Assay Detail
Functional
CHEMBL619242
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of 5-lipoxygenase measured by the reduction of leukotriene B4 (LTB4) in intact basophilic rat leukemia cells
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Polyunsaturated fatty acid 5-lipoxygenase (CHEMBL312) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Design of 5-(3,5-di-tert-butyl-4-hydroxyphenyl)-1,3,4-thiadiazoles, -1,3,4-oxadiazoles, and -1,2,4-triazoles as orally-active, nonulcerogenic antiinflammatory agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 5.65 | 6.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL12395 | — | — | 1 | 6.68 |
| CHEMBL273941 | — | — | 1 | 6.24 |
| CHEMBL12219 | — | — | 1 | 6.16 |
| CHEMBL12809 | — | — | 1 | 5.96 |
| CHEMBL12532 | — | — | 1 | 5.92 |
| CHEMBL16977 | — | — | 1 | 5.85 |
| CHEMBL417073 | — | — | 1 | 5.85 |
| CHEMBL12572 | — | — | 1 | 5.80 |
| CHEMBL94851 | — | — | 1 | 5.75 |
| CHEMBL12302 | — | — | 1 | 5.62 |
| CHEMBL275909 | — | — | 1 | 5.62 |
| CHEMBL122193 | — | — | 1 | 5.55 |
| CHEMBL12234 | — | — | 1 | 5.35 |
| CHEMBL276916 | — | — | 1 | 5.32 |
| CHEMBL12154 | — | — | 1 | 5.29 |
| CHEMBL16827 | — | — | 1 | 5.23 |
| CHEMBL12483 | — | — | 1 | 4.96 |
| CHEMBL509 | MECLOFENAMIC ACID | 4.0 | 1 | 4.62 |
| CHEMBL275445 | — | — | 1 | - |
| CHEMBL273956 | — | — | 1 | - |
| CHEMBL12371 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL12395 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL273941 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL12219 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL12809 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL12532 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL16977 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL417073 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL12572 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL94851 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL12302 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL275909 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL122193 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL12234 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL276916 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL12154 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL16827 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL12483 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL509 | MECLOFENAMIC ACID | IC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL275445 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL273956 | — | IC50 | > | 32000.0 | nM | - |
| CHEMBL12371 | — | IC50 | > | 32000.0 | nM | - |