Assay Detail
Binding
CHEMBL1677365
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Inhibition of Staphylococcus aureus DHFR F98Y mutant by MTS assay
16
Total Activities
9
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Staphylococcus aureus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Inhibition of antibiotic-resistant Staphylococcus aureus by the broad-spectrum dihydrofolate reductase inhibitor RAB1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 7.35 | 8.74 |
| Ki | 4 | 8.55 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1235617 | — | — | 3 | 9.70 |
| CHEMBL560502 | — | — | 3 | 9.05 |
| CHEMBL1673173 | — | — | 3 | 8.19 |
| CHEMBL1236788 | (R)-ICLAPRIM | — | 1 | 8.03 |
| CHEMBL134561 | ICLAPRIM | 3.0 | 1 | 7.57 |
| CHEMBL1673303 | (S)-ICLAPRIM | — | 1 | 7.44 |
| CHEMBL22 | TRIMETHOPRIM | 4.0 | 2 | 7.27 |
| CHEMBL577790 | — | — | 1 | 6.72 |
| CHEMBL459177 | — | — | 1 | 6.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1235617 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL560502 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL1235617 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL1673173 | — | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL560502 | — | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL1236788 | (R)-ICLAPRIM | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL1673173 | — | IC50 | = | 13.5 | nM | 7.87 |
| CHEMBL560502 | — | IC50 | = | 22.6 | nM | 7.65 |
| CHEMBL134561 | ICLAPRIM | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL1673303 | (S)-ICLAPRIM | IC50 | = | 36.3 | nM | 7.44 |
| CHEMBL22 | TRIMETHOPRIM | Ki | = | 53.6 | nM | 7.27 |
| CHEMBL1673173 | — | IC50 | = | 65.4 | nM | 7.18 |
| CHEMBL577790 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL459177 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL22 | TRIMETHOPRIM | IC50 | = | 539.7 | nM | 6.27 |
| CHEMBL1235617 | — | IC50 | = | 1146.0 | nM | 5.94 |