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Assay Detail

CHEMBL3111170

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

Binding
Inhibition of human recombinant 5-LO expressed in Escherichia coli BL21 using arachidonic acid as substrate after 10 mins
21
Total Activities
21
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

Discovery and biological evaluation of novel 1,4-benzoquinone and related resorcinol derivatives that inhibit 5-lipoxygenase.
Filosa R, Peduto A, Aparoy P, Schaible AM, Luderer S, Krauth V, Petronzi C, Massa A, de Rosa M, Reddanna P, Werz O.
Eur J Med Chem (2013) 67 : 269 -279
PubMed 23871907 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 5.57 6.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3109719 1 6.55
CHEMBL93 ZILEUTON 4.0 1 6.25
CHEMBL1668217 1 6.11
CHEMBL3109717 1 6.10
CHEMBL3109718 1 5.85
CHEMBL501426 1 5.55
CHEMBL3109724 1 5.50
CHEMBL1668348 1 5.34
CHEMBL443605 HEXYLRESORCINOL -1.0 1 5.34
CHEMBL3109723 1 5.20
CHEMBL3109722 1 5.13
CHEMBL3109716 1 5.05
CHEMBL3109721 1 5.03
CHEMBL3109730 1 4.96
CHEMBL3109726 1 -
CHEMBL3109727 1 -
CHEMBL3109728 1 -
CHEMBL3109729 1 -
CHEMBL1668215 1 -
CHEMBL3109720 1 -
CHEMBL3109725 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3109719 IC50 = 280.0 nM 6.55
CHEMBL93 ZILEUTON IC50 = 560.0 nM 6.25
CHEMBL1668217 IC50 = 780.0 nM 6.11
CHEMBL3109717 IC50 = 800.0 nM 6.10
CHEMBL3109718 IC50 = 1400.0 nM 5.85
CHEMBL501426 IC50 = 2800.0 nM 5.55
CHEMBL3109724 IC50 = 3200.0 nM 5.50
CHEMBL1668348 IC50 = 4600.0 nM 5.34
CHEMBL443605 HEXYLRESORCINOL IC50 = 4600.0 nM 5.34
CHEMBL3109723 IC50 = 6300.0 nM 5.20
CHEMBL3109722 IC50 = 7400.0 nM 5.13
CHEMBL3109716 IC50 = 9000.0 nM 5.05
CHEMBL3109721 IC50 = 9400.0 nM 5.03
CHEMBL3109730 IC50 = 11000.0 nM 4.96
CHEMBL3109726 IC50 > 10000.0 nM -
CHEMBL3109727 IC50 > 10000.0 nM -
CHEMBL3109728 IC50 > 10000.0 nM -
CHEMBL3109729 IC50 > 10000.0 nM -
CHEMBL1668215 IC50 > 10000.0 nM -
CHEMBL3109720 IC50 > 10000.0 nM -
CHEMBL3109725 IC50 > 10000.0 nM -