Assay Detail
Binding
CHEMBL5374243
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Inhibition of Cy5-labeled p22phox (149 to 162 residues) probe binding to His-tag cleaved human p47phox (151 to 386 residues) expressed in Escherichia coli BL21 (DE3) pLysS incubated for 10 to 15 mins in presence of 0.005% Tween20 and 2% DMSO by fluorescence polarization assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Targeting NOX2 with Bivalent Small-Molecule p47phox-p22phox Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 6.46 | 6.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5411448 | — | — | 1 | 6.66 |
| CHEMBL5419067 | — | — | 1 | 6.62 |
| CHEMBL5410142 | — | — | 1 | 6.62 |
| CHEMBL5427803 | — | — | 1 | 6.51 |
| CHEMBL5410678 | — | — | 1 | 6.38 |
| CHEMBL5437628 | — | — | 1 | 6.25 |
| CHEMBL5412642 | — | — | 1 | 6.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5411448 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL5419067 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL5410142 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL5427803 | — | Ki | = | 310.0 | nM | 6.51 |
| CHEMBL5410678 | — | Ki | = | 420.0 | nM | 6.38 |
| CHEMBL5437628 | — | Ki | = | 560.0 | nM | 6.25 |
| CHEMBL5412642 | — | Ki | = | 680.0 | nM | 6.17 |