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Assay Detail

CHEMBL4376072

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

Binding
Inhibition of FAM-LDEETGEFL-NH2 binding to recombinant human KEAP1 Kelch domain (321 to 609 residues) expressed in Escherichia coli BL21 (DE3) measured after 30 to 60 mins in absence of TCEP buffer by fluorescence polarization assay
4
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Kelch-like ECH-associated protein 1 (CHEMBL2069156)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A Comparative Assessment Study of Known Small-Molecule Keap1-Nrf2 Protein-Protein Interaction Inhibitors: Chemical Synthesis, Binding Properties, and Cellular Activity.
Tran KT, Pallesen JS, Solbak SMØ, Narayanan D, Baig A, Zang J, Aguayo-Orozco A, Carmona RMC, Garcia AD, Bach A.
J Med Chem (2019) 62 : 8028 -8052
PubMed 31411465 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Inhibition 3 - -
IC50 1 4.00 4.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3235901 1 4.00
CHEMBL3617836 1 -
CHEMBL3134423 1 -
CHEMBL3235898 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3235901 IC50 = 100000.0 nM 4.00
CHEMBL3617836 Inhibition - % -
CHEMBL3134423 Inhibition - % -
CHEMBL3235898 Inhibition - % -