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Assay Detail

CHEMBL5529140

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Binding
Inhibition of Keap1-Nrf2 protein-protein interaction (unknown origin) by TR-FRET assay
13
Total Activities
13
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

Structural modification of C2-substituents on 1,4-bis(arylsulfonamido)benzene or naphthalene-N,N'-diacetic acid derivatives as potent inhibitors of the Keap1-Nrf2 protein-protein interaction.
Lee S, Ali AR, Abed DA, Nguyen MU, Verzi MP, Hu L.
Eur J Med Chem (2024) 265 : 116104 -116104
PubMed 38159482 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 7.39 7.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5571025 1 7.72
CHEMBL5570595 1 7.65
CHEMBL3237245 1 7.54
CHEMBL5595521 1 7.26
CHEMBL5567314 1 7.14
CHEMBL5556087 1 7.04
CHEMBL5181633 1 -
CHEMBL5590315 1 -
CHEMBL5557583 1 -
CHEMBL5572451 1 -
CHEMBL5573249 1 -
CHEMBL5594768 1 -
CHEMBL5593633 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5571025 IC50 = 19.0 nM 7.72
CHEMBL5570595 IC50 = 22.3 nM 7.65
CHEMBL3237245 IC50 = 28.5 nM 7.54
CHEMBL5595521 IC50 = 54.3 nM 7.26
CHEMBL5567314 IC50 = 72.2 nM 7.14
CHEMBL5556087 IC50 = 92.0 nM 7.04
CHEMBL5181633 IC50 - -
CHEMBL5590315 IC50 - -
CHEMBL5557583 IC50 - -
CHEMBL5572451 IC50 - -
CHEMBL5573249 IC50 - -
CHEMBL5594768 IC50 - -
CHEMBL5593633 IC50 - -