Assay Detail
Functional
CHEMBL1931064
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human NOX4 expressed in CHO cell membrane coexpressing tetracylin repressor assessed as inhibition of ROS production after 20 mins by cell-free amplex red assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, synthesis and biological activity of original pyrazolo-pyrido-diazepine, -pyrazine and -oxazine dione derivatives as novel dual Nox4/Nox1 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 6.98 | 7.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1927157 | — | — | 1 | 7.17 |
| CHEMBL1927147 | — | — | 1 | 7.14 |
| CHEMBL1927149 | — | — | 1 | 7.12 |
| CHEMBL1927146 | — | — | 1 | 7.06 |
| CHEMBL1927158 | — | — | 1 | 7.03 |
| CHEMBL1927156 | — | — | 1 | 7.03 |
| CHEMBL1927150 | — | — | 1 | 7.00 |
| CHEMBL1927145 | — | — | 1 | 6.99 |
| CHEMBL1927151 | — | — | 1 | 6.99 |
| CHEMBL1927152 | — | — | 1 | 6.96 |
| CHEMBL1927155 | — | — | 1 | 6.96 |
| CHEMBL1927153 | — | — | 1 | 6.95 |
| CHEMBL1927154 | — | — | 1 | 6.94 |
| CHEMBL1927159 | — | — | 1 | 6.88 |
| CHEMBL1926690 | — | — | 1 | 6.85 |
| CHEMBL1927148 | — | — | 1 | 6.84 |
| CHEMBL1927160 | — | — | 1 | 6.81 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1927157 | — | Ki | = | 67.0 | nM | 7.17 |
| CHEMBL1927147 | — | Ki | = | 72.0 | nM | 7.14 |
| CHEMBL1927149 | — | Ki | = | 76.0 | nM | 7.12 |
| CHEMBL1927146 | — | Ki | = | 87.0 | nM | 7.06 |
| CHEMBL1927158 | — | Ki | = | 93.0 | nM | 7.03 |
| CHEMBL1927156 | — | Ki | = | 94.0 | nM | 7.03 |
| CHEMBL1927150 | — | Ki | = | 101.0 | nM | 7.00 |
| CHEMBL1927145 | — | Ki | = | 103.0 | nM | 6.99 |
| CHEMBL1927151 | — | Ki | = | 103.0 | nM | 6.99 |
| CHEMBL1927152 | — | Ki | = | 111.0 | nM | 6.96 |
| CHEMBL1927155 | — | Ki | = | 111.0 | nM | 6.96 |
| CHEMBL1927153 | — | Ki | = | 112.0 | nM | 6.95 |
| CHEMBL1927154 | — | Ki | = | 116.0 | nM | 6.94 |
| CHEMBL1927159 | — | Ki | = | 131.0 | nM | 6.88 |
| CHEMBL1926690 | — | Ki | = | 142.0 | nM | 6.85 |
| CHEMBL1927148 | — | Ki | = | 144.0 | nM | 6.84 |
| CHEMBL1927160 | — | Ki | = | 156.0 | nM | 6.81 |