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Assay Detail

CHEMBL5225095

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

Binding
Inhibition of SARS-CoV-2 BetaCoV/Wuhan/WIV04/2019 Main protease expressed in Escherichia coli BL21 (DE3) using Dabcyl-KTSAVLQ/SGFRKME(Edans) as substrate preincubated for 30 mins followed by substrate addition and measured after 1 hr by FRET assay
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

Targeting SARS-CoV-2 Main Protease for Treatment of COVID-19: Covalent Inhibitors Structure-Activity Relationship Insights and Evolution Perspectives.
La Monica G, Bono A, Lauria A, Martorana A.
J Med Chem (2022) 65 : 12500 -12534
PubMed 36169610 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.71 6.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5266148 1 6.35
CHEMBL318779 1 5.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5266148 IC50 = 450.0 nM 6.35
CHEMBL318779 IC50 = 8600.0 nM 5.07