Assay Detail
Binding
CHEMBL3391327
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Inhibition of full length human NOX2 transfected in COS 22 cells assessed as inhibition of Phorbol 12-myristate 13-acetate-stimulated ROS generation by measuring H2O2 production by fluorescence assay in presence of superoxide dismutase
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | COS 22 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Bridged tetrahydroisoquinolines as selective NADPH oxidase 2 (Nox2) inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 4.44 | 4.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3347543 | — | — | 1 | 4.92 |
| CHEMBL3347550 | — | — | 1 | 4.70 |
| CHEMBL3347492 | — | — | 1 | 4.60 |
| CHEMBL3347583 | — | — | 1 | 4.57 |
| CHEMBL3347503 | — | — | 1 | 4.52 |
| CHEMBL3347551 | — | — | 1 | 4.50 |
| CHEMBL3347542 | — | — | 1 | 4.40 |
| CHEMBL3347491 | — | — | 1 | 4.40 |
| CHEMBL3347549 | — | — | 1 | 4.29 |
| CHEMBL3347554 | — | — | 1 | 4.19 |
| CHEMBL3347502 | — | — | 1 | 4.11 |
| CHEMBL3347567 | — | — | 1 | 4.10 |
| CHEMBL3347555 | — | — | 1 | - |
| CHEMBL3347566 | — | — | 1 | - |
| CHEMBL3347525 | — | — | 1 | - |
| CHEMBL3347524 | — | — | 1 | - |
| CHEMBL3347501 | — | — | 1 | - |
| CHEMBL3347584 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3347543 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL3347550 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL3347492 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL3347583 | — | IC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL3347503 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL3347551 | — | IC50 | = | 32000.0 | nM | 4.50 |
| CHEMBL3347542 | — | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL3347491 | — | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL3347549 | — | IC50 | = | 51000.0 | nM | 4.29 |
| CHEMBL3347554 | — | IC50 | = | 64000.0 | nM | 4.19 |
| CHEMBL3347502 | — | IC50 | = | 78000.0 | nM | 4.11 |
| CHEMBL3347567 | — | IC50 | = | 79000.0 | nM | 4.10 |
| CHEMBL3347555 | — | IC50 | - | — | - | |
| CHEMBL3347566 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3347525 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3347524 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3347501 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3347584 | — | IC50 | > | 100000.0 | nM | - |