Assay Detail
Binding
CHEMBL990977
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Inhibition of leukotriene A4 hydrolase activity in CD1 mouse whole blood assessed as A-23187-stimulated LTB4 production after 15 mins by enzyme immunoassay
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Tissue | Blood |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 6.84 | 7.34 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL481351 | — | — | 1 | 7.34 |
| CHEMBL481863 | — | — | 1 | 7.29 |
| CHEMBL446514 | — | — | 1 | 7.23 |
| CHEMBL472138 | — | — | 1 | 7.22 |
| CHEMBL481280 | — | — | 1 | 7.06 |
| CHEMBL518156 | — | — | 1 | 7.04 |
| CHEMBL480131 | — | — | 1 | 7.03 |
| CHEMBL481343 | — | — | 1 | 7.00 |
| CHEMBL521259 | — | — | 1 | 7.00 |
| CHEMBL479383 | — | — | 1 | 6.98 |
| CHEMBL518155 | — | — | 1 | 6.96 |
| CHEMBL480137 | — | — | 1 | 6.92 |
| CHEMBL480336 | — | — | 1 | 6.89 |
| CHEMBL480130 | — | — | 1 | 6.85 |
| CHEMBL517533 | — | — | 1 | 6.82 |
| CHEMBL482058 | — | — | 1 | 6.80 |
| CHEMBL482056 | — | — | 1 | 6.80 |
| CHEMBL470929 | — | — | 1 | 6.77 |
| CHEMBL481173 | — | — | 1 | 6.75 |
| CHEMBL479382 | — | — | 1 | 6.68 |
| CHEMBL520942 | — | — | 1 | 6.64 |
| CHEMBL454760 | — | — | 1 | 6.64 |
| CHEMBL479752 | — | — | 1 | 6.60 |
| CHEMBL470753 | — | — | 1 | 6.55 |
| CHEMBL511292 | — | — | 1 | 6.52 |
| CHEMBL480136 | — | — | 1 | 6.44 |
| CHEMBL480327 | — | — | 1 | 6.37 |
| CHEMBL482057 | — | — | 1 | 6.29 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL481351 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL481863 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL446514 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL472138 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL481280 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL518156 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL480131 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL481343 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL521259 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL479383 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL518155 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL480137 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL480336 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL480130 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL517533 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL482058 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL482056 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL470929 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL481173 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL479382 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL520942 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL454760 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL479752 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL470753 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL511292 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL480136 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL480327 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL482057 | — | IC50 | = | 510.0 | nM | 6.29 |