Remdesivir nucleoside monophosphate is a metabolite of Remdesivir[1]. Remdesivir is a nucleoside analogue with effective antiviral activity against SARS-CoV and MERS-CoV[2].
XP-59 is a potent inhibitor of the SARS-CoV Mpro, with a Ki of 0.1 μM[1].
Ranitidine bismuth citrate is an orally active Histamine H2-receptor antagonist with an IC50 of 3.3 μM. Ranitidine bismuth citrate has high selectivity for SARS-CoV-2-infected cells. Ranitidine bismuth citrate is a commonly used agent anti-Helicobacter pylori infection with an MIC90 value of 16 ng/L[1][2][3].
Niazinin is a thiocarbamate glycoside with antileishmanial activities, with an IC50 value of 5.25 μM. Niazinin also shows a binding affinity with the target protein 3CL protease. Niazinin has promising leishmanicidal, anti-inflammatory and anti-pyretic activity[1][2].
Saquinavir-d9 (Ro 31-8959-d9) is the deuterium labeled Saquinavir. Saquinavir(Ro 31-8959) is an HIV Protease inhibitor used in antiretroviral therapy. Saquinavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.36 μM[1][2].
Hydroxychloroquine is a synthetic antimalarial agent which can also inhibit Toll-like receptor 7/9 (TLR7/9) signaling. Hydroxychloroquine is efficiently inhibits SARS-CoV-2 infection in vitro[1][2][3].
Plutavimab a humanized IgG1-κ anti-SARS-CoV-2 antibody, targeting to Spike (S) glycoprotein receptor binding domain (RBD)[1][2].
SARS-CoV-2-IN-11 is a potent and nontoxic inhibitor of SARS-CoV-2 3CL protease (3CLpro) with an IC50 and EC50 of 0.17 and 1.45 nM, respectively. SARS-CoV-2 3C-like protease (3CLpro), an enzyme essential for viral replication, is an attractive target for therapeutic intervention. SARS-CoV-2-IN-11 may lead to the emergence of effective SARS-CoV-2-specific antivirals[1].
SARS-CoV-2 Mpro-IN-2 (compound GC-14) is a selective, low cytotoxic and non-covalent Mpro inhibitor (IC50=0.40 μM) with good anti-SARS-CoV-2 activity (EC50=1.1 μM). SARS-CoV-2 Mpro-IN-2 can be used in COVID-19 studies[1].
GS-443902 trisodium (GS-441524 triphosphate trisodium) is a potent viral RNA-dependent RNA-polymerases (RdRp) inhibitor with IC50s of 1.1 µM, 5 µM for RSV RdRp and HCV RdRp, respectively. GS-443902 trisodium is the active triphosphate metabolite of Remdesivir (GS-5734)[1][2].
Gimsilumab (MORAb-022) is a humanized anti-GM-CSF monoclonal antibody. Gimsilumab has the potential for the research of COVID-19 and rheumatoid arthritis (RA)[1][2].
SARS-CoV-2-IN-44, a inhibitor of SARS-CoV-2, inhibits viral replication, with an EC50 of 0.6μM. SARS-CoV-2-IN-44 has no evident cytotoxic effect in Calu-3 cells and can be used for antiviral research[1].
Aviptadil acetate is an analog vasoactive intestinal polypeptide (VIP) with potent vasodilatory effects. Aviptadil acetate induces pulmonary vasodilation and inhibits vascular SMCs proliferation, platelet aggregation. Aviptadil acetate can be used for the research of pulmonary fibrosis, pulmonary arterial hypertension (PAH) and SARS-CoV-2 caused respiratory failure, et al[1].
Kazinol F is a polyphenol from Broussonetia papyrifera. Kazinol F also is an effective Mpro inhibitor. Kazinol F has interaction with both the catalytic residues (His41 and Cys145) of Mpro and exhibits good binding affinity. Kazinol F can be used for the research of COVID-19[1].
SARS-CoV-2-IN-32 (compound 3g) is a COVID-19 inhibitor. SARS-CoV-2-IN-32 shows anti-proliferative activity against cancer cells. SARS-CoV-2-IN-32 exhibits comparatively high binding affinity (-8.8 Kcal/mole) to COVID-19 main protease (Mpro) (PDB ID: 6LU7). SARS-CoV-2-IN-32 can be used in studies of cancer and COVID-19[1].
Z-Leu-Leu-Leu-fluoromethyl ketone (Z-LLL-FMK) is a cysteine protease inhibitor. Z-Leu-Leu-Leu-fluoromethyl ketone inhibits SARS infection. Z-Leu-Leu-Leu-fluoromethyl ketone also protects mice against a T. crassiceps challenge[1][2].
Aplidine (Plitidepsin) is a potent anti-cancer agent by targeting eEF1A2 ( KD=80 nM)[1]. Aplidine possesses antiviral activity and is against SARS-CoV-2 with an IC90 of 0.88 nM. Aplidine is usually used for multiple myeloma and advanced cancer research, and has the potential for COVID-19 research[1][2].
(±)-Alliin is the main active component of garlic. (±)-Alliin is a putative inhibitor of the main protease of SARS-CoV-2 (Mpro)[1].
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].
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].
SARS-CoV-2-IN-38 (compound 24) is a SARS-CoV-2 inhibitor with good oral bioavailability in mice (F%=39.75%)[1].
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].
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.
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].
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].
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].
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].
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].