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Assay Detail

CHEMBL5350047

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of C-terminal His-tagged SARS-CoV-2 PLpro BetaCoV/Wuhan/WIV04/2019 strain (1564 to 1876 residues) expressed in Escherichia coli BL21(DE3) using ISG-AMC substrate incubated for 3 hrs
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Severe acute respiratory syndrome coronavirus 2
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Replicase polyprotein 1ab (CHEMBL4523582)
Type SINGLE PROTEIN
Organism Severe acute respiratory syndrome coronavirus 2

Publication

Repurposing 1,2,4-oxadiazoles as SARS-CoV-2 PLpro inhibitors and investigation of their possible viral entry blockade potential.
Ayoup MS, ElShafey MM, Abdel-Hamid H, Ghareeb DA, Abu-Serie MM, Heikal LA, Teleb M.
Eur J Med Chem (2023) 252 : 115272 -115272
PubMed 36966652 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.02 6.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5174607 1 6.21
CHEMBL5173886 1 6.17
CHEMBL549695 1 5.69

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5174607 IC50 = 620.0 nM 6.21
CHEMBL5173886 IC50 = 670.0 nM 6.17
CHEMBL549695 IC50 = 2050.0 nM 5.69