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Assay Detail

CHEMBL5629633

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

Binding
Inhibition of SARS-CoV-2 3CL protease using Dabcyl-KTSAVLQSGFRKME-Edans as a substrate preincubated for 30 mins followed by substrate addition and measured after for 4 hrs by FRET assay
3
Total Activities
3
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

Exploring 2-methyl-substituted vitamin K<sub>3</sub> derivatives with potent inhibitory activity against the 3CL protease of SARS-CoV-2.
Koharazawa R, Hayakawa M, Takeda K, Miyazaki K, Tode C, Hirota Y, Suhara Y.
Bioorg Med Chem Lett (2024) 100 : 129642 -129642
PubMed 38310976 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 5.57 6.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL269468 1 6.02
CHEMBL590 MENADIONE 4.0 1 5.43
CHEMBL531383 1 5.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL269468 IC50 = 964.0 nM 6.02
CHEMBL590 MENADIONE IC50 = 3670.0 nM 5.43
CHEMBL531383 IC50 = 5350.0 nM 5.27