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Assay Detail

CHEMBL875417

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

Binding
Tested for inhibition of 5-LO by measuring the reduction of leukotriene B4 (LTB4) in intact basophilic rat leukemia cells
4
Total Activities
4
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 (CHEMBL312)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Design of 5-(3,5-di-tert-butyl-4-hydroxyphenyl)-1,3,4-thiadiazoles, -1,3,4-oxadiazoles, and -1,2,4-triazoles as orally-active, nonulcerogenic antiinflammatory agents.
Mullican MD, Wilson MW, Connor DT, Kostlan CR, Schrier DJ, Dyer RD.
J Med Chem (1993) 36 : 1090 -1099
PubMed 8478906 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.58 6.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL16828 1 6.04
CHEMBL8562 1 5.60
CHEMBL12594 E-5110 1 5.37
CHEMBL2079592 1 5.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL16828 IC50 = 920.0 nM 6.04
CHEMBL8562 IC50 = 2500.0 nM 5.60
CHEMBL12594 E-5110 IC50 = 4300.0 nM 5.37
CHEMBL2079592 IC50 = 5000.0 nM 5.30