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Assay Detail

CHEMBL5610442

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

Binding
Inhibition of hCoV-229E 3CLpro using Dabcyl-KTSAVLQSGFRKM-Glu(Edans) as substrate preincubated 1 hr in presence of 2 mM GSH followed by substrate addition and measured after 30 mins by FRET assay
14
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Human coronavirus 229E
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Replicase polyprotein 1ab (CHEMBL4888440)
Type SINGLE PROTEIN
Organism Human coronavirus 229E

Publication

N-acylbenzimidazoles as selective Acylators of the catalytic cystein of the coronavirus 3CL protease.
Chaibi FZ, Brier L, Carré P, Landry V, Desmarets L, Tarricone A, Cantrelle FX, Moschidi D, Herledan A, Biela A, Bourgeois F, Ribes C, Ikherbane S, Malessan M, Dubuisson J, Belouzard S, Hanoulle X, Leroux F, Deprez B, Charton J.
Eur J Med Chem (2024) 276 : 116707 -116707
PubMed 39068863 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.40 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2365410 2 7.70
CHEMBL586628 2 6.73
CHEMBL5612402 2 6.50
CHEMBL5612841 2 6.46
CHEMBL5614072 2 6.13
CHEMBL5612298 2 5.72
CHEMBL5611903 2 5.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2365410 IC50 = 20.0 nM 7.70
CHEMBL2365410 IC50 = 22.91 nM 7.64
CHEMBL586628 IC50 = 186.21 nM 6.73
CHEMBL586628 IC50 = 190.0 nM 6.72
CHEMBL5612402 IC50 = 320.0 nM 6.50
CHEMBL5612402 IC50 = 323.59 nM 6.49
CHEMBL5612841 IC50 = 350.0 nM 6.46
CHEMBL5612841 IC50 = 354.81 nM 6.45
CHEMBL5614072 IC50 = 741.31 nM 6.13
CHEMBL5614072 IC50 = 750.0 nM 6.12
CHEMBL5612298 IC50 = 1900.0 nM 5.72
CHEMBL5612298 IC50 = 1905.46 nM 5.72
CHEMBL5611903 IC50 = 2600.0 nM 5.58
CHEMBL5611903 IC50 = 2630.27 nM 5.58