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].
Velpatasvir-d7 (GS-5816-d7) is the deuterium labeled Velpatasvir. Velpatasvir (GS-5816) is a novel pan-genotypic hepatitis C virus (HCV) nonstructural protein 5A (NS5A) inhibitor with activity against genotype 1 (GT1) to GT6 HCV replicons. Velpatasvir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 2.16 μM[2].
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].
Gallinamide A is a potent inhibitor of cathepsin L with an IC50 value of 17.6 pM.
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].
Narsoplimab (OMS 721) is a high-affinity fully human immunoglobulin gamma 4 (IgG4) monoclonal antibody that binds MASP-2 and blocks lectin pathway activation. Narsoplimab can be used in research of hematopoietic stem-cell transplantation and SARS-CoV-2[1].
D1N8 is a potent SARS-CoV-2 3CLpro inhibitor with an IC50 and CC50 values of 0.44 μM and >20 μM, respectively. D1N8 has the potential for the research of anti-SARS-CoV-2 agents targeting 3CLpro[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].
TKB245 is a highly potent SARS-CoV-2 Mpro inhibitor that effectively blocks SARS-CoV-2 replication in VeroE6 cells[1].
NK007 is a novel anti-SARS-CoV-2 agent with an EC50 value of 30 nM.
Simpinicline (OC-02), a highly selective nicotinic acetylcholine receptor (nAChR) agonist, shows potent antiviral activity against the SARS-CoV-2 variants in cell culture with an IC50 of 0.04 µM[1].
SARS-CoV-2 Mpro-IN-12 (compound D026) is a SARS-CoV-2 main protease (Mpro) inhibitor with antiviral activities[1].
KW-8232, an orally active anti-osteoporotic agent, and can reduces the biosynthesis of PGE2[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].
10-10-Hydroxyaloin A is potent SARS-CoV-2 inhibitor. 10-Hydroxyaloin A exhibits significant efficacy to bind SARS-Cov-2 Mpro active site[1].
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:
Antiviral agent 5 is an intermediate used in antiviral agents targeting 3C and 3CL proteases including SARS-CoV-2 Mpro.
Plonmarlimab (TJ003234) is an anti-GM-CSF monoclonal antibody. Plonmarlimab can be used for research of rheumatoid arthritis and COVID-19[1][2].
Isojacareubin can be isolated from Hypericum japonicum. Isojacareubin covalently inhibits SARS-CoV-2 3CLpro. Isojacareubin also has anti-helicobacter activity. Isojacareubin inhibits PKC, and suppresses hepatocellular carcinoma metastasis and induces apoptosis[1][2][3].
Ensitrelvir (S-217622) fumarate is the first orally active non-covalent, non-peptidic, SARS-CoV-2 3CL protease inhibitor (IC50=13 nM)[1][2].
Cilgavimab (AZD-1061; COV2-2130) is a humanized SARS-CoV-2-neutralizing monoclonal antibody, can compose monoclonal-antibody combination AZD7442 with Tixagevimab (HY-P99556). Cilgavimab shows protective action on mouse models of SARS-CoV-2 infection[1].