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Assay Detail

CHEMBL4053620

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

Binding
Inhibition of 5-LO in human peripheral blood neutrophils using arachidonic acid as substrate preincubated for 15 mins followed by substrate addition measured after 10 mins in presence of Ca2+ ionophore A23187 by RP-HPLC analysis
16
Total Activities
16
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

Evaluation of Dual 5-Lipoxygenase/Microsomal Prostaglandin E2 Synthase-1 Inhibitory Effect of Natural and Synthetic Acronychia-Type Isoprenylated Acetophenones.
Svouraki A, Garscha U, Kouloura E, Pace S, Pergola C, Krauth V, Rossi A, Sautebin L, Halabalaki M, Werz O, Gaboriaud-Kolar N, Skaltsounis AL.
J Nat Prod (2017) 80 : 699 -706
PubMed 28240894 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 5.40 5.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1242095 1 5.85
CHEMBL93 ZILEUTON 4.0 1 5.77
CHEMBL488313 1 5.64
CHEMBL1984096 1 5.35
CHEMBL4096534 1 5.30
CHEMBL4077368 1 5.30
CHEMBL4078358 1 5.28
CHEMBL4087914 1 5.20
CHEMBL4075212 1 5.20
CHEMBL1992376 ACROFOLIONE A 1 5.14
CHEMBL29097 1 -
CHEMBL4069303 1 -
CHEMBL4080027 1 -
CHEMBL4104264 1 -
CHEMBL1241050 1 -
CHEMBL4101532 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1242095 IC50 = 1400.0 nM 5.85
CHEMBL93 ZILEUTON IC50 = 1700.0 nM 5.77
CHEMBL488313 IC50 = 2300.0 nM 5.64
CHEMBL1984096 IC50 = 4500.0 nM 5.35
CHEMBL4096534 IC50 = 5000.0 nM 5.30
CHEMBL4077368 IC50 = 5000.0 nM 5.30
CHEMBL4078358 IC50 = 5300.0 nM 5.28
CHEMBL4087914 IC50 = 6300.0 nM 5.20
CHEMBL4075212 IC50 = 6300.0 nM 5.20
CHEMBL1992376 ACROFOLIONE A IC50 = 7300.0 nM 5.14
CHEMBL29097 IC50 - -
CHEMBL4069303 IC50 > 10000.0 nM -
CHEMBL4080027 IC50 > 10000.0 nM -
CHEMBL4104264 IC50 > 10000.0 nM -
CHEMBL1241050 IC50 - -
CHEMBL4101532 IC50 > 10000.0 nM -