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Assay Detail

CHEMBL1781670

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

Binding
Inhibition of 5-lipoxygenase in A23187-stimulated human PMNL assessed as enzyme product formation preincubated 15 mins by RP-HPLC analysis in presence of exogenous arachidonic acid
26
Total Activities
26
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

Identification of 2-mercaptohexanoic acids as dual inhibitors of 5-lipoxygenase and microsomal prostaglandin E₂ synthase-1.
Greiner C, Zettl H, Koeberle A, Pergola C, Northoff H, Schubert-Zsilavecz M, Werz O.
Bioorg Med Chem (2011) 19 : 3394 -3401
PubMed 21570310 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 5.81 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL314360 1 7.10
CHEMBL29097 1 7.05
CHEMBL1780187 1 6.10
CHEMBL563351 1 6.05
CHEMBL551479 1 5.96
CHEMBL558072 1 5.85
CHEMBL563546 1 5.85
CHEMBL551884 1 5.82
CHEMBL564017 1 5.80
CHEMBL561284 1 5.80
CHEMBL563311 1 5.80
CHEMBL551480 1 5.70
CHEMBL559752 1 5.70
CHEMBL558141 1 5.52
CHEMBL549723 1 5.32
CHEMBL560484 1 5.32
CHEMBL550332 1 5.32
CHEMBL557342 1 5.28
CHEMBL552347 1 5.02
CHEMBL551420 1 -
CHEMBL1780186 1 -
CHEMBL1780185 1 -
CHEMBL1780184 1 -
CHEMBL560205 1 -
CHEMBL561006 1 -
CHEMBL562786 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL314360 IC50 = 80.0 nM 7.10
CHEMBL29097 IC50 = 90.0 nM 7.05
CHEMBL1780187 IC50 = 800.0 nM 6.10
CHEMBL563351 IC50 = 900.0 nM 6.05
CHEMBL551479 IC50 = 1100.0 nM 5.96
CHEMBL558072 IC50 = 1400.0 nM 5.85
CHEMBL563546 IC50 = 1400.0 nM 5.85
CHEMBL551884 IC50 = 1500.0 nM 5.82
CHEMBL564017 IC50 = 1600.0 nM 5.80
CHEMBL561284 IC50 = 1600.0 nM 5.80
CHEMBL563311 IC50 = 1600.0 nM 5.80
CHEMBL551480 IC50 = 2000.0 nM 5.70
CHEMBL559752 IC50 = 2000.0 nM 5.70
CHEMBL558141 IC50 = 3000.0 nM 5.52
CHEMBL549723 IC50 = 4800.0 nM 5.32
CHEMBL560484 IC50 = 4800.0 nM 5.32
CHEMBL550332 IC50 = 4800.0 nM 5.32
CHEMBL557342 IC50 = 5200.0 nM 5.28
CHEMBL552347 IC50 = 9500.0 nM 5.02
CHEMBL551420 IC50 > 10000.0 nM -
CHEMBL1780186 IC50 > 10000.0 nM -
CHEMBL1780185 IC50 > 10000.0 nM -
CHEMBL1780184 IC50 > 10000.0 nM -
CHEMBL560205 IC50 > 10000.0 nM -
CHEMBL561006 IC50 > 10000.0 nM -
CHEMBL562786 IC50 > 10000.0 nM -