Assay Detail
Binding
CHEMBL1681027
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Inhibition of trimethoprim-resistant Staphylococcus aureus DfrB type dihydrofolate reductase F98Y mutant
10
Total Activities
10
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
In vitro and in vivo properties of dihydrophthalazine antifolates, a novel family of antibacterial drugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 6.59 | 7.87 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1673173 | — | — | 1 | 7.87 |
| CHEMBL1650306 | — | — | 1 | 7.65 |
| CHEMBL1673175 | — | — | 1 | 7.39 |
| CHEMBL1673177 | — | — | 1 | 7.19 |
| CHEMBL1650307 | — | — | 1 | 7.15 |
| CHEMBL1650308 | — | — | 1 | 6.91 |
| CHEMBL1673174 | — | — | 1 | 5.94 |
| CHEMBL1673176 | — | — | 1 | 5.54 |
| CHEMBL1673178 | — | — | 1 | 5.24 |
| CHEMBL22 | TRIMETHOPRIM | 4.0 | 1 | 4.99 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1673173 | — | IC50 | = | 13.5 | nM | 7.87 |
| CHEMBL1650306 | — | IC50 | = | 22.6 | nM | 7.65 |
| CHEMBL1673175 | — | IC50 | = | 40.9 | nM | 7.39 |
| CHEMBL1673177 | — | IC50 | = | 64.4 | nM | 7.19 |
| CHEMBL1650307 | — | IC50 | = | 70.2 | nM | 7.15 |
| CHEMBL1650308 | — | IC50 | = | 124.4 | nM | 6.91 |
| CHEMBL1673174 | — | IC50 | = | 1146.0 | nM | 5.94 |
| CHEMBL1673176 | — | IC50 | = | 2917.0 | nM | 5.54 |
| CHEMBL1673178 | — | IC50 | = | 5705.0 | nM | 5.24 |
| CHEMBL22 | TRIMETHOPRIM | IC50 | = | 10243.0 | nM | 4.99 |