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Assay Detail

CHEMBL619225

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

Binding
Inhibitory activity against 5-lipoxygenase obtained from rat basophilic leukemia cells
6
Total Activities
6
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, synthesis, and biological evaluation of conformationally constrained aci-reductone mimics of arachidonic acid.
Hopper AT, Witiak DT, Ziemniak J.
J Med Chem (1998) 41 : 420 -427
PubMed 9484493 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.51 7.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL59356 ATRELEUTON 2.0 1 7.64
CHEMBL132859 1 6.80
CHEMBL135483 1 6.52
CHEMBL135986 1 6.52
CHEMBL93 ZILEUTON 4.0 1 6.30
CHEMBL274642 BW-755C 1 5.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL59356 ATRELEUTON IC50 = 23.0 nM 7.64
CHEMBL132859 IC50 = 160.0 nM 6.80
CHEMBL135483 IC50 = 300.0 nM 6.52
CHEMBL135986 IC50 = 300.0 nM 6.52
CHEMBL93 ZILEUTON IC50 = 500.0 nM 6.30
CHEMBL274642 BW-755C IC50 = 5600.0 nM 5.25