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Assay Detail

CHEMBL618065

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

Binding
Inhibition of 5-lipoxygenase of rat basophilic leukemia (RBL) cell cytosolic enzymes
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type RBL-1
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

A novel series of highly potent 5-lipoxygenase inhibitors; 2-aryldienylbenzoxazoles
Kosaka T, Ochiai K, Ohba S, Wakabayashi T, Murota S
Bioorg Med Chem Lett (1995) 5 : 35 -38
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.60 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL413111 1 7.70
CHEMBL125041 1 7.52
CHEMBL332082 1 6.89
CHEMBL124994 1 6.82
CHEMBL125374 1 6.77
CHEMBL339596 1 6.60
CHEMBL125780 1 6.58
CHEMBL340121 1 6.54
CHEMBL125151 1 6.52
CHEMBL125074 1 6.48
CHEMBL125197 1 6.43
CHEMBL124538 1 6.42
CHEMBL17347 ETHYL CAFFEATE 1 5.94
CHEMBL125727 1 5.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL413111 IC50 = 20.0 nM 7.70
CHEMBL125041 IC50 = 30.0 nM 7.52
CHEMBL332082 IC50 = 130.0 nM 6.89
CHEMBL124994 IC50 = 150.0 nM 6.82
CHEMBL125374 IC50 = 170.0 nM 6.77
CHEMBL339596 IC50 = 250.0 nM 6.60
CHEMBL125780 IC50 = 260.0 nM 6.58
CHEMBL340121 IC50 = 290.0 nM 6.54
CHEMBL125151 IC50 = 300.0 nM 6.52
CHEMBL125074 IC50 = 330.0 nM 6.48
CHEMBL125197 IC50 = 370.0 nM 6.43
CHEMBL124538 IC50 = 380.0 nM 6.42
CHEMBL17347 ETHYL CAFFEATE IC50 = 1150.0 nM 5.94
CHEMBL125727 IC50 = 5800.0 nM 5.24