Tirfipiravir is a nucleoside compound and antiviral agent, against the novel coronavirus or influenza virus[1].
SARS-CoV-2 3CLpro-IN-3 (Compound 3d) is a SARS CoV-2 3CLpro inhibitor with antiviral, antibacterial and antifungal activities[1].
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].
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-16 (Compound 12) is a potent SARS-CoV-2 nucleocapsid protein (NPro) inhibitor. SARS-CoV-2-IN-16 exhibits potent anti-viral activity with the EC50 of 3.69 μM. SARS-CoV-2-IN-16 binds to NPro with the low KD value of 7.82 μM, suggesting that SARS-CoV-2-IN-16 is a potent NPro ligand[1].
Adintrevimab (ADG 20) is a human IgG1 monoclonal SARS-CoV (SARS-CoV) antibody. Adintrevimab inhibits SARS-CoV-2 variants and other SARS-like coronaviruses with pandemic potential[1].
Chloroquine dihydrochloride is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine dihydrochloride is an autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine dihydrochloride is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC50=1.13 μM)[1][2][3][4].
SARS-CoV-2 nsp13-IN-6 (compound C5) is a potent SARS-CoV-2 non-structural protein 13 (nsp13) inhibitor with IC50 values of 27 and 33 μM for ssDNA+ ATPase and ssDNA- ATPase. SARS-CoV-2 nsp13-IN-6 can be used for researching anti-COVID-19[1].
Nepuvibart (ZRC3308-B10) is an anti-SARS-CoV-2 monoclonal antibody (IgG1 type). Nepuvibart shows good binding affinity to a non-competing epitope on the RBD of the SARS-CoV-2 spike protein. Nepuvibart can be used in combination with ZRC3308-A7 (HY-145642) 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].
Zevotrelvir (Compound 52) is a coronavirus inhibitor with IC50 ranges of <0.1 μM and <0.1mM for 229E hCoV and SARS-CoV-23C-like (3CL) proteases, respectively. Zevotrelvir has the potential to study viral infections[1].
Arbemnifosbuvir is a nidovirus DdRp-associated nucleotidyltransferase (NiRAN) domain of non-structural protein 12 (nsp12)-interfering drugs. Arbemnifosbuvir can be used for SARS-CoVs infection research[1].
Cichoriin is an active compounds against SARS-CoV-2, and may be a potential candidate in treating severe COVID-19[1].
M56-S2 iodide is a SARS-CoV-2 Mpro inhibitor (IC50=4.0 μM). M56-S2 iodide showed good oral bioavailability and low toxicity in ADMET prediction. M56-S2 iodide has good drug potential and can be used in antiviral (such as SARS-CoV-2) research[1].
Ipomoeassin F is a potent and selective endoplasmic reticulum (ER) protein-translocation inhibitor by targeting the pore-forming subunit of the Sec61 complex (Sec61α) at the ER membrane. Ipomoeassin F selectively inhibits the ER membrane translocation of SARS-CoV-2 proteins. Ipomoeassin F block the ER translocation of secretory proteins and type I transmembrane proteins (TMPs), but not type III TMPs[1][2][3].
SARS-CoV-2 nsp13-IN-5 (compound C6) is a potent SARS-CoV-2 nsp13 inhibitor with IC50 values of 50 and 55 μM for ssDNA+ ATPase and ssDNA- ATPase. SARS-CoV-2 nsp13-IN-5 can be used for researching anti-COVID-19[1].
ATV006 is a potent, orally active antiviral agent and ester prodrugs of GS-441524. ATV006 inhibits the replication of SARS-CoV-2 and its variants. ATV006 can be used for SARS-CoV-2 research[1].
SARS-CoV-2 Mpro-IN-6 is a covalent, irreversible and selective SARS-CoV-2 Mpro inhibitor with an IC50 of 0.18 μM. SARS-CoV-2 Mpro-IN-6 does not inhibit human cathepsins B, F, K, and L, and caspase 3[1].
SARS-CoV-2 Mpro-IN-12 (compound D026) is a SARS-CoV-2 main protease (Mpro) inhibitor with antiviral activities[1].
