S1386 |
Nafamostat mesilate (FUT-175)
|
Nafamostat mesilate (FUT-175) is a synthetic serine protease inhibitor, used as an anticoagulant during hemodialysis. Nafamostat mesylate blocks activation of SARS-CoV-2 and is investigated as a new treatment option for COVID-19. Nafamostat Mesilate attenuates inflammation and apoptosis. |
-
J Immunother Cancer, 2024, 12(11)e009805
-
Cell Death Dis, 2024, 15(2):109
-
CNS Neurosci Ther, 2024, 30(6):e14822
|
|
S8969 |
Molnupiravir (EIDD-2801)
|
Molnupiravir (EIDD-2801, MK-4482) is an orally bioavailable prodrug of the ribonucleoside analog β-d-N4-hydroxycytidine (NHC; EIDD-1931) with broad-spectrum antiviral activity against SARS-CoV-2, MERS-CoV, SARS-CoV, and the causative agent of COVID-19. |
-
Antiviral Res, 2024, 225:105840
-
Front Pharmacol, 2024, 15:1431617
-
BMC Complement Med Ther, 2024, 24(1):274
|
|
S9866 |
Nirmatrelvir (PF-07321332)
|
Nirmatrelvir (PF-07321332) is an reversible covalent inhibitor of SARS-CoV-2 main protease (Mpro, also referred to as 3CL protease) with an ki of 3.11 nM. PF-07321332 binds directly to the catalytic cysteine (Cys145) residue of the enzyme.
|
-
Antiviral Res, 2024, 225:105840
-
J Biol Chem, 2024, S0021-9258(24)02176-8
-
Viruses, 2024, 16(7)1158
|
|
S0833 |
EIDD-1931 (NHC)
|
EIDD-1931 (NHC) is an active metabolite of EIDD-2801, a promising COVID-19 inhibitor. EIDD-1931 (NHC) has broad spectrum antiviral activity against SARS-CoV-2, MERS-CoV, SARS-CoV, and related zoonotic group 2b or 2c Bat-CoVs with average IC50 of 0.15 μM, as well as increased potency against a coronavirus bearing resistance mutations to the nucleoside analog inhibitor remdesivir. |
-
Nucleic Acids Res, 2023, 10.1093/nar/gkad1002
-
NPJ Digit Med, 2022, 5(1):83
-
J Med Virol, 2022, 10.1002/jmv.27650
|
|
S9731 |
PF-00835231
|
PF-00835231 is a 3CLpro (Mpro) inhibitor that may targets SARS-CoV-2 protease 3CLpro as a potential new treatment for COVID-19. |
-
Mol Cell, 2022, S1097-2765(22)00433-6
-
Bioorg Med Chem Lett, 2022, 66:128732
-
Nat Commun, 2021, 12(1):6786
|
|
S0515 |
PLpro inhibitor
|
PLpro inhibitor is a potent papain-like protease (PLpro) inhibitor with IC50 of 2.6 μM. |
-
PLoS Pathog, 2023, 19(8):e1011592
-
PLoS Pathog, 2023, 19(8):e1011592
-
bioRxiv, 2022, 2022.08.06.503039
|
|
A2403 |
Narsoplimab (Anti-MASP2)
|
Narsoplimab (Anti-MASP2) is a monoclonal antibody against mannan-binding lectin (MBL)-associated serine protease-2 (MASP-2), with potential anti-thrombotic and immunomodulating activities. MW: 145.5 kD. |
|
|
A2853 |
Gimsilumab (Anti-CSF2 / GM-CSF)
|
Gimsilumab (Anti-CSF2 / GM-CSF) is a human immunoglobulin G1 (IgG1) monoclonal antibody directed against the myeloid cell growth factor and inflammatory mediator granulocyte-macrophage colony-stimulating factor (GM-CSF) with potential immunomodulating activity. MW : 145.8 KD. |
|
|
A2854 |
Lenzilumab (Anti-CSF2 / GM-CSF)
|
Lenzilumab (Anti-CSF2 / GM-CSF) is a recombinant monoclonal antibody against the cytokine granulocyte macrophage colony-stimulating factor (GM-CSF), with potential immunomodulating activity. MW: 145.72 KD. |
|
|
E1900New |
Simnotrelvir
|
Simnotrelvir(SIM0417, SARS-CoV-2-IN-41) is an inhibitor of coronavirus main proteinase (3CLpro) (SARS-CoV-2 3CLpro) with an IC50 of 24 nM. It has a potential anti-SARS-CoV-2 activity. |
|
|
S0793 |
ML188
|
ML188 is a non-covalent SARS-CoV 3CLpro inhibitor with IC50 of 1.5 μM. ML188 has antiviral activity. |
|
|
S0875 |
XP-59
|
XP-59 is a potent inhibitor of the SARS-CoV Mpro, with a Ki of 0.1 μM. |
|
|
S6845 |
GRL0617
|
GRL0617 is a potent, selective and competitive noncovalent inhibitor of severe acute respiratory syndrome (SARS-CoV) papain-like protease (PLPro)/deubiquitinase with IC50 of 0.6 μM and Ki of 0.49 μM. GRL0617 inhibits SARS-CoV viral replication in Vero E6 cells with EC50 of 15 microM and has no associated cytotoxicity. |
-
J Virol, 2024, e0085524.
