mpro

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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-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].

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-26 (compound 13) is a covalent inhibitor targeting SARS-CoV-2 Mpro.

SARS-CoV-2 Mpro-IN-27 (Compound 4h) is an effective inhibitor of SARS-CoV-2 Mpro.

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-34 (Compound 26) acts as an inhibitor of SARS-CoV-2 Mpro with an IC50 of 6 nM. It also inhibits OC43 Mpro, demonstrating an IC50 of 33 nM. Furthermore, this compound exhibits antiviral activity in Vero E6 cells infected with SARS-CoV-2, with an EC50 of 0.103 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.

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.

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).

SARS-CoV-2 Mpro-IN-1 (compound 16b-3) is a potent, selective, and irreversible inhibitor of the SARS-CoV-2 main protease (Mpro) with an IC50 value of 116 nM [1].

Mpro PLpro-IN-1 (Compound 29) is a dual-acting inhibitor of SARS-CoV-2 protease, displaying micromolar inhibition of Mpro (IC50: 1.72 μM) and submicromolar inhibition of PLpro (IC50: 0.67 μM).

Mpro 61 is a potent non-covalent inhibitor of SARS-CoV-2 main protease.

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.