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.

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.

XR8-89, a potent inhibitor of papain-like protease (PLpro), exhibits an IC50 value of 0.1 μM and effectively hinders SARS-CoV-2 replication by inducing conformational changes in the SARS-COV-2 papain-like protease. This compound holds potential for SARS-CoV-2 research applications [1].

INSCoV-600K(1) is a potent Mpro(3CLpro) inhibitor, with research potential against SARS-CoV-2 infection. Proteases (PLpro and 3CLpro) are associated with viral transcription and replication.

INSCoV-601I(1) is a potent Mpro(3CLpro) inhibitor linked to viral transcription and replication through proteases (PLpro and 3CLpro). This compound has demonstrated research potential against SARS-CoV-2 infection.

INSCoV-614(1B) is a potent Mpro (3CLpro) inhibitor associated with viral transcription and replication. This compound has demonstrated research potential for SARS-CoV-2 infection by targeting the proteases PLpro and 3CLpro.

SP inhibitor 1 is an inhibitor of SARS-CoV-2 replication at non-toxic concentrations (0.3250<5.98 μM) in vitro. SP inhibitor 1 is a selective inhibitor of SARS-CoV-2 stinger protein (SP), acting on SP protein (IC50: 3.26 μM), Mpro protein (IC50>25 μM) and PLpro protein (IC50>25 μM), and has cellular antiviral effects. and PLpro protein (IC50>25 μM), and has cellular antiviral effects.

Antiviral agent 25 (compound 6g), a novel non-peptide analog covalent inhibitor of SARS-CoV-2 3CL pro, exhibits robust inhibitory activity against both SARS-CoV-2 3CL pro and SARS-CoV-2 PL pro, with IC50 values of 0.118 µM and 0.448 µM, respectively. Furthermore, it demonstrates significant antiviral effects against SARS-CoV-2, achieving an EC50 value of 7.249 µM [1].

SIMR3030, a potent inhibitor of SARS-CoV-2 PLpro, possesses an IC50 of 0.0399 µg mL and demonstrates antiviral activity by diminishing the expression of SARS-CoV spike, ORF1b, IFN-α, and IL-6 mRNA. Additionally, SIMR3030 has been shown to have a satisfactory safety profile in mice [1].