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Assay Detail

CHEMBL3295141

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

Binding
Activation of Nrf2 transcriptional activity in human LNCaP cells after 6 hrs by luciferase reporter gene assay relative to tert-butylhydroquinone
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type LNCaP
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

SAR studies on curcumin's pro-inflammatory targets: discovery of prenylated pyrazolocurcuminoids as potent and selective novel inhibitors of 5-lipoxygenase.
Koeberle A, Muñoz E, Appendino GB, Minassi A, Pace S, Rossi A, Weinigel C, Barz D, Sautebin L, Caprioglio D, Collado JA, Werz O.
J Med Chem (2014) 57 : 5638 -5648
PubMed 24920381 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 12 5.41 6.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL128729 1 6.05
CHEMBL3290186 1 5.51
CHEMBL3290185 1 5.07
CHEMBL140 CURCUMIN 3.0 1 5.00
CHEMBL3290439 1 -
CHEMBL318743 TETRAHYDROCURCUMIN 1 -
CHEMBL180239 CURCUMIN PYRAZOLE 1 -
CHEMBL2413471 1 -
CHEMBL2392187 1 -
CHEMBL2392186 1 -
CHEMBL2392188 1 -
CHEMBL3290441 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL128729 EC50 = 900.0 nM 6.05
CHEMBL3290186 EC50 = 3100.0 nM 5.51
CHEMBL3290185 EC50 = 8600.0 nM 5.07
CHEMBL140 CURCUMIN EC50 = 9900.0 nM 5.00
CHEMBL3290439 EC50 - -
CHEMBL318743 TETRAHYDROCURCUMIN EC50 - -
CHEMBL180239 CURCUMIN PYRAZOLE EC50 - -
CHEMBL2413471 EC50 - -
CHEMBL2392187 EC50 - -
CHEMBL2392186 EC50 - -
CHEMBL2392188 EC50 - -
CHEMBL3290441 EC50 - -