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Assay Detail

CHEMBL5336134

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

Binding
Inhibition of MERS-CoV N-terminal 6His-SUMO-tagged 3CL protease expressed in Escherichia coli BL21 (DE3) using Dabcyl-KTSAVLQSGFRKM-Glu-Edans fluorogenic peptide as substrate pre-incubated for 30 mins in absence of GSH followed by substrate addition measured after 30 mins by FRET assay
6
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Middle East respiratory syndrome-related coronavirus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Novel dithiocarbamates selectively inhibit 3CL protease of SARS-CoV-2 and other coronaviruses.
Brier L, Hassan H, Hanoulle X, Landry V, Moschidi D, Desmarets L, Rouillé Y, Dumont J, Herledan A, Warenghem S, Piveteau C, Carré P, Ikherbane S, Cantrelle FX, Dupré E, Dubuisson J, Belouzard S, Leroux F, Deprez B, Charton J.
Eur J Med Chem (2023) 250 : 115186 -115186
PubMed 36796300 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.98 6.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2365410 2 6.37
CHEMBL5436771 2 5.87
CHEMBL4590273 2 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2365410 IC50 = 430.0 nM 6.37
CHEMBL2365410 IC50 = 426.58 nM 6.37
CHEMBL5436771 IC50 = 1360.0 nM 5.87
CHEMBL5436771 IC50 = 1348.96 nM 5.87
CHEMBL4590273 IC50 = 2000.0 nM 5.70
CHEMBL4590273 IC50 = 1995.26 nM 5.70