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Assay Detail

CHEMBL4149486

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of Keap1 kelch domain (unknow origin)/Nrf2-ETGE peptide (unknown origin) interaction by fluorescence polarization assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Non-covalent Small-Molecule Kelch-like ECH-Associated Protein 1-Nuclear Factor Erythroid 2-Related Factor 2 (Keap1-Nrf2) Inhibitors and Their Potential for Targeting Central Nervous System Diseases.
Pallesen JS, Tran KT, Bach A.
J Med Chem (2018) 61 : 8088 -8103
PubMed 29750408 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.84 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4160447 1 8.00
CHEMBL3890847 1 6.12
CHEMBL4167678 1 5.96
CHEMBL2381968 1 5.64
CHEMBL4167472 1 5.13
CHEMBL4165400 1 4.16
CHEMBL4176009 1 -
CHEMBL3186228 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4160447 IC50 = 10.0 nM 8.00
CHEMBL3890847 IC50 = 750.0 nM 6.12
CHEMBL4167678 IC50 = 1100.0 nM 5.96
CHEMBL2381968 IC50 = 2300.0 nM 5.64
CHEMBL4167472 IC50 = 7400.0 nM 5.13
CHEMBL4165400 IC50 = 69700.0 nM 4.16
CHEMBL4176009 IC50 > 100000.0 nM -
CHEMBL3186228 IC50 > 100000.0 nM -