Assay Detail
Binding
CHEMBL811641
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Affinity towards RFC (Reduced folate carrier) measured by the inhibition of [3H]MTX uptake
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Design and synthesis of Cyclopenta[g]quinazoline-based antifolates as inhibitors of thymidylate synthase and potential antitumor agents(,).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 4.66 | 5.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL55437 | — | — | 1 | 5.22 |
| CHEMBL59261 | — | — | 1 | 4.85 |
| CHEMBL57269 | — | — | 1 | 4.40 |
| CHEMBL299273 | — | — | 1 | 4.16 |
| CHEMBL293148 | — | — | 1 | - |
| CHEMBL301895 | — | — | 1 | - |
| CHEMBL61300 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL55437 | — | Ki | = | 6000.0 | nM | 5.22 |
| CHEMBL59261 | — | Ki | = | 14000.0 | nM | 4.85 |
| CHEMBL57269 | — | Ki | = | 40000.0 | nM | 4.40 |
| CHEMBL299273 | — | Ki | = | 69000.0 | nM | 4.16 |
| CHEMBL293148 | — | Ki | = | 150000.0 | nM | - |
| CHEMBL301895 | — | Ki | = | 200000.0 | nM | - |
| CHEMBL61300 | — | Ki | = | 106000.0 | nM | - |