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Assay Detail

CHEMBL618060

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Functional
Inhibitory activity against 5-lipoxygenase catalysis (5-LO) in sonicated rat basophilic leukemia cell lysate
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Polyunsaturated fatty acid 5-lipoxygenase (CHEMBL312)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Nonsteroidal anti-inflammatory drugs as scaffolds for the design of 5-lipoxygenase inhibitors.
Kolasa T, Brooks CD, Rodriques KE, Summers JB, Dellaria JF, Hulkower KI, Bouska J, Bell RL, Carter GW.
J Med Chem (1997) 40 : 819 -824
PubMed 9057869 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.74 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL355423 1 6.70
CHEMBL168339 1 6.40
CHEMBL445386 1 6.40
CHEMBL93 ZILEUTON 4.0 1 6.30
CHEMBL167577 1 6.22
CHEMBL166844 1 5.54
CHEMBL166644 1 5.32
CHEMBL6 INDOMETHACIN 4.0 1 4.92
CHEMBL521 IBUPROFEN 4.0 1 4.85
CHEMBL154 NAPROXEN 4.0 1 4.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL355423 IC50 = 200.0 nM 6.70
CHEMBL168339 IC50 = 400.0 nM 6.40
CHEMBL445386 IC50 = 400.0 nM 6.40
CHEMBL93 ZILEUTON IC50 = 500.0 nM 6.30
CHEMBL167577 IC50 = 600.0 nM 6.22
CHEMBL166844 IC50 = 2900.0 nM 5.54
CHEMBL166644 IC50 = 4800.0 nM 5.32
CHEMBL6 INDOMETHACIN IC50 = 12000.0 nM 4.92
CHEMBL521 IBUPROFEN IC50 = 14000.0 nM 4.85
CHEMBL154 NAPROXEN IC50 = 17000.0 nM 4.77