Assay Detail
Binding
CHEMBL618007
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Inhibition of 5-lipoxygenase from human whole blood
23
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Blood |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Polyunsaturated fatty acid 5-lipoxygenase (CHEMBL215) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Conformational analysis of 5-lipoxygenase inhibitors: role of the substituents in chiral recognition and on the active conformations of the (methoxyalkyl)thiazole and methoxytetrahydropyran series.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 6.23 | 7.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL20403 | ZD-2138 | — | 1 | 7.57 |
| CHEMBL2092747 | — | — | 1 | 7.22 |
| CHEMBL20749 | — | — | 1 | 7.16 |
| CHEMBL21401 | — | — | 1 | 7.00 |
| CHEMBL21383 | — | — | 1 | 6.82 |
| CHEMBL21764 | — | — | 1 | 6.77 |
| CHEMBL423835 | ZM-211965 | — | 1 | 6.40 |
| CHEMBL21908 | — | — | 1 | 6.36 |
| CHEMBL20953 | — | — | 3 | 6.30 |
| CHEMBL434392 | — | — | 1 | 6.29 |
| CHEMBL20905 | — | — | 1 | 6.22 |
| CHEMBL22106 | — | — | 1 | 6.13 |
| CHEMBL21841 | — | — | 1 | 5.96 |
| CHEMBL2092993 | — | — | 1 | 5.72 |
| CHEMBL20448 | — | — | 1 | 5.64 |
| CHEMBL416735 | — | — | 1 | 5.20 |
| CHEMBL277212 | — | — | 1 | 5.00 |
| CHEMBL21609 | — | — | 1 | 4.40 |
| CHEMBL430908 | — | — | 1 | - |
| CHEMBL433817 | — | — | 1 | - |
| CHEMBL277037 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL20403 | ZD-2138 | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL2092747 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL20749 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL21401 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL21383 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL21764 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL423835 | ZM-211965 | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL21908 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL20953 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL434392 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL20905 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL20953 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL22106 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL21841 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL2092993 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL20448 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL416735 | — | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL277212 | — | IC50 | = | 9900.0 | nM | 5.00 |
| CHEMBL21609 | — | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL430908 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL433817 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL20953 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL277037 | — | IC50 | > | 40000.0 | nM | - |