Assay Detail
Binding
CHEMBL1677364
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Inhibition of Staphylococcus aureus wild type recombinant DHFR by MTS assay
17
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 | 13 | 8.14 | 8.66 |
| Ki | 4 | 8.61 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1235617 | — | — | 3 | 9.05 |
| CHEMBL134561 | ICLAPRIM | 3.0 | 2 | 8.66 |
| CHEMBL1673303 | (S)-ICLAPRIM | — | 1 | 8.62 |
| CHEMBL560502 | — | — | 3 | 8.55 |
| CHEMBL1236788 | (R)-ICLAPRIM | — | 1 | 8.54 |
| CHEMBL1673173 | — | — | 3 | 8.46 |
| CHEMBL22 | TRIMETHOPRIM | 4.0 | 2 | 8.36 |
| CHEMBL577790 | — | — | 1 | 7.21 |
| CHEMBL459177 | — | — | 1 | 7.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1235617 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL134561 | ICLAPRIM | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL1673303 | (S)-ICLAPRIM | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL134561 | ICLAPRIM | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL560502 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL1235617 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL1236788 | (R)-ICLAPRIM | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL1673173 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL1673173 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL22 | TRIMETHOPRIM | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL560502 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL560502 | — | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL1673173 | — | IC50 | = | 11.5 | nM | 7.94 |
| CHEMBL1235617 | — | IC50 | = | 12.5 | nM | 7.90 |
| CHEMBL22 | TRIMETHOPRIM | IC50 | = | 14.4 | nM | 7.84 |
| CHEMBL577790 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL459177 | — | IC50 | = | 61.0 | nM | 7.21 |