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Assay Detail

CHEMBL4143590

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

Binding
Activation of Nrf2 (unknown origin) expressed in human HepG2 cells after 5 hrs by ARE-driven luciferase reporter gene assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HepG2
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Nuclear factor erythroid 2-related factor 2 (CHEMBL1075094)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Activation of anti-oxidant Nrf2 signaling by enone analogues of curcumin.
Deck LM, Hunsaker LA, Vander Jagt TA, Whalen LJ, Royer RE, Vander Jagt DL.
Eur J Med Chem (2018) 143 : 854 -865
PubMed 29223100 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 15 5.09 5.88

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL521819 1 5.88
CHEMBL477053 1 5.48
CHEMBL559673 1 5.48
CHEMBL2316157 1 5.28
CHEMBL4172072 1 5.14
CHEMBL4167461 1 5.14
CHEMBL3105277 1 5.12
CHEMBL2009362 1 5.10
CHEMBL128729 1 5.00
CHEMBL477052 1 4.99
CHEMBL3780720 1 4.84
CHEMBL261295 TETRAMETHOXYCURCUMIN 1 4.78
CHEMBL562131 1 4.74
CHEMBL4162563 1 4.68
CHEMBL140 CURCUMIN 3.0 1 4.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL521819 EC50 = 1320.0 nM 5.88
CHEMBL477053 EC50 = 3300.0 nM 5.48
CHEMBL559673 EC50 = 3300.0 nM 5.48
CHEMBL2316157 EC50 = 5300.0 nM 5.28
CHEMBL4172072 EC50 = 7200.0 nM 5.14
CHEMBL4167461 EC50 = 7300.0 nM 5.14
CHEMBL3105277 EC50 = 7600.0 nM 5.12
CHEMBL2009362 EC50 = 8000.0 nM 5.10
CHEMBL128729 EC50 = 9900.0 nM 5.00
CHEMBL477052 EC50 = 10300.0 nM 4.99
CHEMBL3780720 EC50 = 14400.0 nM 4.84
CHEMBL261295 TETRAMETHOXYCURCUMIN EC50 = 16600.0 nM 4.78
CHEMBL562131 EC50 = 18100.0 nM 4.74
CHEMBL4162563 EC50 = 21100.0 nM 4.68
CHEMBL140 CURCUMIN EC50 = 21000.0 nM 4.68