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Assay Detail

CHEMBL2382889

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Binding
Inhibition of Keap1-Nrf2 interaction in human HepG2 cells expressing ARE-bla assessed as activation of antioxidant response element by beta-lactamase reporter assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HepG2
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

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

Publication

Discovery of a small-molecule inhibitor and cellular probe of Keap1-Nrf2 protein-protein interaction.
Hu L, Magesh S, Chen L, Wang L, Lewis TA, Chen Y, Khodier C, Inoyama D, Beamer LJ, Emge TJ, Shen J, Kerrigan JE, Kong AN, Dandapani S, Palmer M, Schreiber SL, Munoz B.
Bioorg Med Chem Lett (2013) 23 : 3039 -3043
PubMed 23562243 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 4.75 4.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2381968 1 4.75
CHEMBL2381970 1 -
CHEMBL2381969 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2381968 EC50 = 18000.0 nM 4.75
CHEMBL2381970 EC50 > 100000000.0 nM -
CHEMBL2381969 EC50 > 100000.0 nM -