Assay Detail
Binding
CHEMBL619246
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In vitro test for inhibition of 5-lipoxygenase in cell-free preparations from rat PMN leukocytes
41
Total Activities
41
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Polyunsaturated fatty acid 5-lipoxygenase (CHEMBL312) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Substituted thiopyrano[2,3,4-c,d]indoles as potent, selective, and orally active inhibitors of 5-lipoxygenase. Synthesis and biological evaluation of L-691,816.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 41 | 6.63 | 7.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL81812 | — | — | 1 | 7.80 |
| CHEMBL275887 | — | — | 1 | 7.77 |
| CHEMBL96844 | — | — | 1 | 7.70 |
| CHEMBL92469 | — | — | 1 | 7.52 |
| CHEMBL319661 | — | — | 1 | 7.46 |
| CHEMBL275474 | — | — | 1 | 7.46 |
| CHEMBL96253 | — | — | 1 | 7.44 |
| CHEMBL96767 | — | — | 1 | 7.40 |
| CHEMBL329217 | — | — | 1 | 7.40 |
| CHEMBL96300 | — | — | 1 | 7.35 |
| CHEMBL295761 | — | — | 1 | 7.22 |
| CHEMBL274824 | — | — | 1 | 7.17 |
| CHEMBL94307 | — | — | 1 | 6.92 |
| CHEMBL96353 | — | — | 1 | 6.89 |
| CHEMBL96424 | — | — | 1 | 6.89 |
| CHEMBL317085 | — | — | 1 | 6.89 |
| CHEMBL93022 | — | — | 1 | 6.85 |
| CHEMBL328967 | — | — | 1 | 6.85 |
| CHEMBL96899 | — | — | 1 | 6.70 |
| CHEMBL96342 | — | — | 1 | 6.70 |
| CHEMBL319951 | — | — | 1 | 6.50 |
| CHEMBL319478 | — | — | 1 | 6.48 |
| CHEMBL96423 | — | — | 1 | 6.48 |
| CHEMBL327889 | — | — | 1 | 6.46 |
| CHEMBL450016 | — | — | 1 | 6.46 |
| CHEMBL96611 | — | — | 1 | 6.40 |
| CHEMBL430487 | — | — | 1 | 6.40 |
| CHEMBL329529 | — | — | 1 | 6.30 |
| CHEMBL50170 | — | — | 1 | 6.22 |
| CHEMBL96259 | — | — | 1 | 6.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL81812 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL275887 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL96844 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL92469 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL319661 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL275474 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL96253 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL96767 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL329217 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL96300 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL295761 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL274824 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL94307 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL317085 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL96424 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL96353 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL93022 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL328967 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL96899 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL96342 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL319951 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL96423 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL319478 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL327889 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL450016 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL96611 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL430487 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL329529 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL50170 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL96259 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL96412 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL96241 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL92426 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL96169 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL330189 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL319877 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL317482 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL96635 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL96921 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL96688 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL96841 | — | IC50 | > | 2000.0 | nM | - |