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SARS-CoV-23CLpro probe-1 (Compound probe 3) is a selective and activity-based probe for the SARS-CoV-23CL protease. SARS-CoV-23CLpro probe-1 can detect endogenously expressed 3CLpro in SARS-CoV-2-infected cells .
SARS-CoV-23CLpro-IN-15 (compound a) is a beta-nitrostyrene coronavirus SARS-CoV-2 inhibitor that targets the SARS-CoV-23CL protease (3CLpro). SARS-CoV-23CLpro-IN-15 inhibits viral replication and transcription and plays a key role in the discovery of anti-COVID-19 lead compounds .
SARS-CoV-23CLpro-IN-1 (Compound 14c) is a potent inhibitor of SARS-CoV-23CL pro. 3CL pro (main coronaviruses cysteine-protease) has been identified as a promising target for the development of antiviral agents. SARS-CoV-23CLpro-IN-1 has the potential for the research of infection diseases .
SARS-CoV-23CLpro-IN-16 (Compound 3a) is a covalent SARS-CoV-23CLpro inhibitor (IC50s: 2.124 μM). SARS-CoV-23CLpro-IN-16 binds to the active site and forms a covalent bond with Cys145 of 3CLpro .
SARS-CoV-23CLpro-IN-6 is a reversible covalent inhibitor of SARS-CoV-23CL protease. SARS-CoV-23CLpro-IN-6 has potent inhibitory activity for SARS-CoV-23CL pro with an IC50 value of 4.9 μM. SARS-CoV-23CLpro-IN-6 can be used for the research of coronavirus disease 2019 (COVID-19) .
SARS-CoV-23CLpro-IN-14 (compound 11j) is an orally active SARS-CoV-23CLpro inhibitor. SARS-CoV-23CLpro-IN-14 shows significant anti-SARS-CoV-2 activity (EC50 = 0.18 μM) and low cytotoxicity (CC50 > 50 μM) in Vero E6 cells .
SARS-CoV-23CLpro-IN-2 (Compound 1) is a potent inhibitor of 3CL protease. SARS-CoV-23CLpro-IN-2 has the potential for the research of SARS-CoV-2 diseases .
SARS-CoV-23CLpro-IN-13 is a potent SARS-CoV-23CL protease inhibitor with an IC50 value of 21 nM. SARS-CoV-23CLpro-IN-13 shows anti-coronavirus activity .
SARS-CoV-23CLpro-IN-22 (Compound 17) is a cathepsin L (CTSL ) inhibitor with an IC50 value of 32.5 nM. SARS-CoV-23CLpro-IN-22 can be used for the study of SARS-CoV-2 virus .
SARS-CoV-23CLpro-IN-5 is a covalent inhibitor of 3C-like protease (3CL pro). SARS-CoV-23CLpro-IN-5 has inhibitory activity for 3CL pro with an IC50 value of 3.8 nM. SARS-CoV-23CLpro-IN-5 has 9.0% oral bioavailability (BA). SARS-CoV-23CLpro-IN-5 can be used for the research of coronavirus disease 2019 (COVID-19) .
SARS-CoV-23CLpro-IN-23 (Compound Cd3) is a compound that can be isolated from Citrus depressa. SARS-CoV-23CLpro-IN-23 has good inhibitory activity to the SARS-CoV-2 spike protein, with KD of 0.79 μM. SARS-CoV-23CLpro-IN-23 can bind to key amino acid residue, disrupting the formation of the spike protein and h-ACE2 complex .
SARS-CoV-23CLpro-IN-19 (Compound C5a) is a non-covalent, non-peptide SARS-CoV-23CLpro inhibitor (IC50s: 0.7 μM). SARS-CoV-23CLpro-IN-19 has broad-spectrum activity against Omicron subvariants (BA.5, BQ.1.1, and XBB.1.5) infection in human cells, with EC50 values between 30-69 nM .
SARS-CoV-23CLpro-IN-21 (Compound D6) irreversibly and covalently inhibits SARS-CoV-23CL pro with an IC50 of 0.03 μM. SARS-CoV-23CLpro-IN-21 also inhibits SARS-CoV-13CL pro with an IC50 of 0.12μM .
SARS-CoV-2-IN-10 is a potent and nontoxic inhibitor of SARS-CoV-23CL protease(3CLpro) with an IC50 and EC50 of 0.13 and 1.03 nM, respectively. SARS-CoV-23C-like protease (3CLpro), an enzyme essential for viral replication, is an attractive target for intervention. SARS-CoV-2-IN-11 may lead to the emergence of effective SARS-CoV-2-specific antivirals .
