Assay Detail
Binding
CHEMBL3096450
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Inhibition of 5-lipoxygenase in A23187-stimulated human polymorphonuclear leukocytes using arachidonic acid as substrate incubated 15 mins prior to substrate addition measured after 10 mins by HPLC analysis
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Polyunsaturated fatty acid 5-lipoxygenase (CHEMBL215) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Aminothiazole-featured pirinixic acid derivatives as dual 5-lipoxygenase and microsomal prostaglandin E2 synthase-1 inhibitors with improved potency and efficiency in vivo.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 6.19 | 7.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL29097 | — | — | 1 | 7.05 |
| CHEMBL3094410 | — | — | 1 | 6.70 |
| CHEMBL3091499 | — | — | 1 | 6.70 |
| CHEMBL3094426 | — | — | 1 | 6.70 |
| CHEMBL3094412 | — | — | 1 | 6.70 |
| CHEMBL3091500 | — | — | 1 | 6.52 |
| CHEMBL3094422 | — | — | 1 | 6.52 |
| CHEMBL3094419 | — | — | 1 | 6.40 |
| CHEMBL3091497 | — | — | 1 | 6.40 |
| CHEMBL3094411 | — | — | 1 | 6.40 |
| CHEMBL3094413 | — | — | 1 | 6.40 |
| CHEMBL3094418 | — | — | 1 | 6.40 |
| CHEMBL3091498 | — | — | 1 | 6.22 |
| CHEMBL3094428 | — | — | 1 | 6.22 |
| CHEMBL3094425 | — | — | 1 | 6.22 |
| CHEMBL3094420 | — | — | 1 | 6.22 |
| CHEMBL3094427 | — | — | 1 | 6.16 |
| CHEMBL3094421 | — | — | 1 | 6.10 |
| CHEMBL3094423 | — | — | 1 | 6.10 |
| CHEMBL3094432 | — | — | 1 | 6.05 |
| CHEMBL3094414 | — | — | 1 | 6.05 |
| CHEMBL3094431 | — | — | 1 | 6.05 |
| CHEMBL93 | ZILEUTON | 4.0 | 1 | 6.05 |
| CHEMBL3094417 | — | — | 1 | 5.85 |
| CHEMBL3094416 | — | — | 1 | 5.82 |
| CHEMBL3094415 | — | — | 1 | 5.82 |
| CHEMBL3091495 | — | — | 1 | 5.54 |
| CHEMBL3094424 | — | — | 1 | 5.48 |
| CHEMBL3094433 | — | — | 1 | 5.44 |
| CHEMBL518038 | — | — | 1 | 5.41 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL29097 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL3094410 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3091499 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3094426 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3094412 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3091500 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL3094422 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL3094419 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL3091497 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL3094411 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL3094413 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL3094418 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL3091498 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL3094428 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL3094420 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL3094425 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL3094427 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL3094421 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL3094423 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL93 | ZILEUTON | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL3094431 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL3094414 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL3094432 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL3094417 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL3094416 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL3094415 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL3091495 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL3094424 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL3094433 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL518038 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL3091496 | — | IC50 | > | 10000.0 | nM | - |