Assay Detail
Binding
CHEMBL5113161
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Inhibition of 5-LOX in human PMNL assessed as reduction in all-trans isomers of LTB4 and 5-HETE formation preincubated for 15 mins followed by A23187 addition and measured after 10 mins by RP-HPLC analysis
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | PMNL |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Polyunsaturated fatty acid 5-lipoxygenase (CHEMBL215) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery and Optimization of Indoline-Based Compounds as Dual 5-LOX/sEH Inhibitors: <i>In Vitro</i> and <i>In Vivo</i> Anti-Inflammatory Characterization.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 5.74 | 6.23 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5170803 | — | — | 1 | 6.23 |
| CHEMBL5199450 | — | — | 1 | 6.02 |
| CHEMBL4473010 | — | — | 1 | 5.86 |
| CHEMBL5185907 | — | — | 1 | 5.70 |
| CHEMBL5193145 | — | — | 1 | 5.54 |
| CHEMBL5207672 | — | — | 1 | 5.53 |
| CHEMBL5202375 | — | — | 1 | 5.31 |
| CHEMBL5171972 | — | — | 1 | - |
| CHEMBL5173787 | — | — | 1 | - |
| CHEMBL5169630 | — | — | 1 | - |
| CHEMBL5185080 | — | — | 1 | - |
| CHEMBL5192930 | — | — | 1 | - |
| CHEMBL4534966 | — | — | 1 | - |
| CHEMBL5193098 | — | — | 1 | - |
| CHEMBL5184604 | — | — | 1 | - |
| CHEMBL5185283 | — | — | 1 | - |
| CHEMBL5184139 | — | — | 1 | - |
| CHEMBL4458075 | — | — | 1 | - |
| CHEMBL5174746 | — | — | 1 | - |
| CHEMBL4590950 | — | — | 1 | - |
| CHEMBL4449485 | — | — | 1 | - |
| CHEMBL5191521 | — | — | 1 | - |
| CHEMBL5197906 | — | — | 1 | - |
| CHEMBL5205807 | — | — | 1 | - |
| CHEMBL5204046 | — | — | 1 | - |
| CHEMBL5190558 | — | — | 1 | - |
| CHEMBL5197863 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5170803 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL5199450 | — | IC50 | = | 950.0 | nM | 6.02 |
| CHEMBL4473010 | — | IC50 | = | 1380.0 | nM | 5.86 |
| CHEMBL5185907 | — | IC50 | = | 1980.0 | nM | 5.70 |
| CHEMBL5193145 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL5207672 | — | IC50 | = | 2930.0 | nM | 5.53 |
| CHEMBL5202375 | — | IC50 | = | 4870.0 | nM | 5.31 |
| CHEMBL5171972 | — | IC50 | - | — | - | |
| CHEMBL5173787 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5169630 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5185080 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5192930 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4534966 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5193098 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5184604 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5185283 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5184139 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4458075 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5174746 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4590950 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4449485 | — | IC50 | - | — | - | |
| CHEMBL5191521 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5197906 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5205807 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5204046 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5190558 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5197863 | — | IC50 | > | 10000.0 | nM | - |