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Assay Detail

CHEMBL4376095

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

Binding
Inhibition of Alexa633-AFFAQLQLDEETGEFL binding to recombinant human KEAP1 Kelch domain (321 to 609 residues) preincubated for 15 mins followed by Alexa633-AFFAQLQLDEETGEFL addition and measured after 30 mins by fluorescence polarization assay
1
Total Activities
1
Compounds Tested
1
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
IC50 1 6.85 6.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3899754 1 6.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3899754 IC50 = 140.0 nM 6.85