Assay Detail
Functional
CHEMBL619910
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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.
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 | % | - |