Assay Detail
Binding
CHEMBL4054599
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Inhibition of human DHFR using dihydrofolate as substrate after 180 secs by spectrophotometric analysis
8
Total Activities
8
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
Host dihydrofolate reductase (DHFR)-directed cycloguanil analogues endowed with activity against influenza virus and respiratory syncytial virus.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 6.70 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2382332 | — | — | 1 | 7.96 |
| CHEMBL268088 | — | — | 1 | 7.16 |
| CHEMBL7130 | — | — | 1 | 7.00 |
| CHEMBL92583 | CHLORCYCLOGUANIL | — | 1 | 6.96 |
| CHEMBL6948 | — | — | 1 | 6.89 |
| CHEMBL747 | CYCLOGUANIL | 2.0 | 1 | 6.39 |
| CHEMBL36 | PYRIMETHAMINE | 4.0 | 1 | 6.33 |
| CHEMBL4105317 | — | — | 1 | 4.88 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2382332 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL268088 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL7130 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL92583 | CHLORCYCLOGUANIL | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL6948 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL747 | CYCLOGUANIL | Ki | = | 410.0 | nM | 6.39 |
| CHEMBL36 | PYRIMETHAMINE | Ki | = | 470.0 | nM | 6.33 |
| CHEMBL4105317 | — | Ki | = | 13170.0 | nM | 4.88 |