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Assay Detail

CHEMBL620775

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

Binding
Inhibition of [14C]arachidonic acid conversion to 5-HETE by broken cell 5-lipoxygenase in vitro (guinea pig PMN)
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Enzymic and nonenzymic lipid peroxidation: inhibition by substituted phenoxazines
Yu MJ, McCowan JR, Bertsch B, Ho PP
Bioorg Med Chem Lett (1991) 1 : 107 -110
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 6.55 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL276850 PHENOXAZINE 1 7.70
CHEMBL273714 1 7.46
CHEMBL12681 1 7.19
CHEMBL12361 1 7.07
CHEMBL12362 1 7.06
CHEMBL12456 1 6.60
CHEMBL12534 1 6.38
CHEMBL274905 1 6.21
CHEMBL274541 1 6.11
CHEMBL273438 1 5.92
CHEMBL11984 1 5.55
CHEMBL12816 1 5.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL276850 PHENOXAZINE IC50 = 20.0 nM 7.70
CHEMBL273714 IC50 = 35.0 nM 7.46
CHEMBL12681 IC50 = 65.0 nM 7.19
CHEMBL12361 IC50 = 85.0 nM 7.07
CHEMBL12362 IC50 = 87.0 nM 7.06
CHEMBL12456 IC50 = 250.0 nM 6.60
CHEMBL12534 IC50 = 420.0 nM 6.38
CHEMBL274905 IC50 = 610.0 nM 6.21
CHEMBL274541 IC50 = 770.0 nM 6.11
CHEMBL273438 IC50 = 1200.0 nM 5.92
CHEMBL11984 IC50 = 2800.0 nM 5.55
CHEMBL12816 IC50 = 4600.0 nM 5.34