SARS-CoV-2 Mpro-IN-2

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-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-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-22 (compound 4) is an effective inhibitor of the SARS-CoV-2 main protease (Mpro), with an IC50 of 1.2 µg/mL. This hydrolyzable tannin exhibits no significant cytotoxic activity in A549 and HUVEC cell lines.

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-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-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.

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.

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.

SARS-CoV-2 Mpro-IN-40 (compound 119) is an inhibitor of SARS-CoV-2 Mpro, exhibiting an IC50 value of 15.7 nM against Mpro Fret. It demonstrates low metabolic stability in human microsomes.

SARS-CoV-2 Mpro-IN-41 (Compound 7e) is an orally active inhibitor targeting COX-2 and SARS-CoV-2 Mpro, with respective IC50 values of 9.66 μM and 13.24 μM. It also demonstrates inhibitory activity against COX-1 (IC50: 46.11 μM). This compound significantly suppresses the expression of inflammation-related cytokines such as TNF-α, IL-6, and IL-1β, exhibiting anti-inflammatory properties. By selectively inhibiting COX-2 and SARS-CoV-2 Mpro, SARS-CoV-2 Mpro-IN-41 exerts both anti-inflammatory and antiviral effects, making it a potential candidate for research in inflammation and COVID-19 treatment.

SARS-CoV-2 Mpro-IN-43 (Compound 1) is an inhibitor of the coronavirus main protease (Mpro) with an IC50 of 72 μM. It exerts its antiviral effects by interacting non-covalently with the key residues at the Mpro active site. This compound exhibits moderate to low cytotoxicity with CC50 values of 13.24, 41.02, and 42.26 µM in HaCaT, HEK293T, and HepG2 cells, respectively. SARS-CoV-2 Mpro-IN-43 is applicable for SARS-CoV-2 research.

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].

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.