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Assay Detail

CHEMBL5543916

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

Binding
Inhibition of recombinant SARS-CoV-2 main protease using DABCYL-KTSAVLQSGFRKME-EDANS as fluorescent substrate preincubated for 30 mins followed by substrate addition by FRET assay
18
Total Activities
18
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

Peptidomimetics as potent dual SARS-CoV-2 cathepsin-L and main protease inhibitors: In silico design, synthesis and pharmacological characterization.
Ciaglia T, Vestuto V, Di Sarno V, Musella S, Smaldone G, Di Matteo F, Napolitano V, Miranda MR, Pepe G, Basilicata MG, Novi S, Capolupo I, Bifulco G, Campiglia P, Gomez-Monterrey I, Snoeck R, Andrei G, Manfra M, Ostacolo C, Lauro G, Bertamino A.
Eur J Med Chem (2024) 266 : 116128 -116128
PubMed 38232463 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 5.53 6.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2315036 1 6.24
CHEMBL5594341 1 6.14
CHEMBL5070941 1 5.76
CHEMBL5574506 1 5.55
CHEMBL5591434 1 5.08
CHEMBL5576036 1 5.08
CHEMBL5572122 1 4.83
CHEMBL5575599 1 -
CHEMBL5574180 1 -
CHEMBL5592679 1 -
CHEMBL5563602 1 -
CHEMBL5570567 1 -
CHEMBL5569237 1 -
CHEMBL5564969 1 -
CHEMBL5566215 1 -
CHEMBL5566703 1 -
CHEMBL5589813 1 -
CHEMBL5565757 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2315036 IC50 = 570.23 nM 6.24
CHEMBL5594341 IC50 = 730.12 nM 6.14
CHEMBL5070941 IC50 = 1720.44 nM 5.76
CHEMBL5574506 IC50 = 2810.81 nM 5.55
CHEMBL5591434 IC50 = 8350.53 nM 5.08
CHEMBL5576036 IC50 = 8320.26 nM 5.08
CHEMBL5572122 IC50 = 14610.54 nM 4.83
CHEMBL5575599 IC50 > 30000.0 nM -
CHEMBL5574180 IC50 > 30000.0 nM -
CHEMBL5592679 IC50 > 30000.0 nM -
CHEMBL5563602 IC50 > 30000.0 nM -
CHEMBL5570567 IC50 > 30000.0 nM -
CHEMBL5569237 IC50 > 30000.0 nM -
CHEMBL5564969 IC50 > 30000.0 nM -
CHEMBL5566215 IC50 > 30000.0 nM -
CHEMBL5566703 IC50 > 30000.0 nM -
CHEMBL5589813 IC50 > 30000.0 nM -
CHEMBL5565757 IC50 > 30000.0 nM -