Vanillinbananin is an effective inhibitor of the ATPase activity of the SARS Coronavirus helicase with an IC50 value of 0.68 μM.
Bepridil ((±)-Bepridil) is a calcium channel blocking agent used as antiarrhythmic agent. Bepridil inhibits both calcium and sodium currents, has research potential in certain ischemia-induced ventricular arrhythmias. Bepridil also has strong inhibition of SARS-CoV-2 from entry and replication inside Vero E6 and A549 cells[1][2].
SDZ 224-015 is an orally active inhibitor of the interleukin-1 beta (IL-1β) converting enzyme and caspase-1. SDZ 224-015 possesses anti-COVID-19 activity, targeting Mpro (IC50 of 30 nM)[1][2].
Mefloquine (Mefloquin), an orally active and potent quinoline antimalarial agent, is an anti-SARS-CoV-2 entry inhibitor. Mefloquine is also a K+ channel (KvQT1/minK) antagonist with an IC50 of ~1 μM. Mefloquine can be used for malaria, systemic lupus erythematosus and cancer research[1][2][3].
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 However, Bamlanivimab is withdrawn in April 2021 following the rise of SARS-CoV-2 virus variants resistant to Bamlanivimab[1].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).
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].
YH-53 is a potent 3CLpro inhibitor with Ki values of 6.3 nM, 34.7 nM for SARS-CoV-1 3CLpro and SARS-CoV-2 3CLpro, respectively. YH-53 strongly blocks the SARS-CoV-2 replication. YH-53 is a peptidomimetic compound with a unique benzothiazolyl ketone. YH-53 has the potential for COVID-19 research[1][2].
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].
Iodobananin is an effective inhibitor of the ATPase activity of the SARS Coronavirus helicase with an IC50 value of 0.54 μM.
HeE1-2Tyr, a pyridobenzothiazole compound, is a flavivirus RNA dependent RNA polymerases (RdRp) inhibitor. HeE1-2Tyr significantly inhibits West Nile, Dengue and SARS-CoV-2 RdRps (IC50 of 27.6 µM) activity in vitro[1][2].
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].
Eubananin is an effective inhibitor of the ATPase activity of the SARS Coronavirus helicase with an IC50 value of 2.8 μM.
Isomitomycin A is a potential inhibitor against SARS-CoV-2. Isomitomycin A targets to the hACE2 binding site of the modelled surface glycoprotein of SARS-CoV-2. Isomitomycin A can be used in studies of COVID-19[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].
SARS-CoV-2 3CLpro-IN-20 (Compound 5g) is a covalent SARS-CoV-2 3CLpro inhibitor (IC50s: 0.43 μM, Ki: ?0.33?μM)[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].
Lopinavir-d8 (ABT-378-d8) is the deuterium labeled Lopinavir. Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity[1][2]. Lopinavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 14.2 μM[3].
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].
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].