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Assay Detail

CHEMBL619875

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

Binding
Inhibition of 5-lipoxygenase in human whole blood.
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Blood
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

(Methoxyalkyl)thiazoles: a new series of potent, selective, and orally active 5-lipoxygenase inhibitors displaying high enantioselectivity.
Bird, Bruneau P, Crawley GC, Edwards MP, Foster SJ, Girodeau JM, Kingston JF, McMillan RM.
J Med Chem (1991) 34 : 2176 -2186
PubMed 1648621 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.77 6.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL423835 ZM-211965 1 6.40
CHEMBL70191 1 6.30
CHEMBL20905 1 6.22
CHEMBL430614 1 5.32
CHEMBL416735 1 5.20
CHEMBL304320 1 5.16
CHEMBL70580 1 -
CHEMBL308453 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL423835 ZM-211965 IC50 = 400.0 nM 6.40
CHEMBL70191 IC50 = 500.0 nM 6.30
CHEMBL20905 IC50 = 600.0 nM 6.22
CHEMBL430614 IC50 = 4800.0 nM 5.32
CHEMBL416735 IC50 = 6300.0 nM 5.20
CHEMBL304320 IC50 = 7000.0 nM 5.16
CHEMBL70580 IC50 > 40000.0 nM -
CHEMBL308453 IC50 ~ 40000.0 nM -