Assay Detail
Binding
CHEMBL620875
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro inhibition of human 5-Lipoxygenase.
18
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Polyunsaturated fatty acid 5-lipoxygenase (CHEMBL215) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Thiopyrano[2,3,4-cd]indoles as 5-lipoxygenase inhibitors: synthesis, biological profile, and resolution of 2-[2-[1-(4-chlorobenzyl)-4-methyl-6-[(5-phenylpyridin-2-yl)methoxy]-4,5 -dihydro-1H-thiopyrano[2,3,4-cd]indol-2-yl]ethoxy]butanoic acid.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.12 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL275634 | — | — | 5 | 8.10 |
| CHEMBL13931 | — | — | 1 | 7.70 |
| CHEMBL16285 | — | — | 1 | 7.70 |
| CHEMBL277746 | — | — | 1 | 7.66 |
| CHEMBL278632 | — | — | 1 | 7.40 |
| CHEMBL278027 | — | — | 1 | 7.30 |
| CHEMBL279871 | — | — | 1 | 7.26 |
| CHEMBL16366 | — | — | 1 | 7.16 |
| CHEMBL16244 | — | — | 1 | 6.98 |
| CHEMBL16284 | — | — | 1 | 6.92 |
| CHEMBL278478 | — | — | 1 | 6.60 |
| CHEMBL16590 | — | — | 1 | 6.52 |
| CHEMBL16591 | — | — | 1 | 6.05 |
| CHEMBL16574 | — | — | 1 | 5.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL275634 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL275634 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL13931 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL16285 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL275634 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL277746 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL278632 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL278027 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL279871 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL16366 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL275634 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL16244 | — | IC50 | = | 105.0 | nM | 6.98 |
| CHEMBL16284 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL275634 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL278478 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL16590 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL16591 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL16574 | — | IC50 | = | 4000.0 | nM | 5.40 |