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Assay Detail

CHEMBL3242829

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Binding
Displacement of FITC-LDEETGEFL-NH2 from Keap1 Kelch domain (unknown origin) after 30 mins by fluorescence polarization assay
3
Total Activities
3
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 of potent Keap1-Nrf2 protein-protein interaction inhibitor based on molecular binding determinants analysis.
Jiang ZY, Lu MC, Xu LL, Yang TT, Xi MY, Xu XL, Guo XK, Zhang XJ, You QD, Sun HP.
J Med Chem (2014) 57 : 2736 -2745
PubMed 24512214 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 6.59 7.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3237245 1 7.54
CHEMBL3134422 1 6.40
CHEMBL2402207 1 5.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3237245 EC50 = 28.6 nM 7.54
CHEMBL3134422 EC50 = 395.0 nM 6.40
CHEMBL2402207 EC50 = 1460.0 nM 5.84