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Assay Detail

CHEMBL3864467

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

Binding
Inhibition of recombinant human Keap1 Kelch domain (321 to 609 residues) expressed in Escherichia coli BL21(DE3)pLysS interaction with Nrf2 assessed as displacement of FITC-LDEETGEFL-NH2 from Keap1 Kelch domain after 30 mins by FP assay
2
Total Activities
2
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

Discovery and Development of Kelch-like ECH-Associated Protein 1. Nuclear Factor Erythroid 2-Related Factor 2 (KEAP1:NRF2) Protein-Protein Interaction Inhibitors: Achievements, Challenges, and Future Directions.
Jiang ZY, Lu MC, You QD.
J Med Chem (2016) 59 : 10837 -10858
PubMed 27690435 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.08 6.71

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3134422 1 6.71
CHEMBL3975863 1 5.45

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3134422 IC50 = 194.0 nM 6.71
CHEMBL3975863 IC50 = 3570.0 nM 5.45