Assay Detail
Binding
CHEMBL1821395
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Inhibition of TMP-resistant Staphylococcus aureus DHFR F99Y mutant assessed as oxidation of NADPH using dihydrofolate as substrate pre-incubated for 10 mins before substrate addition by spectrophotometry
4
Total Activities
4
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
Structure-based design of new DHFR-based antibacterial agents: 7-aryl-2,4-diaminoquinazolines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 4 | 8.24 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL134561 | ICLAPRIM | 3.0 | 1 | 9.05 |
| CHEMBL1818128 | — | — | 1 | 8.62 |
| CHEMBL1818129 | — | — | 1 | 8.22 |
| CHEMBL22 | TRIMETHOPRIM | 4.0 | 1 | 7.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL134561 | ICLAPRIM | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL1818128 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL1818129 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL22 | TRIMETHOPRIM | Ki | = | 90.0 | nM | 7.05 |