Bonducellpin D is a furanoditerpenoid lactone isolated from Caesalpinia minax. Bonducellpin D exhibits broad-spectrum inhibition potential against SARS-CoV Mpro and MERS-CoV Mpro, with an Ki of 467.11 and 284.86 nM, respectively. Bonducellpin D also exhibits moderate anti-cancer activity in vitro[1][2][3].
EIDD-2801 is an orally bioavailable isopropylester prodrug of the ribonucleoside analog EIDD-1931. EIDD-2801 shows anti-influenza virus and coronaviruses activities. EIDD-2801 has the potential for seasonal and pandemic influenza treatment[1][2].
Antcin-B is a potent inhibitor of 3CLPro with high affinity. Antcin-B can be used in study SARS-CoV-2[1].
Remdesivir O-desphosphate acetonide impurity is an impurity of Remdesivir. Remdesivir (GS-5734), a nucleoside analogue with effective antiviral activity and is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro[1][2].
WU-04 is a non-covalent inhibitor of SARS-CoV-2, targeting the 3CLpro protein. WU-04 has high inhibitory effect on the 3CLpro protein of 6 SARS-CoV-2 variants (Alpha, Beta, Gamma, Delta, Lambda and Omicron) and 2 coronaviruses (SARS-CoV and MERS-CoV)[1].
Imiquimod-d9 is deuterium labeled Imiquimod. Imiquimod (R 837), an immune response modifier, is a selective toll like receptor 7 (TLR7) agonist. Imiquimod exhibits antiviral and antitumor effects in vivo. Imiquimod can be used for the research of external genital, perianal warts, cancer and COVID-19[1][2].
Methylprednisolone is a synthetic corticosteroid with anti-inflammatory and immunomodulating properties.Target: Glucocorticoid ReceptorMethylprednisolone is typically used for its anti-inflammatory effects. Common uses include arthritis therapy and short-term treatment of bronchial inflammation or acute bronchitis due to various respiratory diseases. Methylprednisolone is used both in the treatment of acute periods and long-term management of autoimmune diseases, most notably systemic lupus erythematosus. It is also used for vestibular neuritis [1].After six months the patients who were treated with methylprednisolone within eight hours of their injury had significant improvement as compared with those given placebo in motor function (neurologic change scores of 16.0 and 11.2, respectively; P = 0.03) and sensation to pinprick (change scores of 11.4 and 6.6; P = 0.02) and touch (change scores, 8.9 and 4.3; P = 0.03). Benefit from methylprednisolone was seen in patients whose injuries were initially evaluated as neurologically complete, as well as in those believed to have incomplete lesions [2].
SARS-CoV-2-IN-41 (compound 2) is a potent SARS-CoV-2 3CLpro inhibitor with an IC50 value of 0.022 µM. SARS-CoV-2-IN-41 shows antiviral effect[1].
INSCoV-601I(1) is a potent inhibitor of Mpro (3CLpro). Proteases (PL pro and 3CL pro) are involved with transcription and replication of the virus. INSCoV-601I(1) has the potential for the research of SARS-CoV-2 infection (extracted from patent WO2021219089A1)[1].
SARS-CoV-IN-4 (compound 13) is a potent and specific inhibitor of SARS-CoV nsp14 N7-methyltransferase, with an IC50 of 0.6 μM (SARS-CoV nsp14)[1].
Tipranavir-d4 (PNU-140690-d4) is the deuterium labeled Tipranavir. Tipranavir (PNU-140690) inhibits the enzymatic activity and dimerization of HIV-1 protease, exerts potent activity against multi-protease inhibitor (PI)-resistant HIV-1 isolates with IC50s of 66-410 nM[1][2]. Tipranavir inhibits SARS-CoV-2 3CLpro activity[3].
Etesevimab (JS016) is a recombinant neutralizing human IgG1 anti-SARS-CoV-2 monoclonal antibody[1].
(R)-Hydroxychloroquine is the enantiomer of Hydroxychloroquine[1]. Hydroxychloroquine is a synthetic antimalarial drug which can also inhibit Toll-like receptor 7/9 (TLR7/9) signaling. Hydroxychloroquine is efficiently inhibits SARS-CoV-2 infection in vitro[2][3][4].
SARS-CoV-2-IN-38 (compound 24) is a SARS-CoV-2 inhibitor with good oral bioavailability in mice (F%=39.75%)[1].
6-Thioguanine is an anti-leukemia and immunosuppressant agent, acts as an inhibitor of SARS and MERS coronavirus papain-like proteases (PLpros) and also potently inhibits USP2 activity, with IC50s of 25 μM and 40 μM for Plpros and recombinant human USP2, respectively.
