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Assay Detail

CHEMBL768678

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

Functional
In vitro for inhibition of 5-HETE production in isolated rat polymorphonuclear leukocytes (PMNs)
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Polyunsaturated fatty acid 5-lipoxygenase (CHEMBL312)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and antiallergic activity of a novel series of 5-lipoxygenase inhibitors.
Kees KL, Musser JH, Chang J, Skowronek M, Lewis AJ.
J Med Chem (1986) 29 : 2329 -2334
PubMed 2878078 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 5.02 5.97

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL75651 1 5.97
CHEMBL77872 1 5.96
CHEMBL73936 1 5.80
CHEMBL76884 1 5.70
CHEMBL308573 1 5.56
CHEMBL78007 1 5.46
CHEMBL75123 1 5.43
CHEMBL312747 1 5.34
CHEMBL310232 1 5.27
CHEMBL309048 1 5.25
CHEMBL74615 1 5.11
CHEMBL307264 1 4.92
CHEMBL306979 1 4.85
CHEMBL77631 1 4.68
CHEMBL77048 1 4.66
CHEMBL75830 1 4.60
CHEMBL78210 1 4.59
CHEMBL74841 1 4.54
CHEMBL307575 1 4.49
CHEMBL77704 1 4.44
CHEMBL77722 1 4.41
CHEMBL162358 TOMELUKAST 2.0 1 4.39
CHEMBL78026 1 4.12
CHEMBL77668 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL75651 IC50 = 1080.0 nM 5.97
CHEMBL77872 IC50 = 1100.0 nM 5.96
CHEMBL73936 IC50 = 1590.0 nM 5.80
CHEMBL76884 IC50 = 2010.0 nM 5.70
CHEMBL308573 IC50 = 2730.0 nM 5.56
CHEMBL78007 IC50 = 3440.0 nM 5.46
CHEMBL75123 IC50 = 3710.0 nM 5.43
CHEMBL312747 IC50 = 4540.0 nM 5.34
CHEMBL310232 IC50 = 5350.0 nM 5.27
CHEMBL309048 IC50 = 5600.0 nM 5.25
CHEMBL74615 IC50 = 7740.0 nM 5.11
CHEMBL307264 IC50 = 12100.0 nM 4.92
CHEMBL306979 IC50 = 14200.0 nM 4.85
CHEMBL77631 IC50 = 20800.0 nM 4.68
CHEMBL77048 IC50 = 22000.0 nM 4.66
CHEMBL75830 IC50 = 25100.0 nM 4.60
CHEMBL78210 IC50 = 25530.0 nM 4.59
CHEMBL74841 IC50 = 28500.0 nM 4.54
CHEMBL307575 IC50 = 32670.0 nM 4.49
CHEMBL77704 IC50 = 36300.0 nM 4.44
CHEMBL77722 IC50 = 38560.0 nM 4.41
CHEMBL162358 TOMELUKAST IC50 = 41000.0 nM 4.39
CHEMBL78026 IC50 = 76000.0 nM 4.12
CHEMBL77668 IC50 > 50000.0 nM -