SARS-CoV-2-IN-11 is a potent and nontoxic inhibitor of SARS-CoV-23CL protease(3CLpro) with an IC50 and EC50 of 0.17 and 1.45 nM, respectively. SARS-CoV-23C-like protease (3CLpro), an enzyme essential for viral replication, is an attractive target for intervention. SARS-CoV-2-IN-11 may lead to the emergence of effective SARS-CoV-2-specific antivirals .
Hydroxyethylamine (Compd VII) is a SARS-CoV-23CLpro inhibitor with an IC50 of ~10 μM in the spread assay. Hydroxyethylamine has potent antiviral activities .
3CPLro-IN-1 (compound A17) is a potent and orally active inhibitor of SARS-CoV-23CLpro with an IC50 of 5.65 μM. 3-Chymotrypsin-like cysteine protease (3CLpro) is an indispensable protein in viral replication and represents an attractive agent target for fighting COVID-19 .
MCA-AVLQSGFR-Lys(Dnp)-Lys-NH2 is a fluorescent substrate used for fluorescence resonance energy transfer (FRET) protease assays. This substrate is employed to measure the activity of SARS-CoV-23CLpro .
3CPLro-IN-2 (compound C1) is a potent and orally active inhibitor of SARS-CoV-23CLpro with an IC50 and Ki of 1.55 and 6.09 μM, respectively. 3-Chymotrypsin-like cysteine protease (3CLpro) is an indispensable protein in viral replication and represents an attractive agent target for fighting COVID-19 .
WU-04 is a non-covalent inhibitor of SARS-CoV-2, targeting the 3CLpro protein. WU-04 has high inhibitory effect on the 3CLpro protein of 6 SARS-CoV-2 variants (Alpha, Beta, Gamma, Delta, Lambda and Omicron) and 2 coronaviruses (SARS-CoV and MERS-CoV) .
PROTAC KRAS G12D degrades SARS-CoV-2, 3-curd trypsin-like protease (3CLPro). Protac KRAS G12D degrades SARS-CoV-2, 3-curd trypsin-like protease (3CLPRO). The PROTAC molecule is designed by partially coupling a GC-376-based dipeptidyl 3CLPro ligand with pomadomide via a piperazine-piperidine linker .
Lufotrelvir (PF-07304814), a phosphate proagent of PF-00835231, acts as a potent 3CLpro protease (Mpro) inhibitor with SARS-CoV-2 antiviral activity. Lufotrelvir binds and inhibits SARS-CoV-23CLpro activity with a Ki of 174nM. Lufotrelvir is promising single antiviral agent and also can be used for the research of combination with other antivirals that target other critical stages of the coronavirus life cycle.
Isojacareubin can be isolated from Hypericum japonicum. Isojacareubin covalently inhibits SARS-CoV-23CLpro. Isojacareubin also has anti-helicobacter activity. Isojacareubin inhibits PKC, and suppresses hepatocellular carcinoma metastasis and induces apoptosis[2][3].
SARS-CoV MPro-IN-1 is a SARS-CoV-23CLpro covalent inhibitor, with an IC50 of 40 nM. SARS-CoV MPro-IN-1 shows good anti-SARS-CoV-2-infection activity in cell culture with an EC50 of 0.33 μM. SARS-CoV MPro-IN-1 has the potential for COVID-19 research .
Boceprevir-d9 is the deuterium labeled Boceprevir. Boceprevir (EBP 520) is a potent, highly selective, orally bioavailable HCV NS3 protease inhibitor with a Ki of 14 nM in both enzyme assay and an EC90 of 350 nM in cell-based replicon assay[1][2][3][4][5]. Boceprevir inhibits SARS-CoV-23CLpro activity[6].
Telaprevir-d4 is the deuterium labeled Telaprevir. Telaprevir (VX-950) is a highly selective, reversible, and potent peptidomimetic inhibitor of the HCV NS3-4A protease, the steady-state inhibitory constant (Ki) of Telaprevir is 7 nM against a genotype 1 (H strain) NS3 protease domain plus a NS4A cofactor peptide[1][2][3]. Telaprevir inhibits SARS-CoV-23CLpro activity[4].
