mers-cov

MERS-CoV-IN-1 exhibits excellent inhibitory activity against coronavirus and is useful as a pharmaceutical composition for preventing coronavirus-induced diseases (MERS-CoV and SARS).

Remdesivir (GS-5734) is a nucleoside analog, a broad-spectrum antiviral compound that exerts its activity by inhibiting the RNA-dependent RNA polymerase of viruses. Remdesivir is active against Ebola, SARS, and MERS viruses, and is potentially therapeutic against COVID-19.

MERS-CoV-IN-2 (compound 3c) is an inhibitor of MERS-CoV 3CLpro with an IC50 of 17 nM. It exhibits antiviral activity against SARS-CoV-2 and MERS-CoV by binding to the active site of the 3CLpro enzyme, specifically at the S4 subsite, thereby inhibiting the enzyme's activity.

Anti-MERS-CoV Spike Antibody (3I167) is a Rabbit IgG monoclonal antibody targeting MERS-CoV MERS-CoV Spike.

Anti-MERS-D12 mAb is a fully human monoclonal neutralizing antibody isolated from a recovered patient. It binds specifically to the receptor-binding domain (RBD) of the MERS-CoV spike glycoprotein with extremely high affinity, effectively blocking the interaction between the virus and the host receptor dipeptidyl peptidase 4 (DPP4). This action exerts potent neutralizing activity by preventing viral attachment and entry into host cells.

Bonducellpin D may show inhibitory activities on the Para3 virus. It also exhibits moderate activity against four tested human cancer cell lines, HepG-2, K562, HeLa, and Du145.

Molnupiravir (EIDD-2801) is an isopropyl ester prodrug of the ribonucleoside analog EIDD-1931 with oral bioavailability. Molnupiravir can be used in the study of COVID-19, seasonal and pandemic influenza, and has broad-spectrum antiviral activity against multiple coronaviruses and influenza viruses, such as SARS-CoV-2, MERS-CoV, SARS-CoV.

EIDD-1931 (Beta-d-N4-hydroxycytidine) is a ribonucleoside analog with antiviral activity that inhibits the replication of severe acute respiratory syndrome coronavirus [SARS-CoV] in Vero 76 cells, Middle East respiratory syndrome coronavirus [MERS-CoV] in Calu-3 2B4 cells, and SARS-CoV-2 in Vero cells (IC50s = 0.1, 0.15, and 0.3 μM, respectively).

SARS-CoV-2-IN-1 is a potent inhibitor of Mpro [SARS-CoV-2 Mpro, SARS-CoV Mpro, and MERS-CoV Mpro] with IC50 values of 0.67, 0.90, and 0.58 μM, respectively.

PLpro-IN-5 (compound 21), serving as a PLPro protease inhibitor, boasts an IC50 of 91.14 nM. This compound exhibits a broad-spectrum antivirus efficacy, particularly effective against SARS-CoV, MERS-CoV, and SARS-CoV-2.

PAMAM dendrimer G1.5 carboxylate (PAMAM G1.5 carboxylate) sodium is a polyanionic dendrimer composed of sodium terminal carboxylate groups. It has demonstrated antiviral activity in MERS-CoV plaque reduction assays, with an inhibition rate of 40.5%.

TDI-015051 is an orally active inhibitor of SARS-CoV-2 non-structural protein 14 (SARS-CoV-2 NSP14) with an IC50 of ≤0.15 nM. It effectively inhibits SARS-CoV-2 NSP14 in Huh-7.5 cells (EC50=11.4 nM) and A549 cells expressing ACE2-TMPRSS2 (EC50=64.7 nM). Additionally, TDI-015051 suppresses other coronaviruses such as α-hCoV-NL63, α-hCoV-229E, and β-hCoV-MERS with IC50 values of 1.7, 2.6, and 3.6 nM, respectively. This compound inhibits viral RNA methylation and replication by binding to a stable SAH-cap pocket and demonstrates anti-infection activity in mouse models.

SARS-CoV-2 Mpro-IN-37 (compound 8r) is an inhibitor of the SARS-CoV-2 main protease (Mpro), with an IC50 value of 0.0199 μM. It exhibits IC50 values of 0.00945 μM against SARS-CoV-1 Mpro and 0.111 μM against MERS-CoV Mpro. SARS-CoV-2 Mpro-IN-37 demonstrates potent antiviral activity in the nanomolar range without showing cytotoxicity.