|
|
E1112 |
GS-621763
|
GS-621763, an orally bioavailable prodrug of GS-441524, shows a dose-dependent antiviral effect on SARS-CoV-2 reporter virus expressing nanoluciferase (SARS-CoV-2 nLUC) replication with an EC50 of 2.8 μM, also inhibits reporter SARS-CoV-2 expressing firefly luciferase (SARS-CoV-2 Fluc) replication with EC50 of 0.125 μM. |
|
|
E0613 |
TC-067533
|
TC-067533 is a potent SARS-CoV papain-like protease (PLpro) inhibitor with an IC50 of 8.7 μM. |
|
|
S3553 |
Riamilovir
|
Riamilovir (Triazavirin) is a broad-spectrum antiviral drug candidate, which can be used for potential application against the Coronavirus 2019-nCoV. |
|
|
E1111 |
VV116
|
VV116, a promising orally administered anti-SARS-CoV-2 nucleoside drug candidate, exerts functions by targeting the viral RNA-dependent RNA polymerase through its nucleoside triphosphate form with an IC50 of 0.67±0.24 μM. |
|
|
E0052 |
Merafloxacin
|
Merafloxacin (CI-934) is a fluoroquinolone antibacterial thats inhibit -1 frameshifting efficiency of SARS-CoV-2 and other betacoronaviruses. |
|
|
E1131 |
Ensitrelvir fumarate
|
S-217622 (Ensitrelvir fumarate) is the first orally active non-covalent, non-peptidic, SARS-CoV-2 3CL protease inhibitor with IC50 of 13 nM. |
|
|
S9963 |
paquinimod
|
Paquinimod (ABR 25757), a specific inhibitor of S100A8/A9, could rescue the pneumonia with substantial reduction of viral loads in SARS-CoV-2-infected mice. |
-
Cell Rep, 2024, 43(11):114900
|
|
E1174 |
Coronastat(NK01-63)
|
Coronastat(NK01-63) is a potent inhibitor of the SARS-CoV-2 3CL protease, which is a critical drug target for small molecule COVID-19, given its likely druggability and essentiality in the viral maturation and replication cycle. |
|
|
E1013 |
Bemnifosbuvir Hemisulfate (AT-527)
|
Bemnifosbuvir Hemisulfate (AT-527, RG-6422, RO 7496998) is a hemi-sulfate salt of AT-511. AT-511 is a potent inhibitor of SARS-CoV-2 with an EC90 of 0.47 μM. |
|
|
S1386 |
Nafamostat mesilate (FUT-175)
|
Nafamostat mesilate (FUT-175) is a synthetic serine protease inhibitor, used as an anticoagulant during hemodialysis. Nafamostat mesylate blocks activation of SARS-CoV-2 and is investigated as a new treatment option for COVID-19. Nafamostat Mesilate attenuates inflammation and apoptosis. |
- J Immunother Cancer, 2024, 12(11)e009805
- Cell Death Dis, 2024, 15(2):109
- CNS Neurosci Ther, 2024, 30(6):e14822
|
|
S8969 |
Molnupiravir (EIDD-2801)
|
Molnupiravir (EIDD-2801, MK-4482) is an orally bioavailable prodrug of the ribonucleoside analog β-d-N4-hydroxycytidine (NHC; EIDD-1931) with broad-spectrum antiviral activity against SARS-CoV-2, MERS-CoV, SARS-CoV, and the causative agent of COVID-19. |
- Antiviral Res, 2024, 225:105840
- Front Pharmacol, 2024, 15:1431617
- BMC Complement Med Ther, 2024, 24(1):274
|
|
S9866 |
Nirmatrelvir (PF-07321332)
|
Nirmatrelvir (PF-07321332) is an reversible covalent inhibitor of SARS-CoV-2 main protease (Mpro, also referred to as 3CL protease) with an ki of 3.11 nM. PF-07321332 binds directly to the catalytic cysteine (Cys145) residue of the enzyme.
