Assay Detail
Binding
CHEMBL620873
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5-lipoxygenase Inhibitory activity was measured by enzyme immunoassay using human whole blood stimulated with calcium ionophore (A23187) and LTB4 (leukotriene B4)
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Blood |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Polyunsaturated fatty acid 5-lipoxygenase (CHEMBL215) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
(R)-(+)-N-[3-[5-[(4-fluorophenyl)methyl]-2-thienyl]-1-methyl- 2-propynyl]-N-hydroxyurea (ABT-761), a second-generation 5-lipoxygenase inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 6.87 | 7.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1907933 | — | — | 1 | 7.30 |
| CHEMBL264717 | — | — | 1 | 7.22 |
| CHEMBL90552 | — | — | 1 | 7.10 |
| CHEMBL59598 | — | — | 1 | 7.10 |
| CHEMBL145318 | — | — | 1 | 6.80 |
| CHEMBL59356 | ATRELEUTON | 2.0 | 1 | 6.80 |
| CHEMBL144028 | — | — | 1 | 6.70 |
| CHEMBL145306 | — | — | 1 | 6.70 |
| CHEMBL93 | ZILEUTON | 4.0 | 1 | 6.13 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1907933 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL264717 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL90552 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL59598 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL145318 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL59356 | ATRELEUTON | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL144028 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL145306 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL93 | ZILEUTON | IC50 | = | 740.0 | nM | 6.13 |