Assay Detail
Binding
CHEMBL939889
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Inhibition of 5-lipoxygenase in A-23817-challenged human neutrophils assessed as 5LO product formation by intact cell based assay in presence of exogenous arachidonic acid
46
Total Activities
46
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
Structural optimization and biological evaluation of 2-substituted 5-hydroxyindole-3-carboxylates as potent inhibitors of human 5-lipoxygenase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 46 | 5.81 | 6.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL529218 | — | — | 1 | 6.80 |
| CHEMBL490461 | — | — | 1 | 6.64 |
| CHEMBL519150 | — | — | 1 | 6.50 |
| CHEMBL519508 | — | — | 1 | 6.47 |
| CHEMBL485312 | — | — | 1 | 6.46 |
| CHEMBL483056 | — | — | 1 | 6.36 |
| CHEMBL521164 | — | — | 1 | 6.35 |
| CHEMBL520474 | — | — | 1 | 6.32 |
| CHEMBL482849 | — | — | 1 | 6.31 |
| CHEMBL484277 | — | — | 1 | 6.30 |
| CHEMBL520317 | — | — | 1 | 6.28 |
| CHEMBL519337 | — | — | 1 | 6.28 |
| CHEMBL484482 | — | — | 1 | 6.22 |
| CHEMBL483677 | — | — | 1 | 6.19 |
| CHEMBL504152 | — | — | 1 | 6.16 |
| CHEMBL490460 | — | — | 1 | 6.15 |
| CHEMBL93 | ZILEUTON | 4.0 | 1 | 6.05 |
| CHEMBL490656 | — | — | 1 | 5.92 |
| CHEMBL523292 | — | — | 1 | 5.92 |
| CHEMBL483878 | — | — | 1 | 5.77 |
| CHEMBL520641 | — | — | 1 | 5.77 |
| CHEMBL508183 | — | — | 1 | 5.77 |
| CHEMBL519847 | — | — | 1 | 5.75 |
| CHEMBL487916 | — | — | 1 | 5.70 |
| CHEMBL485243 | — | — | 1 | 5.62 |
| CHEMBL483884 | — | — | 1 | 5.55 |
| CHEMBL486691 | — | — | 1 | 5.55 |
| CHEMBL520798 | — | — | 1 | 5.55 |
| CHEMBL487915 | — | — | 1 | 5.48 |
| CHEMBL505785 | — | — | 1 | 5.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL529218 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL490461 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL519150 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL519508 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL485312 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL483056 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL521164 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL520474 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL482849 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL484277 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL520317 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL519337 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL484482 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL483677 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL504152 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL490460 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL93 | ZILEUTON | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL490656 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL523292 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL483878 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL520641 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL508183 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL519847 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL487916 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL485243 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL483884 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL486691 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL520798 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL487915 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL505785 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL488740 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL483067 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL523291 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL483689 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL488741 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL483684 | — | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL519029 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL527421 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL521133 | — | IC50 | = | 7200.0 | nM | 5.14 |
| CHEMBL483066 | — | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL450838 | — | IC50 | = | 9800.0 | nM | 5.01 |
| CHEMBL483269 | — | IC50 | = | 12500.0 | nM | 4.90 |
| CHEMBL483037 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL482645 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL484084 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL484083 | — | IC50 | > | 10000.0 | nM | - |