TH1217 (ZINC1775962367) is a potent and selective dCTPase pyrophosphatase 1 (dCTPase) inhibitor, with an IC50 of 47 nM. TH1217 enhances the cytotoxic effect of cytidine analogues in leukemia cells. TH1217 also could modulate SARS-Cov-2 interactors, so it shows activity of against COVID-19[1][2].
MI-1851 is a potent furin inhibitor. MI-1851 prevents the proteolytic processing of the S protein of SARS-CoV-2 by endogenous flavoprotease in HEK293 cells. MI-185 has antiviral activity[1][2].
SARS-CoV-2-IN-22 is a SARS-CoV-2 pseudovirus entry inhibitor with an IC50 value of 16.96 µM[1].
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].
Bamlanivimab (Anti-Human SARS-CoV-2) is the first COVID-19 monoclonal antibody (mAb) to be granted Emergency Use Authorization (EUA) in November 2020 by the U.S. Food and Drug Administration (FDA). However, Bamlanivimab is withdrawn in April 2021 following the rise of SARS-CoV-2 virus variants resistant to Bamlanivimab[1].
Chloroquine (diphosphate) is an antimalarial and anti-inflammatory drug widely used to treat malaria and rheumatoid arthritis. Chloroquine is an inhibitor of autophagy and toll-like receptors (TLRs).
Viral polymerase-IN-1 hydrochloride, a Gemcitabine (HY-17026) derivative, potently inhibits influenza A and B viruses infection with IC90 values of 11.4-15.9 μM. Viral polymerase-IN-1 hydrochloride is active against SARS-CoV-2 infection. Viral polymerase-IN-1 hydrochloride suppresses influenza virus infection by affecting viral RNA replication/transcription in cells[1].
PLpro-IN-1 (Compound 2) is a SARS-CoV PLpro inhibitor (IC50: 8.7 μM). PLpro-IN-1 can be used for antiviral research[1].
MM3122 is a selective type II transmembrane serine protease (TMPRSS2) inhibitor with an IC50 value of 0.34 nM. MM3122 effectively blocks TMPRSS2, thereby inhibiting the entry of SARS-CoV-2 and MERS-CoV into human cells[1].
D1N52 is a potent SARS-CoV-2 3CLpro inhibitor with an IC50 of 0.53 μM[1].
Rilpivirine (R278474) hydrochloride is a potent and specific diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). Rilpivirine hydrochloride has high antiviral activity against wild-type HIV (EC50=0.4 nM) and mutant viruses (EC50=0.1-2.0 nM). Rilpivirine hydrochloride has a high genetic barrier to resistance development of HIV[1][2].
AT-9010 tetrasodium, a triphosphate active metabolite of AT-527, is a potent inhibitor of NiRAN (a function essential for viral replication). AT-9010 tetrasodium can inhibit SARS-CoV-2 replication[1].
Hispidulin 4'-O-β-D-glucopyranosid, a natural compound, may serve as a potential COVID-19 main protease inhibitor[1].
Alunacedase alfa (HrsACE2; GSK 2586881) is a human recombinant soluble angiotensin-converting enzyme-2 (hrsACE2). Alunacedase alfa is a genetically modified soluble form of ACE2, it decreases cell entry of SARS-CoV-2 competing for membrane-bound ACE2. Alunacedase alfa has the potential for the research of SARS-CoV-2[1][2].
4'-O-Methylbavachalcone is a chalcone isolated from Psoralea corylifolia, inhibits severe acute respiratory syndrome coronavirus (SARS-CoV) papain-like protease (PLpro) activity, with an IC50 of 10.1 μM[1].
HCoV-OC43-IN-1 (Compound IV-16) is a coronavirus HCoV-OC43 inhibitor. HCoV-OC43-IN-1 has antiviral efficacy (EC50: 90 nM). HCoV-OC43-IN-1 inhibits the mRNA level and expression of viral nucleocapsid protein (NP)[1].
