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Assay Detail

CHEMBL4767839

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

Binding
Inhibition of human 5-Lipoxygenase using H2DCFDA as substrate preincubated for 5 mins and measured by Spectrophotometric assay
7
Total Activities
7
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

Tuning melatonin receptor subtype selectivity in oxadiazolone-based analogues: Discovery of QR2 ligands and NRF2 activators with neurogenic properties.
Herrera-Arozamena C,Estrada-Valencia M,Pérez C,Lagartera L,Morales-García JA,Pérez-Castillo A,Franco-Gonzalez JF,Michalska P,Duarte P,León R,López MG,Mills A,Gago F,García-Yagüe ÁJ,Fernández-Ginés R,Cuadrado A,Rodríguez-Franco MI
Eur J Med Chem (2020) 190 : 112090 -112090
PubMed 32018096 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 5.29 7.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL52 NORDIHYDROGUAIARETIC ACID 1 7.01
CHEMBL93 ZILEUTON 4.0 1 6.82
CHEMBL4797429 1 4.90
CHEMBL4778192 1 4.65
CHEMBL4794879 1 4.22
CHEMBL4793947 1 4.13
CHEMBL4783536 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL52 NORDIHYDROGUAIARETIC ACID IC50 = 97.0 nM 7.01
CHEMBL93 ZILEUTON IC50 = 150.0 nM 6.82
CHEMBL4797429 IC50 = 12500.0 nM 4.90
CHEMBL4778192 IC50 = 22500.0 nM 4.65
CHEMBL4794879 IC50 = 60600.0 nM 4.22
CHEMBL4793947 IC50 = 74200.0 nM 4.13
CHEMBL4783536 IC50 > 100000.0 nM -