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Assay Detail

CHEMBL4273246

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

Binding
Inhibition of human 5-lipoxygenase using arachidonic acid as substrate pretreated for 10 mins followed by substrate and ATP addition and measured after 20 mins by H2DCFDA probe based fluorescence assay
25
Total Activities
25
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

Neurogenic and neuroprotective donepezil-flavonoid hybrids with sigma-1 affinity and inhibition of key enzymes in Alzheimer's disease.
Estrada Valencia M, Herrera-Arozamena C, de Andrés L, Pérez C, Morales-García JA, Pérez-Castillo A, Ramos E, Romero A, Viña D, Yáñez M, Laurini E, Pricl S, Rodríguez-Franco MI.
Eur J Med Chem (2018) 156 : 534 -553
PubMed 30025348 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 4.99 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL52 NORDIHYDROGUAIARETIC ACID 1 7.00
CHEMBL93 ZILEUTON 4.0 1 6.82
CHEMBL4280725 1 5.38
CHEMBL4277548 1 5.01
CHEMBL4284165 1 4.82
CHEMBL4292477 1 4.54
CHEMBL4287970 1 4.13
CHEMBL4285912 1 4.11
CHEMBL4291372 1 4.08
CHEMBL4277332 1 4.02
CHEMBL4295144 1 -
CHEMBL4286799 1 -
CHEMBL4283450 1 -
CHEMBL4291296 1 -
CHEMBL4285779 1 -
CHEMBL4294783 1 -
CHEMBL4287548 1 -
CHEMBL4294609 1 -
CHEMBL4282527 1 -
CHEMBL4290401 1 -
CHEMBL4293801 1 -
CHEMBL972 SELEGILINE 4.0 1 -
CHEMBL92401 IPRONIAZID 2.0 1 -
CHEMBL4283079 1 -
CHEMBL86304 MOCLOBEMIDE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL52 NORDIHYDROGUAIARETIC ACID IC50 = 100.0 nM 7.00
CHEMBL93 ZILEUTON IC50 = 150.0 nM 6.82
CHEMBL4280725 IC50 = 4200.0 nM 5.38
CHEMBL4277548 IC50 = 9800.0 nM 5.01
CHEMBL4284165 IC50 = 15100.0 nM 4.82
CHEMBL4292477 IC50 = 28900.0 nM 4.54
CHEMBL4287970 IC50 = 74300.0 nM 4.13
CHEMBL4285912 IC50 = 77600.0 nM 4.11
CHEMBL4291372 IC50 = 82400.0 nM 4.08
CHEMBL4277332 IC50 = 95100.0 nM 4.02
CHEMBL4295144 IC50 > 100000.0 nM -
CHEMBL4286799 IC50 > 100000.0 nM -
CHEMBL4283450 IC50 > 100000.0 nM -
CHEMBL4291296 IC50 > 100000.0 nM -
CHEMBL4285779 IC50 > 100000.0 nM -
CHEMBL4294783 IC50 > 100000.0 nM -
CHEMBL4287548 IC50 > 100000.0 nM -
CHEMBL4294609 IC50 - -
CHEMBL4282527 IC50 > 100000.0 nM -
CHEMBL4290401 IC50 > 100000.0 nM -
CHEMBL4293801 IC50 > 100000.0 nM -
CHEMBL972 SELEGILINE IC50 - -
CHEMBL92401 IPRONIAZID IC50 - -
CHEMBL4283079 IC50 > 100000.0 nM -
CHEMBL86304 MOCLOBEMIDE IC50 - -