Hydroxychloroquine sulfate is a synthetic antimalarial drug which can also inhibit Toll-like receptor 7/9 (TLR7/9) signaling.
SARS-CoV-2 nsp13-IN-3 (Compound C3) is a SARS-CoV-2 non-structural protein 13 (nsp13) small-molecule inhibitor with an IC50 of 32 μM against nsp13 ssDNA+ ATPase[1].
SARS-CoV-2 Mpro-IN-1 (compound 16b-3) is a potent, selective and irreversible inhibitor of SARS-CoV-2 main protease (Mpro), with an IC50 of 116 nM[1].
Rimteravimab (XVR011) is a bivalent VHH-Fc antibody with potent neutralizing activity with high stability, broad coverage and silenced Fc effector functions against the disease caused by SARS-CoV-2[1].
SARS-CoV-2 nsp13-IN-1 (compound C1) is a potent nsp13 (non-structural protein 13) inhibitor. SARS-CoV-2 nsp13-IN-1 only inhibits nsp13 ssDNA+ ATPase, with an IC50 of 6 μM. SARS-CoV-2 nsp13-IN-1 does not inhibit ssDNA- ATPase. SARS-CoV-2 nsp13-IN-1 can be used for COVID-19 research[1].
SSAA09E3 is a SARS-CoV entry inhibitor that inhibits SARS/HIV pseudotyped virus entry with an EC50 of 9.7 μM in 293T cells and inhibits SARS-CoV infection of Vero cells with an EC50 of 0.15 μM[1][2].
SARS-CoV-2 nsp13-IN-2 (Compound C2) is a SARS-CoV-2 non-structural protein 13 (nsp13) small-molecule inhibitor with an IC50 of 42 μM against nsp13 ssDNA+ ATPase[1].
SARS-CoV-2 nsp13-IN-4 (C4 (d)) is a potent and selective nsp13 helicase small-molecule inhibitor and inhibit the ssDNA+ ATPase activity of nsp13 with an IC50 value of 57 μM. SARS-CoV-2 nsp13-IN-4 is druglike molecule with molecular weight of less than 450Da and can provide a broad-spectrum antiviral effect[1].
AMY-101 TFA (Cp40 TFA), 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].
Ogalvibart (C-135-LS) is a humanized anti-SARS-CoV-2 monoclonal antibody (IgG1 type). Ogalvibart binds to the spike (S) glycoprotein receptor-binding domain (RBD) of SARS-CoV-2. Ogalvibart in combination with C144LS (1:1 ratio) shows good preventive activity and can effectively block the development of COVID19 in a rhesus monkey disease model[1].
SARS-CoV-2-IN-62 (Compound R3b) is an inhibitor of SARS-CoV-2 replication and has low cytotoxicity. SARS-CoV-2-IN-62 inhibits viral replication in Vero E6 cells and Calu-3 cells, with EC50 values of 2.97 μM and 3.82 μM, respectively[1].
Z-Phe-Tyr(tBu)-diazomethylketone is a potent cathepsin L inhibitor. Z-Phe-Tyr(tBu)-diazomethylketone mediates reovirus disassembly. Z-Phe-Tyr(tBu)-diazomethylketone decreases viral detection[1][2].
SARS-CoV MPro-IN-2 (compound 15) is a potent inhibitor of SARS-CoV-2 Mpro with an IC50 value of 72.07 nM. The main protease (Mpro) of the virus as the major enzyme processing viral polyproteins contributes to the replication and transcription of SARS-CoV-2 in host cells, and has been characterized as an attractive target in drug discovery. SARS-CoV MPro-IN-2 has the potential for the research of COVID-19[1].
SARS-CoV MPro-IN-1 is a SARS-CoV-2 3CLpro covalent inhibitor, with an IC50 of 40 nM. SARS-CoV MPro-IN-1 shows good anti-SARS-CoV-2-infection activity in cell culture with an EC50 of 0.33 μM. SARS-CoV MPro-IN-1 has the potential for COVID-19 research[1].