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Assay Detail

CHEMBL5250622

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

Binding
Binding affinity to C-terminal His6-tagged recombinant SARS-CoV-2 MPro transfected in Escherichia coli BL21 (DE3) assessed as dissociation constant by Cheng-Prusoff equation analysis
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
Kd 10 5.32 5.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5287352 1 5.92
CHEMBL92708 CALPEPTIN 1 5.91
CHEMBL5286815 1 5.90
CHEMBL5291013 1 5.49
CHEMBL5279125 1 4.72
CHEMBL5291407 1 4.00
CHEMBL5281857 1 -
CHEMBL5270591 1 -
CHEMBL5287116 1 -
CHEMBL5276189 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5287352 Kd = 1190.0 nM 5.92
CHEMBL92708 CALPEPTIN Kd = 1220.0 nM 5.91
CHEMBL5286815 Kd = 1260.0 nM 5.90
CHEMBL5291013 Kd = 3260.0 nM 5.49
CHEMBL5279125 Kd = 18920.0 nM 4.72
CHEMBL5291407 Kd = 98860.0 nM 4.00
CHEMBL5281857 Kd > 2.13 10^2 uM -
CHEMBL5270591 Kd > 1.07 10^2 uM -
CHEMBL5287116 Kd > 2.13 10^2 uM -
CHEMBL5276189 Kd > 8.5 10^1 uM -