Assay Detail
Binding
CHEMBL3788092
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Inhibition of human recombinant dihydrofolate reductase using dihydrofolate as substrate measured every 30 secs over 6 mins by UV/visible spectrophotometer in presence of NADPH
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
Applying the designed multiple ligands approach to inhibit dihydrofolate reductase and thioredoxin reductase for anti-proliferative activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 5.87 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL34259 | METHOTREXATE | 4.0 | 1 | 8.10 |
| CHEMBL1824770 | — | — | 1 | 6.37 |
| CHEMBL3787397 | — | — | 1 | 5.62 |
| CHEMBL532909 | — | — | 1 | 5.03 |
| CHEMBL3785981 | — | — | 1 | 4.25 |
| CHEMBL7976 | CHALCONE | — | 1 | - |
| CHEMBL3785320 | — | — | 1 | - |
| CHEMBL3787681 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL34259 | METHOTREXATE | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL1824770 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL3787397 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL532909 | — | IC50 | = | 9400.0 | nM | 5.03 |
| CHEMBL3785981 | — | IC50 | = | 56400.0 | nM | 4.25 |
| CHEMBL7976 | CHALCONE | IC50 | > | 100000.0 | nM | - |
| CHEMBL3785320 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3787681 | — | IC50 | > | 100000.0 | nM | - |