TMP1 is an orally active dual inhibitor targeting M pro (IC50= 312.5 nM) and TMPRSS2 (IC50= 1.28 μM, KD= 10.10 μM). It shows broad-spectrum protective effects in vitro against various SARS-CoV-2 variants. In vivo, TMP1 provides cross-protection against highly pathogenic coronaviruses, including SARS-CoV-1, SARS-CoV-2, and MERS-CoV, and effectively blocks the transmission of SARS-CoV-2. Additionally, TMP1 can inhibit the infection of SARS-CoV-2 escape mutants resistant to Nivolumab. TMP1 is useful in coronavirus research.

TPG-20A is an inhibitor of the SARS-CoV-2 main protease with an IC50 value of 27.8 nM. It also inhibits the main protease of MERS-CoV. TPG-20A is applicable for infection-related research, including studies on SARS-CoV-2.

SCR005 is a synthetic carbohydrate receptor (SCR) with broad-spectrum antiviral activity. It inhibits the entry of enveloped viruses from several families, including Coronaviridae (SARS-CoV-1, SARS-CoV-2, MERS-CoV), Filoviridae (EBOV, MARV), and Paramyxoviridae (NiV, HeV), as well as the glycosylated non-enveloped rotavirus. SCR005 binds to viral envelope N-glycans, blocking the virus from attaching to host cells or disrupting both attachment and membrane fusion. It demonstrates a preventive effect in hACE2 mice infected with SARS-CoV-2. SCR005 is applicable for the study and prevention of enveloped viral pandemics.

SARS-CoV-2 Mpro-IN-50 (Compound 30) is a non-covalent inhibitor of SARS-CoV-2 Mpro with an IC50 of 14 nM. This compound also serves as a pan-coronavirus Mpro inhibitor, showing IC50 values ranging from 20 to 190 nM against SARS-CoV-1 Mpro, 229E Mpro, HKU1 Mpro, MERS Mpro, NL63 Mpro, and OC43 Mpro. It exhibits significant antiviral activity against the SARS-CoV-2 omicron variant (EC50: 22 nM). SARS-CoV-2 Mpro-IN-50 is useful for coronavirus infection research.

SCR007 is a synthetic carbohydrate receptor (SCR) known for its broad-spectrum antiviral activity. It inhibits the entry of enveloped viruses across several families, including coronaviruses (SARS-CoV-1, SARS-CoV-2, MERS-CoV), filoviruses (EBOV, MARV), and paramyxoviruses (NiV, HeV), as well as glycosylated non-enveloped rotaviruses. SCR007 targets the N-glycans on virus envelopes, blocking viral attachment to host cells or hindering both attachment and membrane fusion. It exhibits preventive effects in hACE2 mice infected with SARS-CoV-2 and can be employed for research and prevention of pandemics caused by enveloped viruses.

SARS-CoV-2 Mpro-IN-52 (compound 47) is a potent inhibitor of the SARS-CoV-2 main protease (MPro) with an EC50 of 0.0099 µM, exhibiting antiviral activity. It shows strong and broad-spectrum activity against MERS, OC43, and 229E, with EC50 values of 0.00961, 0.138, and 0.117 µM, respectively. SARS-CoV-2 Mpro-IN-52 is applicable for COVID-19 research.

Chlorphenoxamine hydrochloride is an antihistamine and anticholinergic agent that also acts as a GPCR antagonist. It can suppress various deadly viral diseases such as SARS-CoV, MERS-CoV, Ebola virus (EBOV), and malaria. The compound exhibits anti-filovirus activity against both EBOV and Marburg virus (MARV), with IC50 values of 1.1 μM and 6.2 μM, respectively. Chlorphenoxamine hydrochloride is utilized in research related to allergic disorders, urticaria, viral diseases, and Parkinson's disease.

SB-140 is a selective and covalent PLpro inhibitor with an IC50 of ≤2.5 nM against SARS-CoV-2 PLpro. It exhibits antiviral activity against SARS-CoV-2, MERS-CoV, and SARS-CoV-1.

(M)-AVI-4773 is an orally active inhibitor of the coronavirus MPro that can cross the blood-brain barrier, exhibiting an IC50 of 2.5 nM for SARS-CoV-2 MPro. In mouse models infected with MERS-CoV and SARS-CoV-2, (M)-AVI-4773 quickly demonstrates antiviral effects.

Dihydrotanshinone I (DHTS) is a natural compound extracted from Salvia miltiorrhiza Bunge used for treating of cardiovascular diseases.

Anti-MERS-3A1 mAb (MERS-3A1) is a high-affinity human IgG1 monoclonal antibody derived from CHO cells that effectively inhibits the interaction between the MERS-CoV spike protein and the DPP4 receptor[1].