Assay Detail
Binding
CHEMBL864372
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Inhibitory activity against wild type Staphylococcus aureus topoisomerase 4
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Staphylococcus aureus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
DNA topoisomerase 4 subunit A (CHEMBL4088) ↗| Type | SINGLE PROTEIN |
| Organism | Staphylococcus aureus |
Publication
Isothiazoloquinolones containing functionalized aromatic hydrocarbons at the 7-position: synthesis and in vitro activity of a series of potent antibacterial agents with diminished cytotoxicity in human cells.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 5.56 | 6.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL380520 | — | — | 1 | 6.70 |
| CHEMBL430 | GEMIFLOXACIN | 4.0 | 1 | 6.52 |
| CHEMBL202864 | — | — | 1 | 6.30 |
| CHEMBL32 | MOXIFLOXACIN | 4.0 | 1 | 6.10 |
| CHEMBL8 | CIPROFLOXACIN | 4.0 | 1 | 6.00 |
| CHEMBL31 | GATIFLOXACIN | 4.0 | 1 | 5.92 |
| CHEMBL383497 | — | — | 1 | 5.82 |
| CHEMBL204271 | — | — | 1 | 5.80 |
| CHEMBL382817 | — | — | 1 | 5.58 |
| CHEMBL438444 | — | — | 1 | 5.57 |
| CHEMBL380696 | — | — | 1 | 5.14 |
| CHEMBL205011 | — | — | 1 | 5.09 |
| CHEMBL382560 | — | — | 1 | 5.00 |
| CHEMBL205729 | — | — | 1 | 5.00 |
| CHEMBL380505 | — | — | 1 | 4.92 |
| CHEMBL381395 | — | — | 1 | 4.60 |
| CHEMBL203002 | — | — | 1 | 4.39 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL380520 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL430 | GEMIFLOXACIN | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL202864 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL32 | MOXIFLOXACIN | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL8 | CIPROFLOXACIN | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL31 | GATIFLOXACIN | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL383497 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL204271 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL382817 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL438444 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL380696 | — | IC50 | = | 7200.0 | nM | 5.14 |
| CHEMBL205011 | — | IC50 | = | 8200.0 | nM | 5.09 |
| CHEMBL382560 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL205729 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL380505 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL381395 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL203002 | — | IC50 | = | 41000.0 | nM | 4.39 |