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Assay Detail

CHEMBL1012771

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Binding
Inhibition of 5-LO in PMNL cells
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Pirinixic acid derivatives as novel dual inhibitors of microsomal prostaglandin E2 synthase-1 and 5-lipoxygenase.
Koeberle A, Zettl H, Greiner C, Wurglics M, Schubert-Zsilavecz M, Werz O.
J Med Chem (2008) 51 : 8068 -8076
PubMed 19053751 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.16 7.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL29097 1 7.05
CHEMBL314360 1 6.96
CHEMBL456792 1 6.40
CHEMBL463776 1 6.30
CHEMBL459722 1 6.22
CHEMBL460616 1 6.16
CHEMBL462523 1 6.00
CHEMBL457000 1 5.82
CHEMBL518038 1 5.39
CHEMBL455936 1 5.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL29097 IC50 = 90.0 nM 7.05
CHEMBL314360 IC50 = 110.0 nM 6.96
CHEMBL456792 IC50 = 400.0 nM 6.40
CHEMBL463776 IC50 = 500.0 nM 6.30
CHEMBL459722 IC50 = 600.0 nM 6.22
CHEMBL460616 IC50 = 700.0 nM 6.16
CHEMBL462523 IC50 = 1000.0 nM 6.00
CHEMBL457000 IC50 = 1500.0 nM 5.82
CHEMBL518038 IC50 = 4100.0 nM 5.39
CHEMBL455936 IC50 = 5000.0 nM 5.30