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Assay Detail

CHEMBL3242828

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Binding
Binding affinity to recombinant human Keap1 Kelch domain (321 to 609) expressed in Escherichia coli BL21(DE3)pLysS cells after 30 mins by fluorescence anisotropy 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

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
Kd 1 7.59 7.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3237244 1 7.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3237244 Kd = 25.6 nM 7.59