(±)-Tuaimenal A ((+)-1) is a secondary metabolite and a derivative of Sesamol. (±)-Tuaimenal A has potent inhibitory activity against SARS-CoV-2 3CLpro with an IC50 of 33.3  μM. (±)-Tuaimenal A can be used for SARS-CoV-2 infection research.

AVI-6451 is a novel orally effective SARS-CoV-2 Mac1 (IC50 = 28 nM) inhibitor. AVI-6451 can reduce viral load. AVI-6451 can be used for research on viral infections.

LRH-0003 is an inhibitor of the Macrodomain 1 (Mac1) of nonstructural protein 3 (NSP3) from SARS-CoV-2, with an IC50 value of 1.7 μM. LRH-0003 can be used for the research antiviral infection targeting SARS-CoV-2.

AVI-4206 is a selective Mac1 inhibitor with an lC50 of 64 nM. AVI-4206 reduces viral replication, restores an interferon response, and leads to a survival benefit in an animal model of SARS-CoV-2 infection. AVI-4206 can be used the study of SARS-CoV-2 infection.

FL-166 is a SARS coronavirus main protease (Mpro) inhibitor (Ki: 40 nM). FL-166 exerts its inhibitory effect by targeting a cluster of serine residues near the active site of the protease. FL-166 can be used in the study of SARS-CoV.

TPG-20A is a SARS-CoV-2 main protease inhibitor with an IC50 of 27.8 nM. TPG-20A also inhibits MERS-CoV main protease. TPG-20A can be used for the research of infection, such as SARS-CoV-2.

TMP1 is an orally active bispecific inhibitor of M pro (IC50 = 312.5 nM)/TMPRSS2 (IC50 = 1.28 μM, KD = 10.10 μM). TMP1 exhibits broad protection against different SARS-CoV-2 variants in vitro. TMP1 cross-protects against highly pathogenic coronaviruses (SARS-CoV-1, SARS-CoV-2, and MERS-CoV) in vivo and effectively blocks the transmission of SARS-CoV-2. TMP1 can inhibit infection by SARS-CoV-2 escape mutants that are resistant to Nivolumab. TMP1 can be used in coronavirus research.

M2 ion channel blocker-2 (Compound 10) is a M2 channel blocker. M2 ion channel blocker-2 significantly blocks wild-type and mutant M2 (L27F and V27A) ion channels. M2 ion channel blocker-2 has potent antiviral activity against HCoV-229E (EC50: 4.7  μM in cytopathic effect) but not against influenza A virus. M2 ion channel blocker-2 has no significant inhibition of hERG and cytochrome P450 (CYP1A2, CYP2C19, and CYP3A4) activity.

BBH-4 is a SARS-CoV-2 major protease (MPro) inhibitor. BBH-4 can be used in SARS-CoV-2 infection research.

DNDI-6510 (Compound (S)-x38) is a non-covalent SARS-CoV-2 MPro inhibitor with a IC50 of 0.04 μM. DNDI-6510 has a potent antiviral activity across SARS-CoV-2 and its variants as well as a weak efficacy to SARS-CoV-1. DNDI-6510 significantly improves drug exposure in metabolically humanized mice model (8HUM).

MC12 is a thiazole-based derivative and a SARS-CoV-2 main protease inhibitor (IC50: 77.7 nM). MC12 exhibits inhibitory effects on both SARS-CoV and SARS-CoV-2 main proteases, with low cytotoxicity and good stability. MC12 can be used in the research of anti-COVID-19 drugs.

MolPort-010-778-422 is a high-affinity inhibitor targeting the ACE2 receptor of SARS-CoV-2 virus. MolPort-010-778-422 demonstrates excellent antiviral activity (IC50=8.9 nM). MolPort-010-778-422 is promising for research of SARS-CoV-2.

MePT-S-N-Pme is an inhibitor of SARS-CoV-2 RdRp activity. MePT-S-N-Pme demonstrates a significant reduced reporter activity with an IC50 of 7 μM in HEK 293 cells. MePT-S-N-Pme has a slight inhibitory effect on nucleotidyltransferase activity. MePT-S-N-Pme significantly inhibits SARS-CoV-2 replication in vitro.

Amb929 (ZINC000002782982), a nsp3 ligand, is an anti-SARS-CoV-2 agent. Amb929 inhibits SARS-CoV2-mNG replication in VeroE6 cells with an EC50 of 34.7 µM. Amb929 has limited and moderate cytotoxicity for VeroE6 cells (CC50: 281 µM). Amb929 also inhibits SARS-CoV-2-mNG replication in Human Airway Epithelium (HAE).

SCR007 is a synthetic carbohydrate receptor (SCR) with broad-spectrum antiviral activity. SCR007 inhibits the entry of enveloped viruses across multiple families (Coronaviridae: SARS-CoV-1, SARS-CoV-2, MERS-CoV; Filoviridae: EBOV, MARV; Paramyxoviridae: NiV, HeV) and the glycosylated nonenveloped rotavirus. SCR007 binds viral envelope N-glycans, blocking viral binding to host cells or both binding and membrane fusion. SCR007 exerts prophylactic effects in hACE2 mice infected with SARS-CoV-2. SCR007 can be used for the study and prevention of enveloped virus pandemics.

