Assay Detail
Binding
CHEMBL4815322
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Inhibition of Escherichia coli DNA gyrase assessed as reduction in relaxation of supercoiled pNO1 DNA measured after 30 mins by fluorescence assay
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Escherichia coli |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
New dual ATP-competitive inhibitors of bacterial DNA gyrase and topoisomerase IV active against ESKAPE pathogens.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 7.32 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4863169 | — | — | 1 | 7.96 |
| CHEMBL4868407 | — | — | 1 | 7.96 |
| CHEMBL4857352 | — | — | 1 | 7.92 |
| CHEMBL4873935 | — | — | 1 | 7.89 |
| CHEMBL4866587 | — | — | 1 | 7.80 |
| CHEMBL4850124 | — | — | 1 | 7.72 |
| CHEMBL4857324 | — | — | 1 | 7.62 |
| CHEMBL4847572 | — | — | 1 | 7.34 |
| CHEMBL4877862 | — | — | 1 | 7.05 |
| CHEMBL36506 | NOVOBIOCIN | 4.0 | 1 | 6.77 |
| CHEMBL4847369 | — | — | 1 | 6.55 |
| CHEMBL4866508 | — | — | 1 | 6.50 |
| CHEMBL4856321 | — | — | 1 | 6.08 |
| CHEMBL4847090 | — | — | 1 | - |
| CHEMBL4850231 | — | — | 1 | - |
| CHEMBL4877458 | — | — | 1 | - |
| CHEMBL4854181 | — | — | 1 | - |
| CHEMBL4856813 | — | — | 1 | - |
| CHEMBL4850565 | — | — | 1 | - |
| CHEMBL4868482 | — | — | 1 | - |
| CHEMBL4878712 | — | — | 1 | - |
| CHEMBL4873249 | — | — | 1 | - |
| CHEMBL4871682 | — | — | 1 | - |
| CHEMBL4858015 | — | — | 1 | - |
| CHEMBL4876030 | — | — | 1 | - |
| CHEMBL4870243 | — | — | 1 | - |
| CHEMBL4866300 | — | — | 1 | - |
| CHEMBL4852505 | — | — | 1 | - |
| CHEMBL4851285 | — | — | 1 | - |
| CHEMBL4867874 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4863169 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4868407 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4857352 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4873935 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4866587 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4850124 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4857324 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4847572 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL4877862 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL36506 | NOVOBIOCIN | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4847369 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL4866508 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL4856321 | — | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL4874918 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL4857022 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL4862321 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL4863907 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4847190 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL4847090 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL4850231 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL4877458 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL4854181 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL4856813 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4850565 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL4868482 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL4878712 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL4873249 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL4871682 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL4858015 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL4876030 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL4870243 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL4866300 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4852505 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL4851285 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL4867874 | — | IC50 | < | 10.0 | nM | - |