sars cov in 1

SARS-CoV-IN-1 is an effective SARS-CoV replication inhibitor with an EC50 of 4.9 μM in Vero cells.

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].

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 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 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-IN-1 is a potent inhibitor of Mpro [SARS-CoV-2 Mpro, SARS-CoV Mpro, and MERS-CoV Mpro] with IC50 values of 0.67, 0.90, and 0.58 μM, respectively.

SARS-CoV-2 MERS Mpro-IN-1 is a potent inhibitor of the main proteases in SARS-CoV-2 and MERS, with IC50 values of 0.10 and 0.06 µM, respectively.

SARS-CoV-2 nsp13-IN-1 (compound C1) is a potent inhibitor of nsp13 (non-structural protein 13), selectively inhibiting nsp13 ssDNA+ATPase with an IC50 of 6 μM, but not ssDNA-ATPase, 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-38 is an orally available SARS-CoV-2 inhibitor with potential antiviral activity for the study of SARS viral infections.

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 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.

MERS-CoV-IN-1 exhibits excellent inhibitory activity against coronavirus and is useful as a pharmaceutical composition for preventing coronavirus-induced diseases (MERS-CoV and SARS).

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 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-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 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-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].

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-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-IN-29 disodium, a diphosphate ester featuring a benzene system and molecular tweezers architecture, demonstrates antiviral efficacy by targeting SARS-CoV-2 with half-maximal inhibitory concentrations (IC50s) of 1.5 μM for virus activity and 1.6 μM for spike pseudoparticle transduction. Additionally, it disrupts liposomal membranes, evidenced by a half-maximal effective concentration (EC50) of 3.0 μM [1].

SARS-CoV-2-IN-30 disodium, a benzene-system-based two-armed diphosphate ester featuring molecular tweezers, demonstrates antiviral efficacy, with IC50 values of 0.6 μM against SARS-CoV-2 and 6.9 μM for spike pseudoparticle transduction, respectively. Additionally, it disrupts liposomal membranes, evidenced by an EC50 of 6.9 μM [1].

SARS-CoV-2-IN-28 disodium, a diphosphate ester featuring a C7 alkyl chain and extended-length molecular tweezers, demonstrates antiviral efficacy by showing IC50 values of 0.4 μM and 1.0 μM against SARS-CoV-2 activity and spike pseudoparticle transduction, respectively. Additionally, it disrupts liposomal membranes with an EC50 of 4.4 μM [1].

SARS-CoV-2-IN-30, a two-armed diphosphate ester featuring a benzene system and molecular tweezers, demonstrates antiviral properties, achieving IC50 values of 0.6 μM against SARS-CoV-2 activity and 6.9 μM for spike pseudoparticle transduction. Additionally, it disrupts liposomal membranes with an EC50 of 6.9 μM [1].

SARS-CoV-2-IN-23 disodium, a medium-length molecular tweezer and two-armed diphosphate ester, demonstrates antiviral properties by inhibiting SARS-CoV-2 activity and spike pseudoparticle transduction with IC50 values of 8.2 μM and 2.6 μM, respectively. Additionally, it disrupts liposomal membranes with an EC50 of 4.4 μM [1].

SARS-CoV-2-IN-17 (Compound 16) is a highly effective inhibitor of the SARS-CoV-2 nucleocapsid protein (NPro), demonstrating potent antiviral activity with an EC50 value of 2.18 μM and binding to NPro with a low Kd value of 7.82 μM, underscoring its potency as a NPro ligand [1].

SARS-CoV-2-IN-64 (compound 9), derived from chenodeoxycholic acid, is a potent inhibitor of the SARS-CoV-2 spike glycoprotein [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-18 (Compound 26) is a powerful inhibitor of the SARS-CoV-2 3C-like protease, with an IC50 of 45 nM [1].

SARS-CoV-2-IN-39 is a SARS-CoV-2 inhibitor with an EC50 of 1 μM. SARS-CoV-2-IN-39 has antiviral activity and inhibits SARS-CoV-2 by inhibiting SKP2 protein and stabilizing BECN1.

SARS-CoV-2-IN-82 (compound A) acts as an inhibitor of the Programmed-1 ribosomal frameshift (-1 PRF) in SARS-CoV-2 [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-IN-50 (Compound X77C) is a potent inhibitor of the SARS-CoV-2 main protease (M^pro), demonstrating high affinity for the enzyme's catalytic site [1].

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-49 acts as an irreversible covalent inhibitor targeting the main protease of SARS-CoV-2 [1].

ARS-CoV-2-IN-53 (Compd 5d) shows an inhibitory effect on SARS-CoV-2 replication with an EC50 value of 14.3 μM and exhibits significant antiviral activity against human coronavirus 229E (HCoV-229E) [1].

SARS-CoV-2-IN-56 (Compound 63) is a SARS-CoV-2 inhibitor exhibiting antiviral activity, with an IC50 of 0.7 μM in Vero E6 cells [1].

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-58 (Compound 21H) is an antiviral agent targeting SARS-CoV-2, demonstrating an EC50 of 18 μM and specifically inhibiting the SARS-CoV-2 main protease (Mpro) with an IC50 of 0.35 μM [1].

SARS-CoV-2-IN-23 (compound GRL-0617) is an inhibitor of SARS-CoV-2 papain-like protease (PLpro) with an IC50 of 2.3 μM [1].

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-IN-27 disodium, a diphosphate ester featuring a C6 alkyl chain and molecular tweezers of extended length, demonstrates antiviral efficacy by achieving IC50 values of 1.0 μM against SARS-CoV-2 activity and 1.7 μM for spike pseudoparticle transduction. Additionally, it disrupts liposomal membranes, displaying an EC50 value of 6.5 μM [1].

SARS-CoV-2-IN-23, a two-armed diphosphate ester and medium-length molecular tweezers, displays antiviral properties, demonstrating IC50 values of 8.2 μM against SARS-CoV-2 activity and 2.6 μM for spike pseudoparticle transduction. Additionally, it induces liposomal membrane disruption with an EC50 value of 4.4 μM [1].

SARS-CoV-2-IN-15 (compound 11) is a niclosamide analogue exhibiting greater stability in human plasma and liver S9 enzyme assays compared to niclosamide. It enhances bioavailability and half-life upon oral administration and is a potent SARS-CoV-2 inhibitor with an IC50 of 0.49 μM [1].

SARS-CoV-2-IN-66 (1), a derivative of vitamin K, serves as an inhibitor of SARS-CoV-2, with an effective concentration (EC50) of 70.8 μM in VeroE6 TMPRSS2 cells [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-IN-16 (Compound 12) is a potent inhibitor of SARS-CoV-2 nucleocapsid protein (NPro) with antiviral activity (EC50 = 3.69 μM) and binds to NPro with a low Kd value of 7.82 μM, indicating its effectiveness as an NPro ligand [1].

SARS-CoV-2-IN-20 (Compound 1a) is a highly effective SARS-CoV-2 inhibitor with an impressive EC50 value of 6.5 μM, demonstrating significant potential for advancing infectious disease research [1].

Ribavirin (Tribavirin) is a synthetic nucleoside analog of ribofuranose with activity against hepatitis C virus and other RNA viruses.