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.

SARS-CoV-2/MERS Mpro-IN-1 is a potent inhibitor of the main proteases in SARS-CoV-2 and MERS, with IC50 values of 0.10 and 0.06 µM, respectively.

SARS-CoV-2/MERS Mpro-IN-2 is a potent inhibitor of the main proteases of SARS-CoV-2 and MERS, with IC50 values of 0.21 and 0.07 µM, respectively.

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.

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].

Mpro inhibitor N3 hemihydrate is a potent antagonist of the SARS-CoV-2 main protease (Mpro), with an EC50 of 16.77 μM against SARS-CoV-2. It specifically inhibits Mpro in various coronaviruses, including SARS-CoV, MERS-CoV, HCoV-229E (IC50 4.0 μM), FIPV (IC50 8.8 μM), and MHV-A59 (IC50 2.7 μM) [1][2].

Remdesivir nucleoside monophosphate, a metabolite of Remdesivir, is a potent antiviral compound with nucleoside analogue characteristics. It exhibits effective antiviral activity against both SARS-CoV and MERS-CoV.

MM3122 (MM-3122) is a selective type II transmembrane serine protease (TMPRSS2) inhibitor, IC50 = 0.34 nM. MM3122 effectively blocks TMPRSS2, thereby inhibiting the entry of SARS-CoV-2 and MERS-CoV into human cells.

E 64c (EP 475) , a derivative of E-64, is an irreversible and membrane-permeant cysteine protease inhibitor.

Vincapusine is a natural inhibitor of 3C-like protease (3CLpro), targeting SARS-CoV-2 3CLpro, SARS-CoV 3CLpro and MERS-CoV 3CLpro.

UAWJ9-36-3 is a SARS-CoV-2 Protease inhibitor (IC50 = 54 nM). UAWJ9-36-3 showed potent binding and enzymatic inhibition against the Mpro's from SARS-CoV-2, SARS-CoV, MERS-CoV, HCoV-OC43, HCoV-NL63, HCoV-229E, and HCoV-HKU1. UAWJ9-36-3 is a promising candidate to be further developed as a broad-spectrum coronavirus antiviral.

UAWJ9-36-1 is a SARS-CoV-2 Protease inhibitor (IC50 = 51 nM). UAWJ9-36-1 showed potent binding and enzymatic inhibition against the Mpro's from SARS-CoV-2, SARS-CoV, MERS-CoV, HCoV-OC43, HCoV-NL63, HCoV-229E, and HCoV-HKU1. UAWJ9-36-1 is a promising candidate to be further developed as a broad-spectrum coronavirus antiviral.

Blancoxanthone is a molecule isolated from plants could also be potential drug candidates against COVID-19. Moreover, these could also show promising inhibitory effects against influenza-parainfluenza viruses, respiratory syncytial virus, severe acute respiratory syndrome (SARS), and Middle East respiratory syndrome coronavirus (MERS-CoV).

SARS-CoV-2 3CLpro-IN-10(5d) is a potent inhibitor of the SARS-CoV-2 3CL protease with an IC50 value of 190 nM and demonstrates broad-spectrum antiviral activity, exhibiting IC50 values of 790 nM for SARS-CoV-1 and 70 nM for MERS-CoV.