Assay Detail
Binding
CHEMBL2061329
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Inhibition of Staphylococcus aureus DNA gyrase B expressed in Escherichia coli BL21(DE3) cells assessed ATP hydrolysis activity after 18 to 24 hrs by malachite green reagent assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Staphylococcus aureus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of a novel azaindole class of antibacterial agents targeting the ATPase domains of DNA gyrase and Topoisomerase IV.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 7.74 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2059380 | — | — | 1 | 8.70 |
| CHEMBL2059379 | — | — | 1 | 8.40 |
| CHEMBL2059196 | — | — | 1 | 8.30 |
| CHEMBL2059375 | — | — | 1 | 8.05 |
| CHEMBL2059376 | — | — | 1 | 7.96 |
| CHEMBL2059377 | — | — | 1 | 7.64 |
| CHEMBL2059373 | — | — | 1 | 7.41 |
| CHEMBL2059197 | — | — | 1 | 7.24 |
| CHEMBL2059374 | — | — | 1 | 6.88 |
| CHEMBL2059198 | — | — | 1 | 6.83 |
| CHEMBL2059378 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2059380 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL2059379 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2059196 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL2059375 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL2059376 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL2059377 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL2059373 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL2059197 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL2059374 | — | IC50 | = | 133.0 | nM | 6.88 |
| CHEMBL2059198 | — | IC50 | = | 147.0 | nM | 6.83 |
| CHEMBL2059378 | — | IC50 | < | 1.0 | nM | - |