sars cov in 3

SARS-CoV-IN-3 is an effective inhibitor of SARS-CoV replication.

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 nsp14-IN-3 (4975) is a potent inhibitor of the N7-Methyltransferase activity of SARS-CoV-2 nonstructural protein 14 (Nsp14), with an IC50 value of 3.5 μM [1].

SARS-CoV-2 nsp13-IN-3 (Compound C3) is a small molecule inhibitor of SARS-CoV-2 non-structural protein 13 (nsp13), targeting nsp13 ssDNA+ATPase with an IC50 of 32 μM.

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

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

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].

SARS-CoV-2 nsp3-IN-1 (Compound 15c) exhibits significant selectivity for coronavirus macrodomains, particularly SARS-CoV-2 Mac1, and can inhibit Mac1 ADP-ribosylhydrolase activity with an IC50 of 6.1 μM [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-2 is a potent inhibitor of the 3CL protease pair, demonstrating significant research potential for SARS-CoV-2 disease.

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-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].

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-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 nsp3-IN-2 is a SARS-CoV-2 nsp3 macrodomain (Mac1) inhibitor with an IC50 value of 180 μM and functions as an ADP-ribosylhydrolase critical for coronavirus replication and pathogenesis. SARS-CoV-2 nsp3-IN-2 is a small molecule chemical probe useful for viral research[1].

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-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-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-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].

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-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-38 is an orally available SARS-CoV-2 inhibitor with potential antiviral activity for the study of SARS viral infections.

SARS-CoV-2 Mpro-IN-2 is a selective SARS-CoV-2M pro inhibitor with an IC50 value of 0.40 μM.SARS-CoV-2 Mpro-IN-2 has good antiviral activity and can be used to study COVID-19.

SARS-CoV-2 Mpro-IN-9 (compound c7), a nonpeptidic, noncovalent inhibitor of SARS-CoV-2 main protease (Mpro), exhibits potent inhibitory action (IC50 = 0.085 μM) and improved physicochemical and drug metabolism and pharmacokinetics (DMPK) properties. It effectively suppresses viral replication in SARS-CoV-2-infected Vero E6 cells (EC50 = 1.10 μM) and demonstrates low cytotoxicity (CC50 > 50 μM) [1].

SARS-CoV-2-IN-13 (compound 5) is an analogue of niclosamide, displaying greater stability in human plasma and liver S9 enzymes assay. It improves bioavailability and half-life when administered orally and is a potent SARS-CoV-2 inhibitor with an IC50 of 0.057 μM [1].

SARS-CoV-2-IN-62 (Compound R3b) effectively inhibits SARS-CoV-2 replication in Vero E6 and Calu-3 cells, demonstrating low cytotoxicity with EC50 values of 2.97 μM and 3.82 μM, respectively [1].

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-IN-44, an inhibitor of SARS-CoV-2, effectively suppresses viral replication with an EC50 value of 0.6μM and exhibits negligible cytotoxicity in Calu-3 cells, rendering it suitable for antiviral research [1].

SARS-CoV-2-IN-63 (Compound R3e) is an inhibitor of SARS-CoV-2 replication, exhibiting low cytotoxicity and effectively suppressing viral replication in Vero E6 and Calu-3 cells, with half-maximal effective concentration (EC50) values of 1.99 μM and 1.92 μM, respectively [1].

SARS-CoV-2 Mpro-IN-1 (compound 16b-3) is a potent, selective, and irreversible inhibitor of the SARS-CoV-2 main protease (Mpro) with an IC50 value of 116 nM [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.

SARS-CoV-2-IN-65 (compound 2f (81)) is a potent, orally active reversible inhibitor of SARS-CoV-2 entry, mainly blocking the RBD:ACE2 interaction and TMPRSS2 activity in the ACE2-dependent pathway in Calu-3 cells [1].

SARS-CoV-2-IN-33 is an inhibitor of COVID-19. SARS-CoV-2-IN-3 exhibits good binding affinity (-8.0 Kcal/mole) for COVID-19 major protease (Mpro) (PDB ID: 6LU7). SARS-CoV-2-IN-33 exhibits good anti-proliferative effects on cancer cells. SSARS-CoV-2-IN-33 can be used to study cancer and COVID-19.

SARS-CoV-2-IN-45 (Compound 8p) is an effective inhibitor of SARS-CoV-2 that hinders viral replication in Calu-3 cells with an EC50 of 0.5 μM and exhibits negligible cytotoxicity [1].

SARS-CoV-2-IN-75 (compound 13), a chloroacetamide-based inhibitor, effectively suppresses cellular replication of SARS-CoV-2. It achieves a half-log reduction in viral titer (EC 68) at a concentration of 3 μM [1].

SARS-CoV-2-IN-78 (compound 3) functions as an inhibitor of nsp14 in SARS-CoV-2 and exhibits antiviral properties through its activity as an N7 methyltransferase [1].

SARS-CoV-2 Mpro-IN-6 is a selective, covalent, and irreversible inhibitor of SARS-CoV-2 main protease (Mpro) with an inhibition concentration (IC50) of 0.18 μM, and does not inhibit human cathepsins B, F, K, and L, or caspase 3.

SARS-CoV-2-IN-82 (compound A) acts as an inhibitor of the Programmed-1 ribosomal frameshift (-1 PRF) in SARS-CoV-2 [1].

Anti-SARS-CoV-2 Spike mAb (CR3022) is a human monoclonal IgG1 antibody produced from CHO cells, which specifically targets the S1 domain of the Spike protein in both SARS-CoV and SARS-CoV-2.

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.

Compound 8h, also known as SARS-CoV-2-IN-43, is a powerful inhibitor effective in obstructing the replication of SARS-CoV-2, exhibiting significant antiviral activity [1].

SARS-CoV-2-IN-55 (compound 65) is a SARS-CoV-2 inhibitor with low cytotoxicity, characterized by an IC50 of 0.3 μM, and acts through direct interaction with VSV-S pseudoparticles [1].

SARS-CoV-2-IN-57 (compound (+)-R-26) is a potent SARS-CoV-2 inhibitor with an IC50 of 80 nM, and shows high affinity for the Sigma Receptor, with Kis of 13.6 nM (S1R) and 14.4 nM (S2R) [1].

SARS-CoV-2-IN-64 (compound 9), derived from chenodeoxycholic acid, is a potent inhibitor of the SARS-CoV-2 spike glycoprotein [1].

MProinhibitor 11b is an inhibitor of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) main protease (MPro; IC50= 0.04 μM in a TR-FRET assay).1It reduces viral yield in the culture supernatant of SARS-CoV-2-infected Vero E6 cells (EC50= 0.72 μM). MProinhibitor 11b also reduces viral RNA copy numbers in the same model when used at concentrations ranging from 1.85 to 50 μM. 1.Dai, W., Zhang, B., Jiang, X.-M., et al.Structure-based design of antiviral drug candidates targeting the SARS-CoV-2 main proteaseScience368(6497)1331-1335(2020)

SARS-CoV-2 nsp13-IN-2 (Compound C2) is a small molecule inhibitor targeting the SARS-CoV-2 non-structural protein 13 (nsp13), specifically acting on the nsp13 ssDNA+ATPase with an IC50 of 42 μM.