Assay Detail
Binding
CHEMBL668081
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibitory concentration against recombinant human (rh) Dihydrofolate reductase
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Effect of C9-methyl substitution and C8-C9 conformational restriction on antifolate and antitumor activity of classical 5-substituted 2,4-diaminofuro[2,3-d]pyrimidines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 6.16 | 7.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL34259 | METHOTREXATE | 4.0 | 1 | 7.66 |
| CHEMBL104829 | FURO[2,3D]PYRIMIDINE ANTIFOLATE | — | 1 | 6.66 |
| CHEMBL430872 | — | — | 1 | 6.38 |
| CHEMBL106628 | — | — | 1 | 6.35 |
| CHEMBL323565 | — | — | 1 | 6.00 |
| CHEMBL1237205 | — | — | 1 | 5.66 |
| CHEMBL2092925 | — | — | 1 | 4.38 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL34259 | METHOTREXATE | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL104829 | FURO[2,3D]PYRIMIDINE ANTIFOLATE | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL430872 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL106628 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL323565 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL1237205 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL2092925 | — | IC50 | = | 42000.0 | nM | 4.38 |