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Assay Detail

CHEMBL619910

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

Functional
Inhibition of 5-lipoxygenase by measuring 5-HETE levels in RBL-1 cell-free supernatant
25
Total Activities
25
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type RBL-1
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Dibenzoxepinone hydroxylamines and hydroxamic acids: dual inhibitors of cyclooxygenase and 5-lipoxygenase with potent topical antiinflammatory activity.
Hamer RR, Tegeler JJ, Kurtz ES, Allen RC, Bailey SC, Elliott ME, Hellyer L, Helsley GC, Przekop P, Freed BS, White J, Martin LL.
J Med Chem (1996) 39 : 246 -252
PubMed 8568814 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 6.43 8.00
Inhibition 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL82292 1 8.00
CHEMBL82680 1 7.70
CHEMBL52 NORDIHYDROGUAIARETIC ACID 1 6.92
CHEMBL83482 1 6.89
CHEMBL83425 1 6.82
CHEMBL314856 1 6.72
CHEMBL85455 1 6.68
CHEMBL83990 1 6.62
CHEMBL84599 1 6.50
CHEMBL84785 1 6.35
CHEMBL313428 1 6.32
CHEMBL85776 1 6.32
CHEMBL86214 1 6.24
CHEMBL85113 1 6.24
CHEMBL84670 1 6.21
CHEMBL311433 1 6.18
CHEMBL315944 1 6.17
CHEMBL2114190 1 5.92
CHEMBL312837 1 5.91
CHEMBL82325 1 5.89
CHEMBL431007 1 5.70
CHEMBL310794 1 5.05
CHEMBL33211 ISOXEPAC 2.0 1 -
CHEMBL314595 1 -
CHEMBL315801 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL82292 IC50 = 10.0 nM 8.00
CHEMBL82680 IC50 = 20.0 nM 7.70
CHEMBL52 NORDIHYDROGUAIARETIC ACID IC50 = 120.0 nM 6.92
CHEMBL83482 IC50 = 130.0 nM 6.89
CHEMBL83425 IC50 = 150.0 nM 6.82
CHEMBL314856 IC50 = 190.0 nM 6.72
CHEMBL85455 IC50 = 210.0 nM 6.68
CHEMBL83990 IC50 = 240.0 nM 6.62
CHEMBL84599 IC50 = 320.0 nM 6.50
CHEMBL84785 IC50 = 450.0 nM 6.35
CHEMBL313428 IC50 = 480.0 nM 6.32
CHEMBL85776 IC50 = 480.0 nM 6.32
CHEMBL86214 IC50 = 580.0 nM 6.24
CHEMBL85113 IC50 = 580.0 nM 6.24
CHEMBL84670 IC50 = 620.0 nM 6.21
CHEMBL311433 IC50 = 660.0 nM 6.18
CHEMBL315944 IC50 = 670.0 nM 6.17
CHEMBL2114190 IC50 = 1190.0 nM 5.92
CHEMBL312837 IC50 = 1230.0 nM 5.91
CHEMBL82325 IC50 = 1300.0 nM 5.89
CHEMBL431007 IC50 = 2000.0 nM 5.70
CHEMBL310794 IC50 = 9000.0 nM 5.05
CHEMBL33211 ISOXEPAC Inhibition = 1.5 % -
CHEMBL314595 IC50 > 50000.0 nM -
CHEMBL315801 Inhibition = 94.0 % -