SCR005 is a synthetic carbohydrate receptor (SCR) with broad-spectrum antiviral activity. SCR005 inhibits the entry of enveloped viruses across multiple families (Coronaviridae: SARS-CoV-1, SARS-CoV-2, MERS-CoV; Filoviridae: EBOV, MARV; Paramyxoviridae: NiV, HeV) and the glycosylated nonenveloped rotavirus. SCR005 binds viral envelope N-glycans, blocking viral binding to host cells or both binding and membrane fusion. SCR005 exerts prophylactic effects in hACE2 mice infected with SARS-CoV-2. SCR005 can be used for the study and prevention of enveloped virus pandemics.

SARSi-4 sodium is a siRNA that markedly inhibited the replication of SARS-associated coronavirus (SCoV).

2-Chloro-2′-deoxyadenosine monophosphate is an anticoronavirus agent. It exhibits significant inhibitory effects against wild-type novel coronavirus, novel coronavirus variants (Beta, Delta, and Omicron strains), and other coronaviruses such as human coronavirus 229E, human coronavirus OC43, human coronavirus NL63, and mouse coronavirus MHV.

ALG-097558 is an orally active 3CLpro inhibitor. ALG-097558 demonstrates pan-coronavirus activity against various SARS-CoV-2 variants as well as other human coronaviruses (HCoVs) such as SARS-CoV-1, α-HCoV 229E, and β-HCoV OC43. ALG-097558 demonstrates potent inhibition with IC50s of 2 nM (SARS-CoV-2 3CLpro) and 6 nM (229E 3CLpro). ALG-097558 demonstrates antiviral activity in the SARS-CoV-2 hamster infection model. ALG-097558 can be used for the study of viral infections[1].

RLA-3107 is an artemisinin regioisomer that blocks ion channels, thereby preventing cations from entering the host cytoplasm. RLA-3107 is also a viroporin inhibitor.

MU-UNMC-2 is a potential small-molecule inhibitor of S-RBD and ACE-2 interaction, shows antiviral activity against SARS-CoV-2 with IC50 of 1.72 uM in human bronchial epithelial cells.

Remdesivir metabolite.Remdesivir blocks SARS-CoV and MERS-CoV in HAE cells with EC50s of both 74 Nm,and also showed potent activity blocking 2019-nCov(Coronavirus).

ZHAWOC25153 (Compound 17o) is a SARS-CoV-2 papain-like cysteine protease (PLpro) inhibitor, with an IC50 of 7 μM. ZHAWOC25153 exhibits antiviral activity and can be used in research within the field of anti-infection.

XJ5 is a non-nucleoside covalent inhibitor of Nsp12 (IC50=0.12 μM), which is the non-structural protein 12 of the virus. XJ5 has the potential to be an antiviral inhibitor of SARS-CoV-2.

WYFA-15 is a sphingomyelin synthase 1 (SMS1) inhibitor that protects mice against lethal SFTSV infection and reduce SARS-CoV-2 replication and pathogenesis. WYFA-15 can be utilized in anti-virus research.

WEHI-P8 is an orally active inhibitor targeting the papain-like protease (PLpro) of coronaviruses. WEHI-P8 againsts SARS-CoV-2 PLpro with an IC50 value of 12 nM. WEHI-P8 has good cellular activity with a EC50 of 298 nM. WEHI-P8 protects mice from SARS-CoV-2 induced long-term symptoms in lung and brain. WEHI-P8 can be used for post-acute sequelae of COVID-19 study.

VK13 (Compound 6) is a potent inhibitor of human cathepsin L (hCatL) with a Ki value of 0.55 nM and SARS-CoV-2 3CLpro (3CL-PR) with a Ki value of 2.6 nM. VK13 exhibits anti-CoV-2 activity with an EC50 of 1.25 μM.

TKB272 is an orally active and selective antiviral agent targeting the main protease (Mpro) of SARS-CoV-2. It effectively blocks the infection and replication of various SARS-CoV-2 strains, including Omicron variants such as XBB.1.5 and EG.5.1. The enzymatic inhibitory activity of TKB272 shows an IC50 of 0.7 µM (against SARS-CoV-2WK-521 Mpro), and its antiviral activity at the cellular level reaches an EC50 as low as 2.6 nM (against BQ.1.1 strain in HeLahACE2-TMPRSS2 cells), with a cytotoxicity CC50 of 98 µM, indicating no apparent toxicity. In addition, TKB272 significantly suppresses the replication of SARS-CoV-2XBB.1.5 in B6.Cg-Tg(K18-hACE2)2-Prlmn/J transgenic mouse models. TKB272 holds promise for research in the field of SARS-CoV-2 infection.

RU-0415529 is an orally active inhibitor for SARS-CoV-2 nonstructural protein 14 (NSP14) with an IC50 of 356 nM. RU-0415529 binds to the SAH-stabilized cap binding pocket, inhibits viral RNA methylation and the viral replication. RU-0415529 exhibits anti-infectious activity in mouse models.

Remdesivir methylpropyl ester analog (GS-5734 methylpropyl ester analog) is a derivative of Remdesivir-resistant mutants. Jun13296 improves lung viral titers, and prevents lung tissue damage in a SARS-CoV-2 infection model.