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Assay Detail

CHEMBL4603100

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

Binding
Inhibition of Keap1-Nrf2 Interaction (unknown origin) by fluorescence anisotropy
15
Total Activities
15
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

Isoquinoline Kelch-like ECH-Associated Protein 1-Nuclear Factor (Erythroid-Derived 2)-like 2 (KEAP1-NRF2) Inhibitors with High Metabolic Stability.
Lazzara PR, David BP, Ankireddy A, Richardson BG, Dye K, Ratia KM, Reddy SP, Moore TW.
J Med Chem (2020) 63 : 6547 -6560
PubMed 31682434 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 6.58 7.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4634168 1 7.26
CHEMBL4174651 1 7.20
CHEMBL4646536 1 7.14
CHEMBL4641049 1 6.92
CHEMBL4648321 1 6.89
CHEMBL4640762 1 6.68
CHEMBL4649822 1 6.64
CHEMBL4637137 1 6.62
CHEMBL4640093 1 6.55
CHEMBL4641622 1 6.46
CHEMBL4645359 1 6.38
CHEMBL4648175 1 6.37
CHEMBL4635609 1 6.00
CHEMBL4648275 1 5.96
CHEMBL4649258 1 5.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4634168 IC50 = 55.0 nM 7.26
CHEMBL4174651 IC50 = 63.0 nM 7.20
CHEMBL4646536 IC50 = 73.0 nM 7.14
CHEMBL4641049 IC50 = 120.0 nM 6.92
CHEMBL4648321 IC50 = 130.0 nM 6.89
CHEMBL4640762 IC50 = 210.0 nM 6.68
CHEMBL4649822 IC50 = 230.0 nM 6.64
CHEMBL4637137 IC50 = 240.0 nM 6.62
CHEMBL4640093 IC50 = 280.0 nM 6.55
CHEMBL4641622 IC50 = 350.0 nM 6.46
CHEMBL4645359 IC50 = 420.0 nM 6.38
CHEMBL4648175 IC50 = 430.0 nM 6.37
CHEMBL4635609 IC50 = 1000.0 nM 6.00
CHEMBL4648275 IC50 = 1100.0 nM 5.96
CHEMBL4649258 IC50 = 2300.0 nM 5.64