Assay Detail
Binding
CHEMBL3389960
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Inhibition of Escherichia coli DNA gyrase using fluorescence-tagged DNA by fluorescenct polarization assay
17
Total Activities
17
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
Novel DNA gyrase inhibiting spiropyrimidinetriones with a benzisoxazole scaffold: SAR and in vivo characterization.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 6.89 | 9.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3357980 | — | — | 1 | 9.54 |
| CHEMBL3357561 | — | — | 1 | 9.42 |
| CHEMBL3357982 | — | — | 1 | 7.89 |
| CHEMBL3357983 | — | — | 1 | 7.58 |
| CHEMBL3357991 | — | — | 1 | 6.68 |
| CHEMBL3357993 | — | — | 1 | 6.58 |
| CHEMBL8 | CIPROFLOXACIN | 4.0 | 1 | 6.57 |
| CHEMBL3357990 | — | — | 1 | 6.47 |
| CHEMBL3357988 | — | — | 1 | 6.47 |
| CHEMBL3357984 | — | — | 1 | 6.43 |
| CHEMBL3357986 | — | — | 1 | 6.32 |
| CHEMBL3357985 | — | — | 1 | 6.21 |
| CHEMBL3357992 | — | — | 1 | 6.01 |
| CHEMBL3357987 | — | — | 1 | 5.80 |
| CHEMBL3357989 | — | — | 1 | 5.40 |
| CHEMBL3357981 | — | — | 1 | - |
| CHEMBL126 | LINEZOLID | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3357980 | — | IC50 | = | 0.29 | nM | 9.54 |
| CHEMBL3357561 | — | IC50 | = | 0.38 | nM | 9.42 |
| CHEMBL3357982 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3357983 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3357991 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL3357993 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL8 | CIPROFLOXACIN | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL3357990 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL3357988 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL3357984 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL3357986 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL3357985 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL3357992 | — | IC50 | = | 970.0 | nM | 6.01 |
| CHEMBL3357987 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL3357989 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL3357981 | — | IC50 | > | 83.0 | nM | - |
| CHEMBL126 | LINEZOLID | IC50 | > | 32000.0 | nM | - |