GRL0617 is a potent, selective and competitive noncovalent inhibitor of severe acute respiratory syndrome (SARS-CoV) papain-like protease (PLpro)/deubiquitinase, with an IC50 of 0.6 μM, and with a Ki of 0.49 μM[1].
SARS-CoV-2-IN-19 (Compound 6g) is a potent inhibitor of SARS-CoV-2 with an EC50 of 8.8 μM. SARS-CoV-2-IN-19 shows potent activity against SARS-CoV-2 helicase (nsp13), a highly conserved enzyme, highlighting a potentiality against emerging HCoVs outbreaks. SARS-CoV-2-IN-19 has the potential for the research of infection diseases[1].
Paritaprevir (ABT-450) dihydrate is a potent, orally active and antiviral non-structural protein 3/4A (NS3/4A) protease inhibitor with EC50s of 1 and 0.21 nM against HCV 1a and 1b, respectively. Paritaprevir dihydrate is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.31 μM. Paritaprevir dihydrate is metabolized primarily by cytochrome P450 (CYP) 3A. The plasma concentration and half-life of Paritaprevir dihydrate can be enhanced by Ritonavir (a CYP450 inhibitor)[1][2][3][4].
Ketotifen (HC 20-511) is an orally active second-generation noncompetitive histamine 1 (H1) receptor blocker and mast cell stabilizer. Ketotifen can block 6-phosphogluconate dehydrogenase (PGD) in vitro. Ketotifen also has antiviral activity against SARS-CoV-2 and Influenza virus. Ketotifen can be used to the research of autoimmune encephalomyelitis (EAE) and asthma attack prevention[1][2][3][4].
SARS-CoV-2-IN-69 (Compound 7E) is a non-covalent SARS-CoV-2 inhibitor with an EC50 value of 7.4 μM. SARS-CoV-2-IN-69 is a potent inhibitor of SARS-CoV-2 main protease (Mpro) and a non-covalent inhibitor of papain (PLpro)[1].
Regdanvimab (CT-P59) is a human monoclonal antibody that targets the receptor-binding domain of SARS-CoV-2 spike protein, blocking interaction with ACE2 for viral entry. Regdanvimab can be used for the research of COVID-19[1].
SARS-CoV-2-IN-9 is an inhibitor binding to subsites S1 and S2 in SARS-CoV-2 main protease.
Tanshinlactone is a seco-abietanoid that can be isolated from Salvia miltiorrhiza. Tanshinlactone is a coronavirus (CoV) inhibitor. Tanshinlactone modulates interleukin-2 and interferon-γ gene expression[1][2].
Tectoquinone (2-Methylanthraquinone) is a SARSCoV-2 main protease inhibitor against COVID-19. Tectoquinone exhibits strong mosquito larvicidal activity with the LC50 values of 3.3 and 5.4 μg/ml against A. aegypti and A. albopictus in 24 h, respectively[1][2].
PLpro inhibitor is a potent inhibitor of papain-like protease (PLpro) with IC50 of 2.6 uM.IC50 Value: 2.6 uM [1]Target: PLpro; SARS-CoVin vitro: PLpro inhibitor is a potent inhibitor against the papain-like protease (PLpro) from the coronavirus that causes severe acute respiratory syndrome (SARS-CoV). PLpro inhibitor was found to have IC50 value of 2.6 ± 0.1 μM. PLpro inhibitor display significant antiviral activity with EC50 values of 13.1±0.7 uM, without toxicity up to the highest concentration tested. Notably, the increasing antiviral potency correlates with the in vitro inhibition of PLpro, suggesting that the compounds work directly on the enzyme in cells [1,2].in vivo:
Plonmarlimab (TJ003234) is an anti-GM-CSF monoclonal antibody. Plonmarlimab can be used for research of rheumatoid arthritis and COVID-19[1][2].
Enoxaparin (PK 10169), a low-molecular-weight heparin (LMWH) derivative. Enoxaparin exerts anticoagulant activity through antithrombin III, an endogenous inhibitor of factor Xa and thrombin IIa. Enoxaparin protect the rat hippocampus against TBI (traumatic brain injury) via antioxidant and anti-inflammatory properties. Enoxaparin can be used for the research of deep vein thrombosis (DVT), pulmonary embolism, TBI and COVID-19[1][2][3].