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Assay Detail

CHEMBL3822052

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

Binding
Inhibition of KEAP1/NRF2 interaction in human bronchial epithelial cells from COPD patient assessed as induction of TXNRD1 mRNA expression incubated for 6 hrs by RT-PCR method
2
Total Activities
1
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Epithelial cell
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

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

Publication

Monoacidic Inhibitors of the Kelch-like ECH-Associated Protein 1: Nuclear Factor Erythroid 2-Related Factor 2 (KEAP1:NRF2) Protein-Protein Interaction with High Cell Potency Identified by Fragment-Based Discovery.
Davies TG, Wixted WE, Coyle JE, Griffiths-Jones C, Hearn K, McMenamin R, Norton D, Rich SJ, Richardson C, Saxty G, Willems HM, Woolford AJ, Cottom JE, Kou JP, Yonchuk JG, Feldser HG, Sanchez Y, Foley JP, Bolognese BJ, Logan G, Podolin PL, Yan H, Callahan JF, Heightman TD, Kerns JK.
J Med Chem (2016) 59 : 3991 -4006
PubMed 27031670 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 1 7.57 7.57
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3819587 2 7.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3819587 EC50 = 27.0 nM 7.57
CHEMBL3819587 Inhibition - % -