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Assay Detail

CHEMBL5528631

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

Binding
Inhibition of human Keap1 KELCH domain (321 to 609 residues) expressed in Escherichia coli BL21 DE3 pLysS cells/Nrf2 (unknown origin) protein-protein interaction preincubated with Keap1 for 1 hr followed by Nrf2 addition and measured after 1 hr by fluorescence polarization assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Keap1/Nrf2 (CHEMBL3038498)
Type PROTEIN-PROTEIN INTERACTION
Organism Homo sapiens

Publication

Recent progress and applications of small molecule inhibitors of Keap1-Nrf2 axis for neurodegenerative diseases.
Wang J, Cao Y, Lu Y, Zhu H, Zhang J, Che J, Zhuang R, Shao J.
Eur J Med Chem (2024) 264 : 115998 -115998
PubMed 38043492 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 8.01 8.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3237245 1 8.43
CHEMBL5556774 1 7.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3237245 IC50 = 3.7 nM 8.43
CHEMBL5556774 IC50 = 25.7 nM 7.59