|
- Antiviral Res, 2024, 225:105840
- J Biol Chem, 2024, S0021-9258(24)02176-8
- Viruses, 2024, 16(7)1158
|
|
S0833 |
EIDD-1931 (NHC)
|
EIDD-1931 (NHC) is an active metabolite of EIDD-2801, a promising COVID-19 inhibitor. EIDD-1931 (NHC) has broad spectrum antiviral activity against SARS-CoV-2, MERS-CoV, SARS-CoV, and related zoonotic group 2b or 2c Bat-CoVs with average IC50 of 0.15 μM, as well as increased potency against a coronavirus bearing resistance mutations to the nucleoside analog inhibitor remdesivir. |
- Nucleic Acids Res, 2023, 10.1093/nar/gkad1002
- NPJ Digit Med, 2022, 5(1):83
- J Med Virol, 2022, 10.1002/jmv.27650
|
|
S9731 |
PF-00835231
|
PF-00835231 is a 3CLpro (Mpro) inhibitor that may targets SARS-CoV-2 protease 3CLpro as a potential new treatment for COVID-19. |
- Mol Cell, 2022, S1097-2765(22)00433-6
- Bioorg Med Chem Lett, 2022, 66:128732
- Nat Commun, 2021, 12(1):6786
|
|
S0515 |
PLpro inhibitor
|
PLpro inhibitor is a potent papain-like protease (PLpro) inhibitor with IC50 of 2.6 μM. |
- PLoS Pathog, 2023, 19(8):e1011592
- PLoS Pathog, 2023, 19(8):e1011592
- bioRxiv, 2022, 2022.08.06.503039
|
|
E1900New |
Simnotrelvir
|
Simnotrelvir(SIM0417, SARS-CoV-2-IN-41) is an inhibitor of coronavirus main proteinase (3CLpro) (SARS-CoV-2 3CLpro) with an IC50 of 24 nM. It has a potential anti-SARS-CoV-2 activity. |
|
|
S0793 |
ML188
|
ML188 is a non-covalent SARS-CoV 3CLpro inhibitor with IC50 of 1.5 μM. ML188 has antiviral activity. |
|
|
S0875 |
XP-59
|
XP-59 is a potent inhibitor of the SARS-CoV Mpro, with a Ki of 0.1 μM. |
|
|
S6845 |
GRL0617
|
GRL0617 is a potent, selective and competitive noncovalent inhibitor of severe acute respiratory syndrome (SARS-CoV) papain-like protease (PLPro)/deubiquitinase with IC50 of 0.6 μM and Ki of 0.49 μM. GRL0617 inhibits SARS-CoV viral replication in Vero E6 cells with EC50 of 15 microM and has no associated cytotoxicity. |
- J Virol, 2024, e0085524.
|
|
E1112 |
GS-621763
|
GS-621763, an orally bioavailable prodrug of GS-441524, shows a dose-dependent antiviral effect on SARS-CoV-2 reporter virus expressing nanoluciferase (SARS-CoV-2 nLUC) replication with an EC50 of 2.8 μM, also inhibits reporter SARS-CoV-2 expressing firefly luciferase (SARS-CoV-2 Fluc) replication with EC50 of 0.125 μM. |
|
|
E0613 |
TC-067533
|
TC-067533 is a potent SARS-CoV papain-like protease (PLpro) inhibitor with an IC50 of 8.7 μM. |
|
|
E1111 |
VV116
|
VV116, a promising orally administered anti-SARS-CoV-2 nucleoside drug candidate, exerts functions by targeting the viral RNA-dependent RNA polymerase through its nucleoside triphosphate form with an IC50 of 0.67±0.24 μM. |
|
|
E0052 |
Merafloxacin
|
Merafloxacin (CI-934) is a fluoroquinolone antibacterial thats inhibit -1 frameshifting efficiency of SARS-CoV-2 and other betacoronaviruses. |
|
|
E1131 |
Ensitrelvir fumarate
|
S-217622 (Ensitrelvir fumarate) is the first orally active non-covalent, non-peptidic, SARS-CoV-2 3CL protease inhibitor with IC50 of 13 nM. |
|
|
S9963 |
paquinimod
|
Paquinimod (ABR 25757), a specific inhibitor of S100A8/A9, could rescue the pneumonia with substantial reduction of viral loads in SARS-CoV-2-infected mice. |
- Cell Rep, 2024, 43(11):114900
|
|
E1174 |
Coronastat(NK01-63)
|
Coronastat(NK01-63) is a potent inhibitor of the SARS-CoV-2 3CL protease, which is a critical drug target for small molecule COVID-19, given its likely druggability and essentiality in the viral maturation and replication cycle. |
|
|
E1013 |
Bemnifosbuvir Hemisulfate (AT-527)
|
Bemnifosbuvir Hemisulfate (AT-527, RG-6422, RO 7496998) is a hemi-sulfate salt of AT-511. AT-511 is a potent inhibitor of SARS-CoV-2 with an EC90 of 0.47 μM. |
|
|