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Assay Detail

CHEMBL3295140

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

Binding
Inhibition of STAT3 transcriptional activity in human HaCaT cells after 6 hrs by luciferase reporter gene assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Signal transducer and activator of transcription 3 (CHEMBL4026)
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
IC50 12 4.73 5.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL128729 1 5.22
CHEMBL3290185 1 4.81
CHEMBL180239 CURCUMIN PYRAZOLE 1 4.79
CHEMBL2413471 1 4.74
CHEMBL3290186 1 4.71
CHEMBL2392188 1 4.65
CHEMBL140 CURCUMIN 3.0 1 4.47
CHEMBL3290439 1 4.45
CHEMBL318743 TETRAHYDROCURCUMIN 1 -
CHEMBL2392187 1 -
CHEMBL2392186 1 -
CHEMBL3290441 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL128729 IC50 = 6000.0 nM 5.22
CHEMBL3290185 IC50 = 15600.0 nM 4.81
CHEMBL180239 CURCUMIN PYRAZOLE IC50 = 16200.0 nM 4.79
CHEMBL2413471 IC50 = 18200.0 nM 4.74
CHEMBL3290186 IC50 = 19400.0 nM 4.71
CHEMBL2392188 IC50 = 22400.0 nM 4.65
CHEMBL140 CURCUMIN IC50 = 33900.0 nM 4.47
CHEMBL3290439 IC50 = 35700.0 nM 4.45
CHEMBL318743 TETRAHYDROCURCUMIN IC50 > 50000.0 nM -
CHEMBL2392187 IC50 > 50000.0 nM -
CHEMBL2392186 IC50 > 50000.0 nM -
CHEMBL3290441 IC50 > 50000.0 nM -