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Assay Detail

CHEMBL5225084

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

Binding
Inhibition of SARS-CoV-2 Main protease
20
Total Activities
20
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 20 6.80 8.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5267069 1 8.12
CHEMBL5267414 1 7.85
CHEMBL5193976 1 7.82
CHEMBL5290282 1 7.82
CHEMBL5270743 1 7.76
CHEMBL4802135 NIRMATRELVIR 4.0 1 7.72
CHEMBL5195364 1 7.55
CHEMBL5205750 1 7.47
CHEMBL490822 1 7.26
CHEMBL5278950 1 7.25
CHEMBL5281998 1 7.10
CHEMBL164 MYRICETIN 1 6.70
CHEMBL5283004 1 6.37
CHEMBL274056 NAPHTHAZALIN 1 6.31
CHEMBL5287918 1 6.28
CHEMBL5287068 1 6.08
CHEMBL218394 BOCEPREVIR 4.0 1 5.80
CHEMBL5271977 1 5.54
CHEMBL590 MENADIONE 4.0 1 5.10
CHEMBL5288729 1 4.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5267069 IC50 = 7.6 nM 8.12
CHEMBL5267414 IC50 = 14.0 nM 7.85
CHEMBL5193976 IC50 = 15.24 nM 7.82
CHEMBL5290282 IC50 = 15.2 nM 7.82
CHEMBL5270743 IC50 = 17.2 nM 7.76
CHEMBL4802135 NIRMATRELVIR IC50 = 19.2 nM 7.72
CHEMBL5195364 IC50 = 27.95 nM 7.55
CHEMBL5205750 IC50 = 34.2 nM 7.47
CHEMBL490822 IC50 = 55.0 nM 7.26
CHEMBL5278950 IC50 = 56.0 nM 7.25
CHEMBL5281998 IC50 = 80.0 nM 7.10
CHEMBL164 MYRICETIN IC50 = 200.0 nM 6.70
CHEMBL5283004 IC50 = 430.0 nM 6.37
CHEMBL274056 NAPHTHAZALIN IC50 = 490.0 nM 6.31
CHEMBL5287918 IC50 = 530.0 nM 6.28
CHEMBL5287068 IC50 = 830.0 nM 6.08
CHEMBL218394 BOCEPREVIR IC50 = 1590.0 nM 5.80
CHEMBL5271977 IC50 = 2860.0 nM 5.54
CHEMBL590 MENADIONE IC50 = 7960.0 nM 5.10
CHEMBL5288729 IC50 = 86320.0 nM 4.06