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Assay Detail

CHEMBL5136659

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

Binding
Inhibition of full length SARS CoV-2 main protease expressed in Escherichia coli BL21 (DE3) expression system using Mca-AVLQSGFR-K(Dnp)K as substrate by fluorescence method
2
Total Activities
2
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

Small-Molecule Thioesters as SARS-CoV-2 Main Protease Inhibitors: Enzyme Inhibition, Structure-Activity Relationships, Antiviral Activity, and X-ray Structure Determination.
Pillaiyar T, Flury P, Krüger N, Su H, Schäkel L, Barbosa Da Silva E, Eppler O, Kronenberger T, Nie T, Luedtke S, Rocha C, Sylvester K, Petry MRI, McKerrow JH, Poso A, Pöhlmann S, Gütschow M, O'Donoghue AJ, Xu Y, Müller CE, Laufer SA.
J Med Chem (2022) 65 : 9376 -9395
PubMed 35709506 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.66 5.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5190583 1 5.68
CHEMBL472940 1 5.63

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5190583 IC50 = 2080.0 nM 5.68
CHEMBL472940 IC50 = 2350.0 nM 5.63