Assay Detail
Binding
CHEMBL3366023
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of 5-LOX in human PMNL cells assessed as reduction in 5-LOX product formation pre-incubated for 15 mins by HPLC based cell-free assay
15
Total Activities
15
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
Identification of pirinixic acid derivatives bearing a 2-aminothiazole moiety combines dual PPARα/γ activation and dual 5-LO/mPGES-1 inhibition.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 5.72 | 6.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3094412 | — | — | 1 | 6.52 |
| CHEMBL3094431 | — | — | 1 | 6.10 |
| CHEMBL3094426 | — | — | 1 | 5.80 |
| CHEMBL3094417 | — | — | 1 | 5.75 |
| CHEMBL3094410 | — | — | 1 | 5.72 |
| CHEMBL3094425 | — | — | 1 | 5.72 |
| CHEMBL3091498 | — | — | 1 | 5.70 |
| CHEMBL3094418 | — | — | 1 | 5.64 |
| CHEMBL3094415 | — | — | 1 | 5.64 |
| CHEMBL3094416 | — | — | 1 | 5.60 |
| CHEMBL3091499 | — | — | 1 | 5.52 |
| CHEMBL3094432 | — | — | 1 | 5.42 |
| CHEMBL3094433 | — | — | 1 | 5.18 |
| CHEMBL3318411 | — | — | 1 | - |
| CHEMBL3091496 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3094412 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL3094431 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL3094426 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL3094417 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL3094410 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL3094425 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL3091498 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL3094418 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL3094415 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL3094416 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL3091499 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL3094432 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL3094433 | — | IC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL3318411 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3091496 | — | IC50 | > | 10000.0 | nM | - |