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Assay Detail

CHEMBL5167238

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Binding
Inhibition of Keap1-Nrf2 (unknown origin) protein-protein interaction by SPR assay
5
Total Activities
5
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

Phenyl Bis-Sulfonamide Keap1-Nrf2 Protein-Protein Interaction Inhibitors with an Alternative Binding Mode.
Georgakopoulos N, Talapatra S, Dikovskaya D, Dayalan Naidu S, Higgins M, Gatliff J, Ayhan A, Nikoloudaki R, Schaap M, Valko K, Javid F, Dinkova-Kostova AT, Kozielski F, Wells G.
J Med Chem (2022) 65 : 7380 -7398
PubMed 35549469 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 5 6.76 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3237245 1 7.70
CHEMBL4174651 1 6.99
CHEMBL3617852 1 6.96
CHEMBL3632882 1 6.40
CHEMBL2402207 1 5.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3237245 Kd = 20.0 nM 7.70
CHEMBL4174651 Kd = 102.0 nM 6.99
CHEMBL3617852 Kd = 110.0 nM 6.96
CHEMBL3632882 Kd = 400.0 nM 6.40
CHEMBL2402207 Kd = 1700.0 nM 5.77