sars

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 3CLpro-IN-16 is a covalent SARS-CoV-2 3CLpro inhibitor that inhibits 3CLpro activity and achieves its inhibitory effect by forming a covalent bond with Cys145.

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

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

SARS-CoV-2-IN-63 (Compound R3e) serves as an inhibitor of SARS-CoV-2 replication, demonstrating low cytotoxicity. It effectively suppresses viral replication within Vero E6 cells and Calu-3 cells, yielding half-maximal effective concentration (EC50) values of 1.99 μM and 1.92 μM, respectively [1].

SARS-CoV-2-IN-11 is a highly potent and non-toxic inhibitor of the 3C-like protease (3CLpro) of SARS-CoV-2, demonstrating IC50 and EC50 values of 0.17 nM and 1.45 nM, respectively. This compound targets the essential viral replication enzyme, 3CLpro, making it an attractive candidate for intervention strategies. SARS-CoV-2-IN-11 holds significant promise in the development of specific antivirals against SARS-CoV-2.

SARS-CoV-2-IN-66 (1), a derivative of vitamin K, functions as an inhibitor of SARS-CoV-2, exhibiting an effective concentration (EC50) of 70.8 μM in VeroE6/TMPRSS2 cells [1].

SARS-CoV-2-IN-68 (compound 6C) is a covalent inhibitor of both SARS-CoV-2 PLpro and Mpro, exhibiting potent antiviral properties by targeting the Zn-finger domain of PLpro [1].

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

SARS-CoV-2-IN-69 (Compound 7E) is a potent, non-covalent inhibitor of the SARS-CoV-2 main protease (M^pro) with an EC50 of 7.4 μM and also inhibits the papain-like protease (PL^pro) [1].

SARS-CoV-2 Mpro-IN-12 (compound D026) serves as an inhibitor of the main protease (Mpro) of SARS-CoV-2, exhibiting antiviral properties [1].

SARS-CoV-2-IN-67 (Compound 16), a derivative of vitamin K, exhibits anti-SARS-CoV-2 properties, with an effective concentration (EC50) of 64.8 μM in VeroE6/TMPRSS2 cells, and inhibits SARS-CoV-2 RdRp activity [1].

SARS-CoV-2-IN-46 is a SARS-CoV-2 inhibitor.

SARS-CoV-2-IN-59 (compound E07), an imidazoline derivative, is a non-peptide small molecule that inhibits SARS-CoV-2 by targeting its main protease (Mpro). It exhibits robust binding with Mpro residues (Met 165, Gln 166, Met 165, His 41, Gln 189) [1].

SARS-CoV-2 3CLpro-IN-15 (compound a), a beta-nitrostyrene derivative, acts as an inhibitor of the SARS-CoV-2 3CL protease (3CLpro), effectively inhibiting viral replication and transcription. It is instrumental in the identification of potential anti-COVID-19 lead compounds [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-57 (compound (+)-R-26) is a potent inhibitor of SARS-CoV-2 with an IC50 of 80 nM and demonstrates high affinity for the Sigma Receptor, exhibiting Kis of 13.6 nM (S1R) and 14.4 nM (S2R) [1].

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].

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

SARS-CoV-2 nsp3-IN-1 (Compound 15c) shows significant selectivity for coronavirus macrodomains, especially SARS-CoV-2 Mac1. SARS-CoV-2 nsp3-IN-1 can inhibit Mac1 ADP-ribosylhydrolase activity that is an inhibitor of Mac1 (IC50 = 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)

Anti-SARS-80R mAb (SARS-80R) is a human IgG1 monoclonal antibody that is derived from CHO cells. Its main function is to selectively bind to the Spike (S1) protein, effectively preventing the infection of susceptible cells by the SARS virus[1].

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

SARS-CoV-2 3CLpro-IN-10(5d) is a potent inhibitor of the SARS-CoV-2 3CL protease, exhibiting an IC50 value of 190 nM, and demonstrates varied efficiency against other coronaviruses with IC50 values of 790 nM for SARS-CoV-1 and 70 nM for MERS-CoV, indicating broad-spectrum antiviral activity.

SARS-CoV MPro-IN-2 effectively inhibits the SARS-CoV-2 main protease (M pro), crucial for the virus's replication and transcription in host cells, with an IC50 value of 72.07 nM. Given its significant role in processing viral polyproteins, M pro is regarded as a key target in drug discovery efforts. Consequently, SARS-CoV MPro-IN-2 holds promise for COVID-19 research.

SARS-CoV-2 Mpro-IN-5 is a dual inhibitor targeting Main Protease (M Pro) and Cathepsin L (CatL) with IC50 values of 1800 nM and 145 nM, respectively. This compound demonstrates antiviral activity by inhibiting SARS-CoV-2 replication in hACE2 expressing A549 cells, with an IC50 value of 14.7 nM.

SARS-CoV-2 nsp13-IN-2 (Compound C2) is a small molecule inhibitor of SARS-CoV-2 non-structural protein 13 (nsp13) that acts on nsp13 ssDNA+ATPase (IC50: 42 μM).

SARS-CoV-2-IN-25 (Compound CP026) disodium, a potent inhibitor of SARS-CoV-2 spike pseudoparticle transduction, demonstrates significant efficacy with an IC50 value of 1.6 μM. Additionally, it effectively inhibits enveloped viruses and liposomes, showcasing its broad-spectrum antiviral potential.

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

SARS-CoV-2-IN-17 (Compound 16) is a highly effective inhibitor of SARS-CoV-2 nucleocapsid protein (NPro). It demonstrates potent anti-viral activity, with an EC50 value of 2.18 μM. Furthermore, SARS-CoV-2-IN-17 binds to NPro with a low Kd value of 7.82 μM, highlighting its potency as a NPro ligand [1].

SARS-CoV-2-IN-6 is an inhibitor of SARS-CoV-2 3CLpro with the IC 50 value of 73 nM.

SARS-CoV-2-IN-22 is a SARS-CoV-2 pseudovirus inhibitor (IC50: 16.96 μM).

SARS-CoV-2 nsp13-IN-4 (C4 (d)) is a potent and selective small-molecule inhibitor of nsp13 helicase. SARS-CoV-2 nsp13-IN-4 inhibits the ssDNA+ ATPase activity of nsp13 with an IC 50 of 57 μM. SARS-CoV-2 nsp13-IN-4 can provide a broad-spectrum antiviral effect.

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-18 (Compound 26) is a potent inhibitor of SARS-CoV-2 3C-like protease (IC50 = 45 nM) [1].

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

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

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 a critical enzyme 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-58 (Compound 21H) serves as an antiviral agent targeting SARS-CoV-2, demonstrating efficacy with an EC50 of 18 μM. It specifically inhibits the SARS-CoV-2 main protease (Mpro) with an IC50 value of 0.35 μM [1].

SARS-CoV-2 Mpro-IN-10 (27h) is a potent inhibitor of the Mpro enzyme, exhibiting IC50 and EC50 values of 10.9 nM and 43.6 nM, respectively. It is utilized in research focused on the SARS-CoV-2 virus [1].

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