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Assay Detail

CHEMBL4368174

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

Binding
Inhibition of human 5-LOX expressed in Escherichia coli BL21 using arachidonic acid as substrate preincubated for 15 mins followed by substrate addition by HPLC analysis
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Polyunsaturated fatty acid 5-lipoxygenase (CHEMBL215)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Protective effect of piceatannol and bioactive stilbene derivatives against hypoxia-induced toxicity in H9c2 cardiomyocytes and structural elucidation as 5-LOX inhibitors.
Boccellino M, Donniacuo M, Bruno F, Rinaldi B, Quagliuolo L, Ambruosi M, Pace S, De Rosa M, Olgaç A, Banoglu E, Alessio N, Massa A, Kahn H, Werz O, Fiorentino A, Filosa R.
Eur J Med Chem (2019) 180 : 637 -647
PubMed 31351395 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.78 6.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL332610 1 6.50
CHEMBL119576 1 6.11
CHEMBL69863 PICEATANNOL 1 5.96
CHEMBL296411 TRISMETHOXYRESVERATROL 1 5.44
CHEMBL83527 PTEROSTILBENE 2.0 1 5.41
CHEMBL419378 1 5.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL332610 IC50 = 320.0 nM 6.50
CHEMBL119576 IC50 = 780.0 nM 6.11
CHEMBL69863 PICEATANNOL IC50 = 1100.0 nM 5.96
CHEMBL296411 TRISMETHOXYRESVERATROL IC50 = 3620.0 nM 5.44
CHEMBL83527 PTEROSTILBENE IC50 = 3910.0 nM 5.41
CHEMBL419378 IC50 = 5490.0 nM 5.26