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Assay Detail

CHEMBL5230561

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Binding
Inhibition of human Keap1-Nrf2 protein-protein interaction by fluorescence polarization assay
17
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Recent progress in Keap1-Nrf2 protein-protein interaction inhibitors.
Mou Y, Wen S, Li YX, Gao XX, Zhang X, Jiang ZY.
Eur J Med Chem (2020) 202 : 112532 -112532
PubMed 32668381 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 6.47 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4160447 1 8.00
CHEMBL4858288 1 7.84
CHEMBL4169002 1 7.51
CHEMBL3632711 1 7.20
CHEMBL5277720 1 7.20
CHEMBL3928693 1 6.94
CHEMBL5285536 1 6.82
CHEMBL3617787 2 6.71
CHEMBL5273301 1 6.70
CHEMBL1969108 1 6.59
CHEMBL4648717 1 5.60
CHEMBL4208450 1 5.57
CHEMBL5273569 2 4.00
CHEMBL5275624 2 4.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4160447 IC50 = 10.0 nM 8.00
CHEMBL4858288 IC50 = 14.4 nM 7.84
CHEMBL4169002 IC50 = 31.0 nM 7.51
CHEMBL3632711 IC50 = 63.0 nM 7.20
CHEMBL5277720 IC50 = 63.0 nM 7.20
CHEMBL3928693 IC50 = 115.0 nM 6.94
CHEMBL5285536 IC50 = 153.0 nM 6.82
CHEMBL3617787 IC50 = 194.0 nM 6.71
CHEMBL5273301 IC50 = 200.0 nM 6.70
CHEMBL1969108 IC50 = 258.0 nM 6.59
CHEMBL3617787 IC50 = 389.0 nM 6.41
CHEMBL4648717 IC50 = 2500.0 nM 5.60
CHEMBL4208450 IC50 = 2700.0 nM 5.57
CHEMBL5275624 IC50 = 100000.0 nM 4.00
CHEMBL5273569 IC50 = 100000.0 nM 4.00
CHEMBL5275624 IC50 = 185200.0 nM -
CHEMBL5273569 IC50 = 185200.0 nM -