Jaceidin triacetate(compound 54) is a natural compound isolated formmarulabark.Jaceidin triacetatecan inhibitSARS-CoV-2 Mpro, with theIC50of 11.9μM.Jaceidin triacetateinhibits the replication of Sars-Cov-2 Viral in Vero-E6 cells[1][2].
AT-9010 triethylamine, a triphosphate active metabolite of AT-527, is a potent inhibitor of NiRAN (a function essential for viral replication). AT-9010 triethylamine can inhibit SARS-CoV-2 replication[1].
Lomtegovimab (BI 767551) is a humanized anti-SARS-COV-2 spike glycoprotein monoclonal antibody. Lomtegovimab binds and neutralizes SARS-CoV-2. Lomtegovimab shows antiviral efficacy. Lomtegovimab has the potential for the research of COVID-19[1][2].
AMY-101 (Cp40), a peptidic inhibitor of the central complement component C3 (KD = 0.5 nM), inhibits naturally occurring periodontitis in non-human primates (NHPs). AMY-101 (Cp40) exhibits a favorable anti-inflammatory activity in models with COVID-19 severe pneumonia with systemic hyper inflammation[1][2].
2-Hydroxycinnamic acid is isolated from the methanol extract of Cinnamomum cassia. 2-Hydroxycinnamic acid shows inhibitory effects on infection of HIV/SARS-CoV S pseudovirus with an IC50 of 0.3 mM[2]
A potent, mixed sigma2 agonist and sigma1 antagonist with Ki of 0.28 and 13.0 nM, respectively; inhibits cancer cell growth, modulates P-glycoprotein, and synergizes with doxorubicin in MCF7 and MCF ADR cells with IC50 in nanomolar range; increase G0-G1-phase fraction and caspase-independent apoptosis, also reduces P-gp expression.
Setrobuvir (ANA598) is an orally active non-nucleosidic HCV NS5B polymerase inhibitor. ANA-598 inhibits both de novo RNA synthesis and primer extension, with IC50s between 4 and 5 nM. Setrobuvir also shows excellent binding affinity to SARS-CoV-2 RdRp and induces RdRp inhibition[1][2].
(S)-Hydroxychloroquine ((S)-HCQ) is the enantiomer of Hydroxychloroquine[1]. Hydroxychloroquine, a synthetic antimalarial drug, inhibits Toll-like receptor 7/9 (TLR7/9) signaling, and shows efficiently inhibits SARS-CoV-2 infection in vitro[2][3][4].
Antiviral agent 25 (compound 6g) is a new non-peptide analog covalent inhibitor of SARS-CoV-2 3CLpro. Antiviral agent 25 has a strong inhibitory effect on SARS-CoV-2 3CLpro and SARS-CoV-2 PLpro with IC50 values of 0.118 µM, 0.448 µM, respectively. Antiviral agent 25 has antiviral effect on SARS-CoV-2 with an EC50 value of 7.249 µM[1].
SARS-CoV-2-IN-17 (Compound 16) is a potent SARS-CoV-2 nucleocapsid protein (NPro) inhibitor. SARS-CoV-2-IN-17 exhibits potent anti-viral activity with the EC50 of 2.18 μM. SARS-CoV-2-IN-17 binds to NPro with the low KD value of 7.82 μM, suggesting that SARS-CoV-2-IN-17 is a potent NPro ligand[1].
CDD-1733 is a non-covalent and non-peptide potent SARS-CoV-2 Mpro inhibitor with a Ki of 12 nM. CDD-1733 also inhibits ΔP168, A173V, and ΔP168/A173V Mpro variants[1].
Monolaurin (1-Monolaurin) possesses anti-viral and anti-bacterial activity[1][2].
Beludavimab (BMS 4182137; VIR 7832) is a monoclonal antibody targeting the spike glycoprotein of SARS-CoV-2. Beludavimab binds to recombinant spike protein receptor-binding domain (S-RBD) with an EC50 value of 14.9 ng/mL and a Kd of 0.21 nM[1].
Quipazine dimaleate is a 5-HT agonist with a Ki value of 1.4 nM for displaces [3H]GR65630 from 5-HT3R in rat. Quipazine dimaleate shows antiviral activity against SARS-CoV-2 with an EC50 of 31.64 μM. Quipazine dimaleate behaves as a 5-HT3R antagonist in peripheral models. Quipazine dimaleate can be used for neurological disease research[1][2][3][4].
AT-9010, a triphosphate active metabolite of AT-527, is a potent inhibitor of NiRAN (a function essential for viral replication). AT-9010 can inhibit SARS-CoV-2 replication[1].