Antiviral agent 25 (compound 6g) is a new non-peptide analog covalent inhibitor of SARS-CoV-23CL pro. Antiviral agent 25 has a strong inhibitory effect on SARS-CoV-23CL pro and SARS-CoV-2 PL pro with IC50 values of 0.118 µM, 0.448 µM, respectively. Antiviral agent 25 has antiviral effect on SARS-CoV-2 with an EC50 value of 7.249 µM .
Nirmatrelvir (PF-07321332) is a potent and orally active SARS-CoV 3C-like protease (3CL PRO) inhibitor. Nirmatrelvir (PF-07321332) targets to the SARS-CoV-2 virus and can be used for COVID-19 research .
CCF0058981 (CCF981), 3-chlorophenyl analogue, is a noncovalent SARS-CoV-23CL pro(SC2) inhibitor with an IC50 of 68 nM. CCF0058981 inhibits SC1 (SARS-CoV-1 3CL pro) with an IC50 of 19 nM. CCF0058981 has antiviral efficacy and has the potential for COVID-19 research .
INSCoV-601I(1) is a potent inhibitor of M pro(3CLpro). Proteases (PL pro and 3CL pro) are involved with transcription and replication of the virus. INSCoV-601I(1) has the potential for the research of SARS-CoV-2 infection (extracted from patent WO2021219089A1) .
INSCoV-614(1B) is a potent inhibitor of M pro(3CLpro). Proteases (PL pro and 3CL pro) are involved with transcription and replication of the virus. INSCoV-614(1B) has the potential for the research of SARS-CoV-2 infection (extracted from patent WO2021219089A1) .
INSCoV-600K(1) is a potent inhibitor of M pro(3CLpro). Proteases (PL pro and 3CL pro) are involved with transcription and replication of the virus. INSCoV-600K(1) has the potential for the research of SARS-CoV-2 infection (extracted from patent WO2021219089A1) .
Nirmatrelvir (Standard) is the analytical standard of Nirmatrelvir. This product is intended for research and analytical applications. Nirmatrelvir (PF-07321332) is a potent and orally active SARS-CoV 3C-like protease (3CL PRO) inhibitor. Nirmatrelvir (PF-07321332) targets to the SARS-CoV-2 virus and can be used for COVID-19 research .
YH-53 is a potent 3CL pro inhibitor with Ki values of 6.3 nM, 34.7 nM for SARS-CoV-1 3CL pro and SARS-CoV-23CL pro, respectively. YH-53 strongly blocks the SARS-CoV-2 replication. YH-53 is a peptidomimetic compound with a unique benzothiazolyl ketone. YH-53 has the potential for COVID-19 research [2].
SARS-CoV-23CLpro probe-1 (Compound probe 3) is a selective and activity-based probe for the SARS-CoV-23CL protease. SARS-CoV-23CLpro probe-1 can detect endogenously expressed 3CLpro in SARS-CoV-2-infected cells .
MCA-AVLQSGFR-Lys(Dnp)-Lys-NH2 is a fluorescent substrate used for fluorescence resonance energy transfer (FRET) protease assays. This substrate is employed to measure the activity of SARS-CoV-23CLpro .
Isojacareubin can be isolated from Hypericum japonicum. Isojacareubin covalently inhibits SARS-CoV-23CLpro. Isojacareubin also has anti-helicobacter activity. Isojacareubin inhibits PKC, and suppresses hepatocellular carcinoma metastasis and induces apoptosis[2][3].
Boceprevir-d9 is the deuterium labeled Boceprevir. Boceprevir (EBP 520) is a potent, highly selective, orally bioavailable HCV NS3 protease inhibitor with a Ki of 14 nM in both enzyme assay and an EC90 of 350 nM in cell-based replicon assay[1][2][3][4][5]. Boceprevir inhibits SARS-CoV-23CLpro activity[6].
Telaprevir-d4 is the deuterium labeled Telaprevir. Telaprevir (VX-950) is a highly selective, reversible, and potent peptidomimetic inhibitor of the HCV NS3-4A protease, the steady-state inhibitory constant (Ki) of Telaprevir is 7 nM against a genotype 1 (H strain) NS3 protease domain plus a NS4A cofactor peptide[1][2][3]. Telaprevir inhibits SARS-CoV-23CLpro activity[4].
SARS-CoV-23CLpro probe-1 (Compound probe 3) is a selective and activity-based probe for the SARS-CoV-23CL protease. SARS-CoV-23CLpro probe-1 can detect endogenously expressed 3CLpro in SARS-CoV-2-infected cells .
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