SARS-CoV-2 3CLpro-IN-16 (Compound 3a) is a covalent SARS-CoV-2 3CLpro inhibitor (IC50s: 2.124 μM). SARS-CoV-2 3CLpro-IN-16 binds to the active site and forms a covalent bond with Cys145 of 3CLpro[1].
F8-S40 is an inhibitor of SARS-CoV-2 main protease, with an IC50 of 10.88 μM[1].
Amprenavir-d4-1 is deuterium labeled Amprenavir. Amprenavir (VX-478) is a HIV protease inhibitor (Ki=0.6 nM) used to treat HIV infection. Amprenavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.09 μM.
Umifenovir is a potent, orally active broad-spectrum antiviral agent with activity against a number of enveloped and non-enveloped viruses. Umifenovir is used as an anti-influenza virus agent. Umifenovir could effectively inhibit the fusion of virus with host cells[1][2]. Umifenovir is an efficient inhibitor of SARS-CoV-2 in vitro[2]. Umifenovir shows anti-inflammatory activity[3].
SARS-CoV-2 nsp14-IN-3 (4975) is an inhibitor of the SARS-CoV-2 Nsp14 N7-Methyltransferase (IC50: 3.5 μM)[1].
Burfiralimab (hzVSF-v13) is a monoclonal IgG4 antibody against vimentin expressed on the surface of virus-infected cells, with broad-spectrum antiviral activity and anti-inflammatory effects against virus-induced inflammation. Burfiralimab can be used in severe COVID-19 studies[1].
SARS-CoV-2-IN-21 (compound 10), a penicillin sulfone benzyl C6 derivative, is a potent SARS-CoV-2 main protease inhibitor, with an IC50 of 5.3 μM. SARS-CoV-2-IN-21 can be used for COVID-19 research[1].
SARS-CoV-2-IN-43 (Compound 8h) is a potentSARS-CoV-2replication inhibitor with antiviral activity[1].
SARS-CoV-2 3CLpro-IN-1 (Compound 14c) is a potent inhibitor of SARS-CoV-2 3CLpro. 3CLpro (main coronaviruses cysteine-protease) has been identified as a promising target for the development of antiviral drugs. SARS-CoV-2 3CLpro-IN-1 has the potential for the research of infection diseases[1].
Tirfipiravir is a nucleoside compound and antiviral agent, against the novel coronavirus or influenza virus[1].
MERS-CoV-IN-1 exhibits excellent inhibitory activity against coronavirus. MERS-CoV-IN-1 is useful as a pharmaceutical composition for preventing coronavirus-induced diseases (MERS-CoV and SARS) (extracted from patent WO2018174442A1, compound 1)[1].
SARS-CoV-2 3CLpro-IN-3 (Compound 3d) is a SARS CoV-2 3CLpro inhibitor with antiviral, antibacterial and antifungal activities[1].
Cleistanthin B (Diphyllin O-glucoside) is an orally active arylnaphthalene lignan lactone glycoside. Cleistanthin B exhibits anti-SARS-CoV-2 effects in Vero cells, with EC50 of 6.51 µM. Cleistanthin B also exhibits antitumor, diuretic and antihypertensive effects in vivo[1][2][3][4].
Methyl tanshinonate is a tanshinone, that can be isolated from Salvia miltiorrhiza (S. miltiorrhiza) Bunge (Lamiaceae). Methyl tanshinonate is a potent inhibitor of Mpro enzyme in SARS-CoV (IC50 = 21.1 µM). Methyl tanshinonate can be used for diabetes and SARS-CoV research[1][2][3].
Ritonavir-d6 (ABT 538-d6) is the deuterium labeled Ritonavir. Ritonavir (ABT 538) is an inhibitor of HIV protease used to treat HIV infection and AIDS. Ritonavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.61 μM[1][2].
INSCoV-600K(1) is a potent inhibitor of Mpro (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)[1].
2-Hydroxyacetophenone is a principal root volatile of the Carissa edulis[1]. 2-Hydroxyacetophenone shows inhibitory effects on infection of HIV/SARS-CoV S pseudovirus with an IC50 of 1.8 mM[2].
MMT5-14 is a remdesivir analogue with a higher antiviral activity in four variants of SARS-CoV-2 than Remdesivir (HY-104077). MMT5-14 inhibits SARS-CoV-2, α, β, γ and δ variants with EC50s of 0.4, 2.5, 15.9, 1.7 and 5.6 μM, respectively. MMT5-14 can be used for the research of COVID-19[1].
Z-FA-FMK ((1S)-Z-FA-FMK; Compound 6) is a broad-spectrum halomethyl ketone inhibitor sgainst Coronavirus (SARS-CoV) main protease 3CL with a Ki of 25.7 μM[1].
SARS-CoV-2 3CLpro-IN-4 (Compound 5g) is a SARS CoV-2 3CLpro inhibitor with antiviral, antibacterial and antifungal activities[1].
SARS-CoV-2-IN-35 is a potent and orally active SARS-CoV-2 M pro inhibitor with a Ki value of 12.1 nM. SARS-CoV-2-IN-35 can be used in research of COVID-19[1].
BC-11 hydrobromide is a selective TMPRSS2 inhibitor (TMPRSS2 is a key host cellular factor for viral entry and SARS-CoV-2 pathogenesis), and a selective urokinase (uPA) inhibitor (IC50=8.2 μM). BC-11 hydrobromide is cytotoxic to triple-negative MDA-MB231 breast cancer cells. BC-11 hydrobromide is used in research on viral infections and cancer[1][2][3].
EIDD-2749 (4'-Fluorouridine) is an orally active, low cytotoxic and broad-spectrum mononegavirus inhibitor (SI≥1877). EIDD-2749 effectively blocks the replication of respiratory syncytial virus (RSV) and SARS-CoV-2. EIDD-2749 can be used in the study of RSV, SARSCoV-2 and related RNA virus infections[1].
Amantadine (1-Adamantanamine) sulfate is an orally avtive and potent antiviral agent with activity against influenza A viruses. Amantadine sulfate inhibits several ion channels such as NMDA and M2, and also inhibits Coronavirus ion channels. Amantadine sulfate also has anti-orthopoxvirus and anticancer activity. Amantadine sulfate can be used for Parkinson's disease, postoperative cognitive dysfunction (POCD) and COVID-19 research[1][2][3][4][5][6].
ML188, a first in class probe, is a selective non-covalent SARS-CoV 3CLpro inhibitor with an IC50 of 1.5 μM. Antiviral activity[1].
GS-621763, an orally bioavailable prodrug of GS-441524, shows antiviral activity against SARS-CoV-2 pathogenesis in mice.
Masavibart (ZRC3308-A7) is an anti-SARS-CoV-2 monoclonal antibody (IgG1 type). Masavibart shows good binding affinity to a non-competing epitope on the RBD of the SARS-CoV-2 spike protein. Masavibart can be used in combination with ZRC3308-B10 (HY-145643) at a ratio of 1:1, which is effective for the prevention of COVID-19 and the early stage of COVID-19 before the development of severe disease[1].
SARS-CoV-2-IN-66 (1), a vitaminK derivative, is a SARS-CoV-2 inhibitor, with an EC50 of 70.8 μM in VeroE6/TMPRSS2 cells[1].
SARS-CoV-2-IN-20 (Compound 1a) is a potent inhibitor of SARS-CoV-2 with an EC50 of 6.5 μM. SARS-CoV-2-IN-20 has the potential for the research of infection diseases[1].
Kansuinine B inhibits IL-6-induced Stat3 activation. Kansuinine B possesses anti-viral activity and could be used in the study for COVID-19[1][2][3].