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Assay Detail

CHEMBL4149487

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

Binding
Inhibition of human Keap1 kelch domain binding to Nrf2-ETGE peptide preincubated for 15 mins followed by peptide addition 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

Non-covalent Small-Molecule Kelch-like ECH-Associated Protein 1-Nuclear Factor Erythroid 2-Related Factor 2 (Keap1-Nrf2) Inhibitors and Their Potential for Targeting Central Nervous System Diseases.
Pallesen JS, Tran KT, Bach A.
J Med Chem (2018) 61 : 8088 -8103
PubMed 29750408 · 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