Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL3637037

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

Binding
Inhibition of Keap1-NRF2 interaction (unknown origin) expressed in Escherichia coli BL21 (DE3) cells assessed as reduction in FITC-9mer NRF2 peptide binding after 1 hr by fluorescence anisotropy assay
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type BL21-DE3
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

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

Publication

Probing the structural requirements of non-electrophilic naphthalene-based Nrf2 activators.
Jain AD, Potteti H, Richardson BG, Kingsley L, Luciano JP, Ryuzoji AF, Lee H, Krunic A, Mesecar AD, Reddy SP, Moore TW.
Eur J Med Chem (2015) 103 : 252 -268
PubMed 26363505 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 33 6.49 7.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3237245 1 7.62
CHEMBL3617852 1 7.21
CHEMBL3632711 1 7.20
CHEMBL3632882 1 7.07
CHEMBL3632705 1 6.72
CHEMBL3632881 1 6.39
CHEMBL3632699 1 6.20
CHEMBL3632706 1 6.18
CHEMBL3632704 1 6.05
CHEMBL2402207 1 6.03
CHEMBL3632703 1 5.96
CHEMBL3632887 1 5.26
CHEMBL3632702 1 -
CHEMBL3632707 1 -
CHEMBL3632708 1 -
CHEMBL3632709 1 -
CHEMBL3632710 1 -
CHEMBL3632712 1 -
CHEMBL3632714 1 -
CHEMBL3632880 1 -
CHEMBL3632890 1 -
CHEMBL3632889 1 -
CHEMBL3632888 1 -
CHEMBL3632713 1 -
CHEMBL3632885 1 -
CHEMBL3632884 1 -
CHEMBL3632883 1 -
CHEMBL3392606 1 -
CHEMBL2133303 1 -
CHEMBL3632886 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3237245 IC50 = 24.0 nM 7.62
CHEMBL3617852 IC50 = 61.0 nM 7.21
CHEMBL3632711 IC50 = 63.0 nM 7.20
CHEMBL3632882 IC50 = 85.0 nM 7.07
CHEMBL3632705 IC50 = 190.0 nM 6.72
CHEMBL3632881 IC50 = 410.0 nM 6.39
CHEMBL3632699 IC50 = 630.0 nM 6.20
CHEMBL3632706 IC50 = 660.0 nM 6.18
CHEMBL3632704 IC50 = 890.0 nM 6.05
CHEMBL2402207 IC50 = 940.0 nM 6.03
CHEMBL3632703 IC50 = 1100.0 nM 5.96
CHEMBL3632887 IC50 = 5500.0 nM 5.26
CHEMBL484276 IC50 > 25000.0 nM -
CHEMBL3632700 IC50 > 25000.0 nM -
CHEMBL3632701 IC50 > 25000.0 nM -
CHEMBL3632702 IC50 > 25000.0 nM -
CHEMBL3632707 IC50 > 25000.0 nM -
CHEMBL3632708 IC50 > 25000.0 nM -
CHEMBL3632709 IC50 > 25000.0 nM -
CHEMBL3632710 IC50 > 25000.0 nM -
CHEMBL3632712 IC50 > 25000.0 nM -
CHEMBL3632714 IC50 > 25000.0 nM -
CHEMBL3632880 IC50 > 25000.0 nM -
CHEMBL3632890 IC50 > 25000.0 nM -
CHEMBL3632889 IC50 > 25000.0 nM -
CHEMBL3632888 IC50 > 25000.0 nM -
CHEMBL3632713 IC50 > 25000.0 nM -
CHEMBL3632885 IC50 > 25000.0 nM -
CHEMBL3632884 IC50 > 25000.0 nM -
CHEMBL3632883 IC50 > 25000.0 nM -
CHEMBL3392606 IC50 > 25000.0 nM -
CHEMBL2133303 IC50 > 25000.0 nM -
CHEMBL3632886 IC50 > 25000.0 nM -