sars cov-1 3clpro

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].

Atazanavir (BMS-232632)(BMS-232632) is an highly effective HIV-1 protease inhibitor.

Ritonavir (ABT 538) is a peptidomimetic agent that inhibits both HIV-1 and HIV-2 proteases. Ritonavir is highly inhibited by serum proteins but boosts the effect of other HIV proteases by blocking their degradation by cytochrome P450.

Lopinavir (ABT-378) is a peptidomimetic HIV protease inhibitor effective against HIV protease with the Val 82 mutation. It is less affected by serum protein binding compared to the structurally related drug ritonavir.

Velpatasvir (GS-5816), also known as GS-5816, is a potent and selective Hepatitis C virus NS5A inhibitor. GS-5816 has demonstrated pan-genotypic activity and a high barrier to resistance in HCV replicon assays. GS-5816 demonstrated pangenotypic antiviral activity in patients with genotype 1-4 HCV infection. It will be further evaluated in combination with other pangenotypic direct-acting antivirals to achieve the goal of developing a well-tolerated, highly effective treatment for all HCV genotypes.

Glecaprevir (ABT-493) is an HCV NS3 4A protease inhibitor, (IC50s: 3.5-11.3 nM).

Telaprevir (Incivek) (VX-950) is an effective inhibitor of HCV NS3-4A serine protease (IC50: 0.35 μM).

Paritaprevir (ABT450) is an inhibitor of non-structural protein 3 4A protease with EC50 values of 1 and 0.21 nM for HCV 1a and HCV 1b, respectively.

Tipranavir is a protease inhibitor that inhibits HIV-1 resistant to more than 1 protease inhibitor .Tipranavir effectively inhibits HIV-1 protease enzyme activity and dimerisation and has potent activity against multiple protease inhibitor (PI) HIV-1 isolates (IC50 of 66-410 nM). Tipranavir inhibits SARS-CoV-2 3CLpro activity.

Indinavir sulfate (L735524 sulfate) is a HIV protease inhibitor.It inhibits the HIV-1 protease with an IC50 value of 0.41 nM and Ki value of 0.24 nM.

CCF0058981 (CCF981) is a 3-chlorophenyl analogue, serving as a noncovalent inhibitor of SARS-CoV-2 3CL pro (SC2), demonstrating potent activity with an IC50 of 68 nM. It also exhibits inhibitory effects against SARS-CoV-1 3CL pro (SC1) with an IC50 of 19 nM, highlighting its antiviral efficacy and potential in COVID-19 research [1].

3CPLro-IN-1 (compound A17) is a potent, orally active inhibitor of SARS-CoV-2 3-Chymotrypsin-like cysteine protease (3CLpro) with an IC50 of 5.65 μM, making it an attractive drug target against COVID-19 and also considered an antitumor agent-51.

INSCoV-600K(1) is a potent Mpro(3CLpro) inhibitor, with research potential against SARS-CoV-2 infection. Proteases (PLpro and 3CLpro) are associated with viral transcription and replication.

INSCoV-601I(1) is a potent Mpro(3CLpro) inhibitor linked to viral transcription and replication through proteases (PLpro and 3CLpro). This compound has demonstrated research potential against SARS-CoV-2 infection.

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-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-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].

Antiviral agent 25 (compound 6g), a novel non-peptide analog covalent inhibitor of SARS-CoV-2 3CL pro, exhibits robust inhibitory activity against both SARS-CoV-2 3CL pro and SARS-CoV-2 PL pro, with IC50 values of 0.118 µM and 0.448 µM, respectively. Furthermore, it demonstrates significant antiviral effects against SARS-CoV-2, achieving an EC50 value of 7.249 µM [1].

SARS-CoV-2-IN-41 (compound 2) is a potent SARS-CoV-2 3CL protease inhibitor with an IC50 of 0.022 µM, demonstrating significant antiviral efficacy [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].

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-18 (Compound 3C) is a covalent inhibitor of SARS-CoV-2 3CLpro with an IC50 of 0.478 μM. It inhibits SARS-CoV-2 in Vero E6 cells with an EC50 of 2.499 μM and exhibits low cytotoxicity (CC50 > 200 μM) [1].