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Assay Detail

CHEMBL3398679

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

Binding
Inhibition of 5-LO in human human PMNL assessed as reduction in 5-LO product formation pre-incubated for 15 mins before addition of arachidonic acid substrate by HPLC analysis
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

SAR-studies of γ-secretase modulators with PPARγ-agonistic and 5-lipoxygenase-inhibitory activity for Alzheimer's disease.
Flesch D, Ness J, Lamers C, Dehm F, Popella S, Steri R, Ogorek I, Hieke M, Dannhardt G, Werz O, Weggen S, Schubert-Zsilavecz M.
Bioorg Med Chem Lett (2015) 25 : 841 -846
PubMed 25575659 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 6.14 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3397723 1 6.70
CHEMBL3397721 1 6.70
CHEMBL1819479 1 6.70
CHEMBL3397726 1 6.60
CHEMBL3397717 1 6.52
CHEMBL3397716 1 6.52
CHEMBL3397728 1 6.30
CHEMBL3397715 1 6.30
CHEMBL3397710 1 6.26
CHEMBL461883 1 6.22
CHEMBL3397719 1 6.16
CHEMBL3397711 1 6.12
CHEMBL1171834 1 6.10
CHEMBL3397720 1 6.05
CHEMBL3397724 1 6.05
CHEMBL3397727 1 5.77
CHEMBL3397709 1 5.68
CHEMBL3397718 1 5.64
CHEMBL3397708 1 5.24
CHEMBL3397722 1 5.17
CHEMBL3397713 1 -
CHEMBL3397714 1 -
CHEMBL3397712 1 -
CHEMBL3397725 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3397723 IC50 = 200.0 nM 6.70
CHEMBL3397721 IC50 = 200.0 nM 6.70
CHEMBL1819479 IC50 = 200.0 nM 6.70
CHEMBL3397726 IC50 = 250.0 nM 6.60
CHEMBL3397717 IC50 = 300.0 nM 6.52
CHEMBL3397716 IC50 = 300.0 nM 6.52
CHEMBL3397728 IC50 = 500.0 nM 6.30
CHEMBL3397715 IC50 = 500.0 nM 6.30
CHEMBL3397710 IC50 = 550.0 nM 6.26
CHEMBL461883 IC50 = 600.0 nM 6.22
CHEMBL3397719 IC50 = 700.0 nM 6.16
CHEMBL3397711 IC50 = 750.0 nM 6.12
CHEMBL1171834 IC50 = 800.0 nM 6.10
CHEMBL3397720 IC50 = 900.0 nM 6.05
CHEMBL3397724 IC50 = 900.0 nM 6.05
CHEMBL3397727 IC50 = 1700.0 nM 5.77
CHEMBL3397709 IC50 = 2100.0 nM 5.68
CHEMBL3397718 IC50 = 2300.0 nM 5.64
CHEMBL3397708 IC50 = 5700.0 nM 5.24
CHEMBL3397722 IC50 = 6700.0 nM 5.17
CHEMBL3397713 IC50 - -
CHEMBL3397714 IC50 - -
CHEMBL3397712 IC50 - -
CHEMBL3397725 IC50 - -