Assay Detail
Binding
CHEMBL4414745
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of 5-LO in human PMNL cells assessed as reduction in leukotriene formation preincubated for 5 mins followed by thapsigargin stimulation measured after 15 mins by RP-HPLC analysis
6
Total Activities
5
Compounds Tested
2
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
Discovery of a novel 2,5-dihydroxycinnamic acid-based 5-lipoxygenase inhibitor that induces apoptosis and may impair autophagic flux in RCC4 renal cancer cells.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 6.09 | 6.48 |
| Inhibition | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL131678 | — | — | 2 | 6.48 |
| CHEMBL4579523 | — | — | 1 | 6.28 |
| CHEMBL4582170 | — | — | 1 | 6.05 |
| CHEMBL319244 | CAFFEIC ACID PHENETHYL ESTER | — | 1 | 6.01 |
| CHEMBL93 | ZILEUTON | 4.0 | 1 | 5.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL131678 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL4579523 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL4582170 | — | IC50 | = | 890.0 | nM | 6.05 |
| CHEMBL319244 | CAFFEIC ACID PHENETHYL ESTER | IC50 | = | 970.0 | nM | 6.01 |
| CHEMBL93 | ZILEUTON | IC50 | = | 2310.0 | nM | 5.64 |
| CHEMBL131678 | — | Inhibition | - | % | - |