Assay Detail
Binding
CHEMBL3829095
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Inhibition of recombinant human DHFR assessed as reduction in NADPH oxidation using dihydrofolate as substrate preincubated for 5 mins followed by substrate addition
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Charged Nonclassical Antifolates with Activity Against Gram-Positive and Gram-Negative Pathogens.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 6.19 | 6.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3828291 | — | — | 1 | 6.80 |
| CHEMBL3827532 | — | — | 1 | 6.70 |
| CHEMBL3828485 | — | — | 1 | 6.63 |
| CHEMBL3828724 | — | — | 1 | 6.46 |
| CHEMBL3827326 | — | — | 1 | 6.42 |
| CHEMBL3828581 | — | — | 1 | 6.41 |
| CHEMBL3827760 | — | — | 1 | 6.35 |
| CHEMBL3827086 | — | — | 1 | 5.60 |
| CHEMBL22 | TRIMETHOPRIM | 4.0 | 1 | 4.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3828291 | — | Ki | = | 158.77 | nM | 6.80 |
| CHEMBL3827532 | — | Ki | = | 200.77 | nM | 6.70 |
| CHEMBL3828485 | — | Ki | = | 234.23 | nM | 6.63 |
| CHEMBL3828724 | — | Ki | = | 346.15 | nM | 6.46 |
| CHEMBL3827326 | — | Ki | = | 376.62 | nM | 6.42 |
| CHEMBL3828581 | — | Ki | = | 388.62 | nM | 6.41 |
| CHEMBL3827760 | — | Ki | = | 451.15 | nM | 6.35 |
| CHEMBL3827086 | — | Ki | = | 2494.9 | nM | 5.60 |
| CHEMBL22 | TRIMETHOPRIM | Ki | = | 45783.5 | nM | 4.34 |