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Assay Detail

CHEMBL618765

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

Binding
Inhibition of 5-Lipoxygenase (5-LOX)
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

New cyclooxygenase-2/5-lipoxygenase inhibitors. 3. 7-tert-butyl-2, 3-dihydro-3,3-dimethylbenzofuran derivatives as gastrointestinal safe antiinflammatory and analgesic agents: variations at the 5 position.
Janusz JM, Young PA, Ridgeway JM, Scherz MW, Enzweiler K, Wu LI, Gan L, Chen J, Kellstein DE, Green SA, Tulich JL, Rosario-Jansen T, Magrisso IJ, Wehmeyer KR, Kuhlenbeck DL, Eichhold TH, Dobson RL.
J Med Chem (1998) 41 : 3515 -3529
PubMed 9719605 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 4.97 5.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL13878 TEBUFELONE 2.0 1 5.52
CHEMBL2112567 1 5.40
CHEMBL117911 1 5.22
CHEMBL326295 1 5.12
CHEMBL118839 1 5.05
CHEMBL332028 1 5.00
CHEMBL332937 1 5.00
CHEMBL119433 1 4.92
CHEMBL117615 1 4.66
CHEMBL422075 1 4.52
CHEMBL419947 1 4.30
CHEMBL119170 1 -
CHEMBL122065 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL13878 TEBUFELONE IC50 = 3000.0 nM 5.52
CHEMBL2112567 IC50 = 4000.0 nM 5.40
CHEMBL117911 IC50 = 6000.0 nM 5.22
CHEMBL326295 IC50 = 7500.0 nM 5.12
CHEMBL118839 IC50 = 9000.0 nM 5.05
CHEMBL332028 IC50 = 10000.0 nM 5.00
CHEMBL332937 IC50 = 10000.0 nM 5.00
CHEMBL119433 IC50 = 12000.0 nM 4.92
CHEMBL117615 IC50 = 22000.0 nM 4.66
CHEMBL422075 IC50 = 30000.0 nM 4.52
CHEMBL419947 IC50 = 50000.0 nM 4.30
CHEMBL119170 IC50 > 50000.0 nM -
CHEMBL122065 IC50 > 50000.0 nM -