Assay Detail
Binding
CHEMBL939890
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Inhibition of human recombinant 5-lipoxygenase expressed in Escherichia coli assessed as 5LO product formation by cell free assay
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 | 6.25 | 7.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL482849 | — | — | 1 | 7.51 |
| CHEMBL529218 | — | — | 1 | 7.42 |
| CHEMBL519337 | — | — | 1 | 7.35 |
| CHEMBL520798 | — | — | 1 | 7.31 |
| CHEMBL519150 | — | — | 1 | 7.17 |
| CHEMBL490656 | — | — | 1 | 7.08 |
| CHEMBL490461 | — | — | 1 | 7.07 |
| CHEMBL484482 | — | — | 1 | 7.02 |
| CHEMBL484277 | — | — | 1 | 7.02 |
| CHEMBL523292 | — | — | 1 | 7.01 |
| CHEMBL520317 | — | — | 1 | 6.89 |
| CHEMBL483056 | — | — | 1 | 6.89 |
| CHEMBL485312 | — | — | 1 | 6.89 |
| CHEMBL519508 | — | — | 1 | 6.85 |
| CHEMBL521164 | — | — | 1 | 6.82 |
| CHEMBL483677 | — | — | 1 | 6.82 |
| CHEMBL520474 | — | — | 1 | 6.77 |
| CHEMBL490460 | — | — | 1 | 6.62 |
| CHEMBL483878 | — | — | 1 | 6.60 |
| CHEMBL485243 | — | — | 1 | 6.52 |
| CHEMBL483884 | — | — | 1 | 6.48 |
| CHEMBL523291 | — | — | 1 | 6.24 |
| CHEMBL519847 | — | — | 1 | 6.19 |
| CHEMBL488740 | — | — | 1 | 6.16 |
| CHEMBL93 | ZILEUTON | 4.0 | 1 | 6.10 |
| CHEMBL483684 | — | — | 1 | 5.92 |
| CHEMBL504152 | — | — | 1 | 5.92 |
| CHEMBL520641 | — | — | 1 | 5.80 |
| CHEMBL486691 | — | — | 1 | 5.77 |
| CHEMBL508183 | — | — | 1 | 5.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL482849 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL529218 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL519337 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL520798 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL519150 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL490656 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL490461 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL484482 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL484277 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL523292 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL520317 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL483056 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL485312 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL519508 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL483677 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL521164 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL520474 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL490460 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL483878 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL485243 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL483884 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL523291 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL519847 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL488740 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL93 | ZILEUTON | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL483684 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL504152 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL520641 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL486691 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL508183 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL487916 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL483067 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL484083 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL483689 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL487915 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL483269 | — | IC50 | = | 6900.0 | nM | 5.16 |
| CHEMBL488741 | — | IC50 | = | 7300.0 | nM | 5.14 |
| CHEMBL519029 | — | IC50 | = | 8100.0 | nM | 5.09 |
| CHEMBL505785 | — | IC50 | = | 8300.0 | nM | 5.08 |
| CHEMBL521133 | — | IC50 | = | 9800.0 | nM | 5.01 |
| CHEMBL450838 | — | IC50 | = | 10200.0 | nM | 4.99 |
| CHEMBL483066 | — | IC50 | = | 13400.0 | nM | 4.87 |
| CHEMBL483037 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL482645 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL484084 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL527421 | — | IC50 | > | 10000.0 | nM | - |