mpro

SARS-CoV-2 Mpro-IN-9 (compound c7), a nonpeptidic, noncovalent inhibitor of SARS-CoV-2 main protease (Mpro), exhibits potent inhibitory action (IC50 = 0.085 μM) and improved physicochemical and drug metabolism and pharmacokinetics (DMPK) properties. It effectively suppresses viral replication in SARS-CoV-2-infected Vero E6 cells (EC50 = 1.10 μM) and demonstrates low cytotoxicity (CC50 > 50 μM) [1].

MProinhibitor 11b is an inhibitor of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) main protease (MPro; IC50= 0.04 μM in a TR-FRET assay).1It reduces viral yield in the culture supernatant of SARS-CoV-2-infected Vero E6 cells (EC50= 0.72 μM). MProinhibitor 11b also reduces viral RNA copy numbers in the same model when used at concentrations ranging from 1.85 to 50 μM. 1.Dai, W., Zhang, B., Jiang, X.-M., et al.Structure-based design of antiviral drug candidates targeting the SARS-CoV-2 main proteaseScience368(6497)1331-1335(2020)

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].

Coronavirus main protease (Mpro) inhibitor (respective IC50 values are 2.7, 4 and 8.8 μM for MHV-A29, HCoV-229E and FOPV replication in vitro). Inhibits viral cell infection in an MHV plaque reduction assay. Also inhibits SARS-CoV-2 viral cell entry in a plaque reduction assay (IC50 = 16.8 μM).

Mpro inhibitor 818 is a novel fragment-like inhibitor targeting the main protease of SARS-CoV-2, demonstrating antiviral activity in vitro.

Mpro Inhibitor 737 is a novel fragment-based inhibitor targeting the main protease of SARS-CoV-2. It has demonstrated antiviral activity in in vitro models.

Ebselen (CCG-39161) is a organoselenium compound with anti-inflammatory, anti-oxidant and cytoprotective activity. Ebselen acts as a glutathione peroxidase mimetic and is thereby able to prevent cellular damage induced by reactive oxygen species (ROS). In addition, this agent inhibits the activity of a variety of enzymes including nitric oxide synthase (NOS), 5-lipoxygenase, cyclooxygenase, protein kinase C (PKC), NADPH oxidase and gastric H+/K+-ATPase. Furthermore, ebselen may be neuroprotective due to its ability to neutralize free radicals upon NMDA receptor activation thus, reducing lipoperoxidation mediated by glutamate-induced excitotoxicity.

Carmofur (HCFU) is a highly potent acid ceramidase inhibitor, used in the treatment of breast and colorectal cancer. Carmofur has been known to induce leukoencephalopathy.

Bofutrelvir (FB2001) is a SARS-CoV-2 3CL protease inhibitor with antiviral activity for the study of novel coronavirus pneumonia (COVID-19) infections.

SARS-CoV-2 Mpro-IN-2 is a selective SARS-CoV-2M pro inhibitor with an IC50 value of 0.40 μM.SARS-CoV-2 Mpro-IN-2 has good antiviral activity and can be used to study COVID-19.

SARS-CoV-2 Mpro-IN-25 (Compound 3a) is a protease inhibitor for SARS-CoV-2, exhibiting an IC50 value of 0.26 μM. It demonstrates antiviral activity and is useful for research in the field of pneumonia.

SARS-CoV-2 Mpro-IN-31 (Compound 18) is an inhibitor of SARS-CoV-2 MPro with an IC50 of 11 nM. Additionally, this compound effectively inhibits the enzymatic activity of the cysteine proteases cathepsin B and cathepsin L, with IC50 values of 24 nM and 1.8 nM, respectively.

SARS-CoV-2 Mpro-IN-32 (Compound 1) is a selective inhibitor of SARS-CoV-2 MPro with an IC50 value of 230 nM. In vitro, it also inhibits the replication of various SARS-CoV-2 variants.

SARS-CoV-2 Mpro-IN-28 (Compound 1K) is an inhibitor of SARS-CoV-2 Mpro, exhibiting an EC50 of 24 μM.

SARS-CoV-2 Mpro-IN-29 (Compound 7) is an inhibitor of the SARS-CoV-2 main protease (Mpro), with an IC50 of 310 nM for Mpro and an EC50 of 0.5 μM in Vero cells. By binding to the active site of Mpro, it prevents the cleavage of viral polyproteins, exhibiting significant antiviral activity and enhanced metabolic properties. SARS-CoV-2 Mpro-IN-29 holds potential for research in SARS-CoV-2 antiviral drug development.

SARS-CoV-2 Mpro-IN-35 (compound 14) is an inhibitor of SARS-CoV-2 Mpro and is applicable in the study of the SARS-CoV-2 virus.

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.

SARS-CoV-2 Mpro-IN-36 (Compound 6d) is an inhibitor of SARS-CoV-2 Mpro with an IC50 of 110 nM. This compound demonstrates antiviral activity with an EC50 of 1.6 μM.

SARS-CoV-2 Mpro-IN-38 (2-5a) is an inhibitor of SARS-CoV‑2 Mpro with an IC50 value of 0.0435 μM.

Mpro/PLPro-IN-2 (Compound 22l) is a non-covalent competitive dual inhibitor of SARS-CoV-2's papain-like protease and main protease, exhibiting a Ki of 0.2 μM for the papain-like protease and 1.1 μM for the main protease. Mpro/PLPro-IN-2 is applicable in research related to anti-SARS-CoV-2 efforts.

SARS-CoV-2 Mpro-IN-39 (Compound 9d) is an inhibitor of the SARS-CoV-2 main protease (Mpro) with an IC50 value of 5.94 µM. It inhibits the replication of SARS-CoV-2 in Vero cells with an EC50 value of 9.33 µM, and has a cytotoxicity CC50 value of 289.63 µM. This compound is applicable in COVID-19 related research.

SARS-CoV-2 Mpro-IN-30 (compound L2) is a SARS-CoV-2 Mpro inhibitor with an IC50 value of 9.1 nM.

SARS-CoV-2 Mpro-IN-44 (Compound 25) is a broad-spectrum inhibitor of the main protease (Mpro) for coronaviruses. It exhibits inhibitory activity against several high-risk coronaviruses, including SARS-CoV-2 and PEDV, with an IC50 of less than 0.6 μM. The broad inhibition of coronaviruses by SARS-CoV-2 Mpro-IN-44 is achieved through enhanced interaction with conserved sites of Mpro. This compound is a potential candidate for the development of antiviral drugs against coronaviruses.

SARS-CoV-2 Mpro-IN-42 (compound C5) is a potent inhibitor of SARS-CoV-2 Mpro, exhibiting an IC50 value of 33.6 nM. It is applicable for research concerning SARS-CoV-2.