-IN-14 is a potent and oral inhibitor of SARS-CoV-2 (IC50:0.39 μM), which is an analogue of niclosamide. SARS-CoV-2-IN-14 was more stable than niclosamide in the determination of human plasma and liver S9 enzyme. Oral administration of SARS-CoV-2-IN-14 can improve its bioavailability and half-life.

SARS-CoV-2 3CLpro-IN-30 (compound 29) is a potent inhibitor of the SARS-CoV-2 3CL protease (SARS-CoV-2 3CLpro), with an IC50 of 0.04 μM and an EC50 of 0.3 μM.

SARS-CoV-2 3CLpro-IN-2 is a potent inhibitor of the 3CL protease pair, demonstrating significant research potential for SARS-CoV-2 disease.

SARS-CoV-2 3CLpro-IN-1 (Compound 14c) is a highly potent inhibitor specifically designed to target and inhibit the activity of SARS-CoV-2 3CL pro, a cysteine protease found in the main coronaviruses. This enzyme is a promising target for antiviral drug development, positioning SARS-CoV-2 3CLpro-IN-1 as significant for advancing research in infectious diseases [1].

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 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 3CLpro-IN-6 is a reversible covalent inhibitor of the SARS-CoV-2 3CL protease, showing potent inhibitory activity with an IC50 of 4.9 μM, and is used in the research of coronavirus disease 2019 (COVID-19).

SARS-CoV-2 3CLpro-IN-7 is a reversible covalent inhibitor of the SARS-CoV-2 3CL protease, with an inhibitory concentration (IC50) of 1.4 µM.

SARS-CoV-2 3CLpro-IN-13 is a potent inhibitor of the SARS-CoV-2 3CL protease, exhibiting significant anti-coronavirus activity with an IC50 value of 21 nM [1].

Compound 3h, also known as SARS-CoV-2 3CLpro-IN-17, is a selective inhibitor of the SARS-CoV-2 3CL protease, demonstrating an IC50 of 0.322 μM [1].

SARS-CoV-2 3CLpro-IN-21 (Compound D6) is an irreversible, covalent inhibitor of SARS-CoV-2 3CL pro, demonstrating potent inhibition with an IC50 of 0.03 μM. It also exhibits inhibitory activity against SARS-CoV-1 3CL pro with an IC50 of 0.12 μM [1].

SARS-CoV-2 3CLpro-IN-15 (compound a), a beta-nitrostyrene derivative, inhibits the SARS-CoV-2 3CL protease (3CLpro), thereby suppressing viral replication and transcription. It is instrumental in identifying potential anti-COVID-19 lead compounds [1].

SARS-CoV-2 3CLpro-IN-25 (compound 56) effectively inhibits the SARS-CoV-2 3CLpro enzyme, exhibiting an IC50 value of 70 nM, and demonstrates cellular antiviral activity with an EC50 of 3.1 μM.

SARS-CoV-2 3CLpro-IN-27 (Compound 9H) is an inhibitor of SARS-CoV-2 3CLpro, demonstrating an IC50 of 21 nM. It also exhibits robust anti-replicase activity against SARS-CoV-2, with an EC50 of 5 nM.

SARS-CoV-2 3CLpro-IN-26 (Compound (S,R)-4y) is a conformational inhibitor of SARS-CoV-2 3CLpro with an IC50 of 0.43 μM. It demonstrates good cellular permeability, being able to effectively cross the cell membrane following co-incubation with Vero-E6 cells.

3CLPro-IN-3 (Compound A36) is an inhibitor of SARS-CoV-2 3CLpro with an IC50 value of 51.3 nM. It exhibits antiviral activity against human coronaviruses 229E, OC43, and the murine coronavirus MHV.

SARS-CoV-2 3CLpro-IN-28 (Compound 19) is an inhibitor of SARS-CoV-2 3CLpro, exhibiting an IC50 value of 0.018 μM.

SARS-CoV-2 3CLpro-IN-4 (Compound 5g) is a multifunctional inhibitor of SARS-CoV-2 3CLpro with antiviral, antibacterial, and antifungal properties.

SARS-CoV-2 3CLpro-IN-3, a SARS-CoV-2 3CLpro inhibitor, demonstrates antiviral, antibacterial, and antifungal properties.

SARS-CoV-2 3CLpro-IN-5 is a covalent inhibitor targeting the 3C-like protease (3CLpro), with potent inhibitory activity (IC50: 3.8 nM) and 9.0% oral bioavailability (BA), used in COVID-19 research [1].

SARS-CoV-2 3CLpro-IN-19 (Compound C5a), a non-covalent, non-peptide inhibitor of the SARS-CoV-2 3CLpro enzyme, exhibits potent in vitro activity with an IC50 of 0.7 μM. It demonstrates broad-spectrum efficacy against infection by Omicron subvariants (BA.5, BQ.1.1, and XBB.1.5) in human cells, with EC50 values ranging from 30-69 nM [1].

SARS-CoV-2 3CLpro-IN-14 (compound 11j) is an orally active inhibitor of SARS-CoV-2 3CLpro, demonstrating potent anti-SARS-CoV-2 properties with an EC50 of 0.18 μM and exhibits minimal cytotoxicity, having a CC50 greater than 50 μM, in Vero E6 cells [1].