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Assay Detail

CHEMBL1930630

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Binding
Inhibition of 5-LOX assessed as decrease in oxygen concentration using arachidonic acid as substrate by polarigraphic method with Clark's oxygen electrode
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Structure based drug design, synthesis and evaluation of 4-(benzyloxy)-1-phenylbut-2-yn-1-ol derivatives as 5-lipoxygenase inhibitors.
Reddy NP, Chandramohan Reddy T, Aparoy P, Achari C, Sridhar PR, Reddanna P.
Eur J Med Chem (2012) 47 : 351 -359
PubMed 22118829 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 4.54 5.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL304818 DOCEBENONE 2.0 1 5.77
CHEMBL1929096 1 5.10
CHEMBL1929095 1 4.92
CHEMBL1929093 1 4.39
CHEMBL1929094 1 4.21
CHEMBL1929089 1 4.16
CHEMBL1929090 1 4.14
CHEMBL1929091 1 4.10
CHEMBL1929092 1 4.10
CHEMBL1929086 1 -
CHEMBL1929087 1 -
CHEMBL1929088 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL304818 DOCEBENONE IC50 = 1700.0 nM 5.77
CHEMBL1929096 IC50 = 8000.0 nM 5.10
CHEMBL1929095 IC50 = 12000.0 nM 4.92
CHEMBL1929093 IC50 = 41000.0 nM 4.39
CHEMBL1929094 IC50 = 62000.0 nM 4.21
CHEMBL1929089 IC50 = 69000.0 nM 4.16
CHEMBL1929090 IC50 = 72000.0 nM 4.14
CHEMBL1929091 IC50 = 80000.0 nM 4.10
CHEMBL1929092 IC50 = 80000.0 nM 4.10
CHEMBL1929086 IC50 > 100000.0 nM -
CHEMBL1929087 IC50 > 100000.0 nM -
CHEMBL1929088 IC50 > 100000.0 nM -