Assay Detail
Binding
CHEMBL4825465
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Inhibition of Staphylococcus aureus DNA gyrase assessed as reduction in DNA supercoiling using relaxed pNO1 plasmid DNA as substrate incubated for 30 mins by fluorimetric assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Staphylococcus aureus |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Structurally Optimized Potent Dual-Targeting NBTI Antibacterials with an Enhanced Bifurcated Halogen-Bonding Propensity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 7.71 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4879265 | — | — | 1 | 8.40 |
| CHEMBL4873479 | — | — | 1 | 8.40 |
| CHEMBL4862136 | — | — | 1 | 8.22 |
| CHEMBL4868908 | — | — | 1 | 8.15 |
| CHEMBL4866999 | — | — | 1 | 8.05 |
| CHEMBL4862951 | — | — | 1 | 8.05 |
| CHEMBL4864750 | — | — | 1 | 8.05 |
| CHEMBL4873185 | — | — | 1 | 7.85 |
| CHEMBL4879088 | — | — | 1 | 7.85 |
| CHEMBL4858549 | — | — | 1 | 7.58 |
| CHEMBL4861727 | — | — | 1 | 7.46 |
| CHEMBL4855172 | — | — | 1 | 6.91 |
| CHEMBL4874688 | — | — | 1 | 6.55 |
| CHEMBL3317856 | GEPOTIDACIN | 3.0 | 1 | 6.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4879265 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4873479 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4862136 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4868908 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4866999 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4862951 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4864750 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4873185 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4879088 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4858549 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4861727 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4855172 | — | IC50 | = | 123.0 | nM | 6.91 |
| CHEMBL4874688 | — | IC50 | = | 283.0 | nM | 6.55 |
| CHEMBL3317856 | GEPOTIDACIN | IC50 | = | 374.0 | nM | 6.43 |