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Assay Detail

CHEMBL615380

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

Binding
Inhibition of 1-lipoxygenase (LOX)in RBL cells
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type RBL
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

New cyclooxygenase-2/5-lipoxygenase inhibitors. 2. 7-tert-butyl-2,3-dihydro-3,3-dimethylbenzofuran derivatives as gastrointestinal safe antiinflammatory and analgesic agents: variations of the dihydrobenzofuran ring.
Janusz JM, Young PA, Scherz MW, Enzweiler K, Wu LI, Gan L, Pikul S, McDow-Dunham KL, Johnson CR, Senanayake CB, Kellstein DE, Green SA, Tulich JL, Rosario-Jansen T, Magrisso IJ, Wehmeyer KR, Kuhlenbeck DL, Eichhold TH, Dobson RL.
J Med Chem (1998) 41 : 1124 -1137
PubMed 9544212 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.08 5.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL13878 TEBUFELONE 2.0 1 5.52
CHEMBL13920 1 5.22
CHEMBL13623 1 5.10
CHEMBL15058 1 5.10
CHEMBL13980 1 5.07
CHEMBL13661 1 4.92
CHEMBL279166 1 4.92
CHEMBL15014 1 4.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL13878 TEBUFELONE IC50 = 3000.0 nM 5.52
CHEMBL13920 IC50 = 6000.0 nM 5.22
CHEMBL13623 IC50 = 8000.0 nM 5.10
CHEMBL15058 IC50 = 8000.0 nM 5.10
CHEMBL13980 IC50 = 8500.0 nM 5.07
CHEMBL13661 IC50 = 12000.0 nM 4.92
CHEMBL279166 IC50 = 12000.0 nM 4.92
CHEMBL15014 IC50 = 18000.0 nM 4.75