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Assay Detail

CHEMBL4433109

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Binding
Inhibition of Keap1 Kelch domain/FITC-9mer Nrf2 (unknown origin) interaction after 30 mins by fluorescence polarization assay
9
Total Activities
9
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

Polar Recognition Group Study of Keap1-Nrf2 Protein-Protein Interaction Inhibitors.
Lu MC, Tan SJ, Ji JA, Chen ZY, Yuan ZW, You QD, Jiang ZY.
ACS Med Chem Lett (2016) 7 : 835 -840
PubMed 27660687 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.87 7.87

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3601212 1 7.87
CHEMBL4544116 1 7.80
CHEMBL4515723 1 6.21
CHEMBL4455786 1 5.58
CHEMBL4592064 1 -
CHEMBL4540101 1 -
CHEMBL4546347 1 -
CHEMBL4587926 1 -
CHEMBL4469585 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3601212 IC50 = 13.4 nM 7.87
CHEMBL4544116 IC50 = 15.8 nM 7.80
CHEMBL4515723 IC50 = 609.0 nM 6.21
CHEMBL4455786 IC50 = 2600.0 nM 5.58
CHEMBL4592064 IC50 > 50000.0 nM -
CHEMBL4540101 IC50 > 50000.0 nM -
CHEMBL4546347 IC50 > 50000.0 nM -
CHEMBL4587926 IC50 > 50000.0 nM -
CHEMBL4469585 IC50 > 50000.0 nM -