plpro inhibitor

PLpro inhibitor is a potent papain-like protease (PLpro) inhibitor(IC50 of 2.6 uM)

PLpro/RBD-IN-1 is a dual inhibitor of SARS-CoV-2 PLpro and the spiny protein RBD, with anti-novel coronavirus activity, and is seen for the study of viral infections.

GRL0617 is a selective and competitive noncovalent inhibitor of SARS-CoVPLpro and deubiquitinase (IC50: 0.6 μM, Ki: 0.49 μM).

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.

PLpro-IN-6 (compound 6) serves as an inhibitor for the papain-like protease (PLpro), demonstrating potent activity with an IC 50 of 0.019 μM against the SARS-CoV-2 PLpro enzyme.

PF-07957472 (Compound 4) is an orally effective inhibitor of the SARS-CoV-2 papain-like protease (PLpro). In NHBE cells infected with SARS-CoV-2, it demonstrated cytopathic effects with an EC50 of 13.9 nM. Additionally, PF-07957472 exhibited antiviral activity in a mouse-adapted COVID-19 infection model.

PLpro-IN-8 (compound 1) serves as an inhibitor of the SARS-CoV papain-like protease (PLpro), exhibiting IC50 values of 5.9 μM for SARS-CoV-2 PLpro and 0.46 μM for SARS-CoV-1 PLpro. Additionally, it hinders the Wuhan SARS-CoV-2 strain WK-521 with an EC50 of 2.7 μM.

PLpro-IN-7 (compound 83) is a novel papain-like protease (PLpro) inhibitor with an IC50 of 3 nM.

SARS-CoV-2 PLpro-IN-1 (Compound 85) is a non-covalent competitive inhibitor of SARS-CoV-2 PLpro with an IC50 value of 15.06 μM and a Ki value of 22.93 μM. It inhibits the proliferation of Vero cells, exhibiting an IC50 of 7.47 μM.

ZHAWOC25153 (Compound 17o) is an inhibitor of the SARS-CoV-2 papain-like protease (PLpro) with an IC50 of 7 μM. It demonstrates antiviral properties and is applicable for research in the field of anti-infective studies.

9-AMN is an inhibitor of the SARS-CoV-2 papain-like protease (SARS-CoV-2 PLpro), effectively reducing its deubiquitinating (DUB) activity and protease activity, with IC50 values of 4.55 µM and 4.15 µM, respectively. Additionally, 9-AMN suppresses the replication of the SARS-CoV variants Delta and Omicron in Calu-3 cells, with IC50 values of 1.04 µM and 2.35 µM, respectively.

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.

WEHI-P8 is an orally active inhibitor targeting the coronavirus papain-like protease (PLpro). It inhibits SARS-CoV-2 PLpro with an IC50 of 12 nM and demonstrates excellent cellular activity with an EC50 of 298 nM. Additionally, WEHI-P8 has protective effects in mice against prolonged lung and brain symptoms caused by SARS-CoV-2. This compound is applicable for research on post-COVID-19 syndrome.

PLpro-IN-2 (Compound 16) is an inhibitor of the SARS-CoV-2 papain-like protease (PLpro), with an IC50 value of 0.25 μM.

Jun11165 is an inhibitor of SARS-CoV-2 PLpro with an IC50 of ≤ 0.6 μM, and it has an EC50 of ≤ 6 μM against SARS-CoV-2. Jun11165 is applicable for research on viral infections.

Jun12682 is an inhibitor of the SARS-CoV-2 papain-like protease (PLpro). It has a Ki value of 37.7 nM against PLpro and an EC50 value of 1.1 μM in the FlipGFP PLpro assay. Jun12682 is also orally active.

GZNL-P36 is an orally active inhibitor of SARS-CoV-2 papain-like protease (PLpro), with an IC50 of 6.45 nM. It effectively inhibits SARS-CoV and its variants, showing an EC50 ranging from 58.2 nM to 2.66 μM. In CD-1 mouse models, GZNL-P36 reaches a maximum plasma concentration (Cmax) of 549 ng/mL, with a half-life (T1/2) of 1.45 hours and a bioavailability of 74.7%. Additionally, GZNL-P36 exhibits antiviral activity in mice infected with SARS-CoV-2 XXB.1.

PLpro-IN-3 (compound 26R) is a potent papain-like protease (PLpro) inhibitor with an IC50 of 1.0 μM. It exhibits antiviral activity against SARS-CoV-2, with an EC50 of 4.3 μM.

4'-O-Methylbavachalcone (O-Methylbroussochalcone B) is isolated from Psoralea corylifolia, inhibits severe acute respiratory syndrome coronavirus (SARS-CoV) papain-like protease (PLpro) activity (IC50: 10.1 μM).

SARS-CoV-2-IN-23 (compound GRL-0617) is an inhibitor of SARS-CoV-2 papain-like protease (PLpro) with an IC50 of 2.3 μM [1].

PLP_Snyder530 is a potent papain-like protease (PL pro) inhibitor that induces conformational changes in SARS-CoV-2 papain-like protease, thereby inhibiting SARS-CoV-2 replication; it can be used for SARS-CoV-2 research [1].

XR8-69, a SARS-CoV-2 PLpro inhibitor, exhibits a low micromolar antiviral effect in SARS-CoV-2 infected human cells.

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).

SARS-CoV-2-IN-24 is a potent inhibitor of papain-like proteases (PLpro) that induces conformational changes in SARS-COV-2 papain-like proteases, inhibits SARS-COV-2 replication, and can be used to study SARS-CoV-2.