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Assay Detail

CHEMBL5225077

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

Binding
Binding affinity to SARS-CoV-2 Main protease assessed as inhibition constant
8
Total Activities
8
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
Ki 8 6.37 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4802135 NIRMATRELVIR 4.0 1 8.52
CHEMBL5266355 1 7.51
CHEMBL5179454 1 7.11
CHEMBL3427166 1 7.03
CHEMBL218394 BOCEPREVIR 4.0 1 5.93
CHEMBL4874639 1 5.67
CHEMBL164 MYRICETIN 1 4.80
CHEMBL5271977 1 4.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4802135 NIRMATRELVIR Ki = 3.0 nM 8.52
CHEMBL5266355 Ki = 31.0 nM 7.51
CHEMBL5179454 Ki = 78.0 nM 7.11
CHEMBL3427166 Ki = 94.0 nM 7.03
CHEMBL218394 BOCEPREVIR Ki = 1180.0 nM 5.93
CHEMBL4874639 Ki = 2150.0 nM 5.67
CHEMBL164 MYRICETIN Ki = 15730.0 nM 4.80
CHEMBL5271977 Ki = 38360.0 nM 4.42