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].
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].
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].
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].
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].
PLpro/RBD-IN-1 (compound 5) is a dual SARS-CoV-2 PLpro and spike protein RBD inhibitor with IC50s of 7.197 μM and 8.673 μM, respectively[1].
SARS-CoV-2-IN-15 (compound 11) is a potent inhibitor of SARS-CoV-2 with an IC50 of 0.49 μM. SARS-CoV-2-IN-15 is a niclosamide analogue. SARS-CoV-2-IN-15 contains higher stability in human plasma and liver S9 enzymes assay than niclosamide, which can improve bioavailability and half-life when administered orally[1].
F8-S43-S3 is an inhibitor of SARS-CoV-2 main protease, with an IC50 of 9.69 μM[1].
CDD-1845 is a non-covalent and non-peptide potent SARS-CoV-2 Mpro inhibitor with a Ki of 3 nM. CDD-1845 also inhibits ΔP168, A173V, and ΔP168/A173V Mpro variants[1].
Z-Arg-Leu-Arg-Gly-Gly-AMC is a peptide substrate of SARS-CoV PLpro[1].
Ivermectin B1a, a derivative of Avermectin B1a (HY-15308), is a main component of Ivermectin (HY-15310)[1]. Ivermectin (MK-933) is a broad-spectrum anti-parasite agent. Ivermectin is a candidate therapeutic against SARS-CoV-2/COVID-19[2].
INSCoV-614(1B) is a potent inhibitor of Mpro (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)[1].
Antioxidant agent-9 is a peptide with the sequence Asp-Trp. Antioxidant agent-9 shows antioxidant activity. Antioxidant agent-9 also is potential as SARS-CoV-2 antiviral, with an affinity strength equal to Chloroquine (HY-17589A) and Favipiravir (HY-14768)[1][2].
Teicoplanin sodium (Antibiotic MDL-507 sodium) is a potent lipoglycopeptide antibiotic. Teicoplanin sodium shows antiviral activity for HIV-1, SARS-CoV1 and SARS-CoV2. Teicoplanin sodium shows anti-MRSA activity[1][2].
Bofutrelvir (FB2001) is a SARS-CoV-2 main protease Mpro inhibitor with an IC50 value of 53 nM and an EC50 value of 0.53 μM. Bofutrelvir exhibits potent antiviral efficacy against several current SARS-CoV-2 variants with EC50 values of 0.26-0.42 μM. Bofutrelvir has an additive antiviral effect when combined with Remdesivir (HY-104077)[1][2].
SARS-CoV-2-IN-59 (compound E07), an imidazoline derivative, is a non-peptide small molecule inhibitor of SARS-CoV-2 that targets the main protease (Mpro) of the coronavirus. SARS-CoV-2-IN-59 has a strong interaction with residues on Mpro (Met 165, Gln 166, Met 165, His 41, Gln 189)[1].
SARS-CoV-2-IN-18 (Compound 26) is a potent SARS-CoV-2 3C-like protease inhibitor with an IC50 of 45 nM[1].
Propiolactone (β-propiolactone; 2-Oxetanone) is a viral chemical inactivator that causes the infectious inactivation of viruses. Propiolactone was co-incubated with SARS-CoV at a ratio of 1:1000 (v:v) and used as a bacteriostatic agent to formulate the BPL-inactivated influenza virus vaccine (Flu-BPL)[1][2].
Bananin is an effective inhibitor of the ATPase activity of the SARS Coronavirus helicase with an IC50 value of 2.3 μM.
SARS-CoV-2-IN-14 (compound 6) is a potent inhibitor of SARS-CoV-2 with an IC50 of 0.39 μM. SARS-CoV-2-IN-14 is a niclosamide analogue. SARS-CoV-2-IN-14 contains higher stability in human plasma and liver S9 enzymes assay than niclosamide, which can improve bioavailability and half-life when administered orally[1].
Clazakizumab is a monoclonal antibody with high affinity and specificity for the IL-6 (interleukin-6) cytokine. Clazakizumab may be helpful in inhibiting the cytokine response to SARS-CoV-2 in COVID-19. Clazakizumab can be used for the research of psoriatic arthritis (PsA) and renal antibody-mediated rejection[1][2].
SARS-CoV-2-IN-63 (Compound R3e) is an inhibitor of SARS-CoV-2 replication and has low cytotoxicity. SARS-CoV-2-IN-63 inhibits viral replication in Vero E6 cells and Calu-3 cells, with EC50 values of 1.99 μM and 1.92 μM, respectively[1].
SARS-CoV-2-IN-13 (compound 5) is a potent inhibitor of SARS-CoV-2 with an IC50 of 0.057 μM. SARS-CoV-2-IN-13 is a niclosamide analogue. SARS-CoV-2-IN-13 contains higher stability in human plasma and liver S9 enzymes assay than niclosamide, which can improve bioavailability and half-life when administered orally[1].
Aranotin strongly binds to Nsp15 viral protein. Aranotin can be used as promising SARS-CoV-2 replication strong inhibitor. Aranotin has the potential for COVID-19 research[1].
PB28 is a cyclohexylpiperazine derivative and a high affinity and selective sigma 2 (σ2) receptor agonist with a Ki of 0.68 nM. PB28 is also a σ1 antagonist with a Ki of 0.38 nM. PB28 is less affinity for other receptors. PB28 inhibits electrically evoked twitch in guinea pig bladder and ileum with EC50 values of 2.62 μM and 3.96 μM, respectively. PB28 can modulate SARS-CoV-2-human protein-protein interaction. PB28 induces caspase-independent apoptosis and has antitumor activity[1][2][3][4][5].
Pomotrelvir (PBI-0451) is a selective, orally active SARS-CoV-2 3CL protease inhibitor. Pomotrelvir has antiviral activity and can be used in the research of novel coronavirus (COVID-19)[1].
Vanillinbananin is an effective inhibitor of the ATPase activity of the SARS Coronavirus helicase with an IC50 value of 0.68 μM.
NHC-diphosphate is an active phosphorylated intracellular metabolite of β-d-N4-Hydroxycytidine (NHC) (HY-125033) as a diphosphate form[1]. NHC is a pyrimidine ribonucleoside and behaves as a potent anti-virus agent. NHC effectively inhibits the replication of venezuelan equine encephalitis virus (VEEV), Chikungunya virus (CHIKV) and hepatitis C virus (HCV)[1].