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Assay Detail

CHEMBL2382890

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Binding
Binding affinity to Keap1 kelch domain (unknown origin) by competitive SPR assay
8
Total Activities
8
Compounds Tested
2
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 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
Activity 4 - -
Kd 4 5.24 6.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2381968 1 6.00
CHEMBL1460757 1 5.72
CHEMBL2381969 1 4.00
CHEMBL2381965 1 -
CHEMBL2381967 1 -
CHEMBL2381964 1 -
CHEMBL2381966 1 -
CHEMBL2381970 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2381968 Kd = 1000.0 nM 6.00
CHEMBL1460757 Kd = 1900.0 nM 5.72
CHEMBL2381969 Kd = 100000.0 nM 4.00
CHEMBL2381965 Activity - -
CHEMBL2381967 Activity - -
CHEMBL2381964 Activity - -
CHEMBL2381966 Activity - -
CHEMBL2381970 Kd = 700000.0 nM -