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Assay Detail

CHEMBL4810319

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

Binding
Inhibition of SARS-CoV-2 Main protease expressed in Escherichia coli BL21 (DE3) preincubated for 30 mins followed by addition of Dabcyl-KTSAVLQ/SGFRKME(Edans) substrate and measured after 1 hr by FRET assay
5
Total Activities
5
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

A head-to-head comparison of the inhibitory activities of 15 peptidomimetic SARS-CoV-2 3CLpro inhibitors.
Vankadara S, Wong YX, Liu B, See YY, Tan LH, Tan QW, Wang G, Karuna R, Guo X, Tan ST, Fong JY, Joy J, Chia CSB.
Bioorg Med Chem Lett (2021) 48 : 128263 -128263
PubMed 34271072 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.76 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3559293 1 7.52
CHEMBL4518490 1 5.50
CHEMBL64925 MG-132 1 5.41
CHEMBL4868590 1 5.38
CHEMBL92708 CALPEPTIN 1 4.97

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3559293 IC50 = 30.0 nM 7.52
CHEMBL4518490 IC50 = 3140.0 nM 5.50
CHEMBL64925 MG-132 IC50 = 3900.0 nM 5.41
CHEMBL4868590 IC50 = 4130.0 nM 5.38
CHEMBL92708 CALPEPTIN IC50 = 10690.0 nM 4.97