Assay Detail
Binding
CHEMBL1775520
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of Staphylococcus aureus DNA gyrase Ser84Leu mutant assessed as inhibition of supercoiling of pBR322 DNA after 60 min by gel electrophoresis assay
7
Total Activities
7
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
Exploration of the activity of 7-pyrrolidino-8-methoxyisothiazoloquinolones against methicillin-resistant Staphylococcus aureus (MRSA).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 5.13 | 5.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1774147 | — | — | 1 | 5.50 |
| CHEMBL1256993 | — | — | 1 | 5.38 |
| CHEMBL1774264 | — | — | 1 | 4.92 |
| CHEMBL1774153 | — | — | 1 | 4.73 |
| CHEMBL8 | CIPROFLOXACIN | 4.0 | 1 | - |
| CHEMBL32 | MOXIFLOXACIN | 4.0 | 1 | - |
| CHEMBL430 | GEMIFLOXACIN | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1774147 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL1256993 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL1774264 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL1774153 | — | IC50 | = | 18700.0 | nM | 4.73 |
| CHEMBL8 | CIPROFLOXACIN | IC50 | > | 200000.0 | nM | - |
| CHEMBL32 | MOXIFLOXACIN | IC50 | > | 200000.0 | nM | - |
| CHEMBL430 | GEMIFLOXACIN | IC50 | > | 200000.0 | nM | - |