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Assay Detail

CHEMBL5250616

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

Binding
Inhibition of C-terminal His6-tagged recombinant SARS-CoV-2 MPro transfected in Escherichia coli BL21 (DE3) using Dabcyl-KTSAVLQSGFRKM-E(Edans)-NH2 as substrate preincubated for 15 mins followed by substrate addition measured after 30 mins by FRET assay
10
Total Activities
10
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

Rational design of the zonulin inhibitor AT1001 derivatives as potential anti SARS-CoV-2.
Di Micco S, Rahimova R, Sala M, Scala MC, Vivenzio G, Musella S, Andrei G, Remans K, Mammri L, Snoeck R, Bifulco G, Di Matteo F, Vestuto V, Campiglia P, Márquez JA, Fasano A.
Eur J Med Chem (2022) 244 : 114857 -114857
PubMed 36332548 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.29 5.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5287352 1 5.62
CHEMBL92708 CALPEPTIN 1 5.61
CHEMBL5286815 1 5.60
CHEMBL5291013 1 5.19
CHEMBL5279125 1 4.42
CHEMBL5281857 1 -
CHEMBL5270591 1 -
CHEMBL5287116 1 -
CHEMBL5291407 1 -
CHEMBL5276189 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5287352 IC50 = 2370.0 nM 5.62
CHEMBL92708 CALPEPTIN IC50 = 2430.0 nM 5.61
CHEMBL5286815 IC50 = 2510.0 nM 5.60
CHEMBL5291013 IC50 = 6490.0 nM 5.19
CHEMBL5279125 IC50 = 37840.0 nM 4.42
CHEMBL5281857 IC50 > 425000.0 nM -
CHEMBL5270591 IC50 > 213000.0 nM -
CHEMBL5287116 IC50 > 425000.0 nM -
CHEMBL5291407 IC50 = 197730.0 nM -
CHEMBL5276189 IC50 > 170000.0 nM -