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Assay Detail

CHEMBL3620077

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Binding
Inhibition of Keap1 (unknown origin) interaction to Nrf2
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 Autocuration

Target

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

Publication

Design, Synthesis, and Evaluation of Triazole Derivatives That Induce Nrf2 Dependent Gene Products and Inhibit the Keap1-Nrf2 Protein-Protein Interaction.
Bertrand HC, Schaap M, Baird L, Georgakopoulos ND, Fowkes A, Thiollier C, Kachi H, Dinkova-Kostova AT, Wells G.
J Med Chem (2015) 58 : 7186 -7194
PubMed 26348784 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 8 5.62 7.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3617852 1 7.54
CHEMBL2381968 1 5.64
CHEMBL2402207 1 5.57
CHEMBL3235901 1 5.54
CHEMBL3617787 1 5.27
CHEMBL3134423 1 5.01
CHEMBL3617788 1 4.77
CHEMBL2402206 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3617852 EC50 = 28.6 nM 7.54
CHEMBL2381968 EC50 = 2300.0 nM 5.64
CHEMBL2402207 EC50 = 2700.0 nM 5.57
CHEMBL3235901 EC50 = 2900.0 nM 5.54
CHEMBL3617787 EC50 = 5400.0 nM 5.27
CHEMBL3134423 EC50 = 9800.0 nM 5.01
CHEMBL3617788 EC50 = 17100.0 nM 4.77
CHEMBL2402206 EC50 = 118000.0 nM -