Assay Detail
Functional
CHEMBL914517
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Growth inhibition of methotrexate-transport-resistant human CCRF-CEM R2 cells after 120 hrs
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CCRF-CEM |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Synthesis of N-{4-[(2,4-diamino-5-methyl-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)thio]benzoyl}-L-glutamic acid and N-{4-[(2-amino-4-oxo-5-methyl-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)thio]benzoyl}-L-glutamic acid as dual inhibitors of dihydrofolate reductase and thymidylate synthase and as potential antitumor agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 3 | 5.47 | 5.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL34259 | METHOTREXATE | 4.0 | 1 | 5.82 |
| CHEMBL389643 | — | — | 1 | 5.11 |
| CHEMBL224974 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL34259 | METHOTREXATE | EC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL389643 | — | EC50 | = | 7750.0 | nM | 5.11 |
| CHEMBL224974 | — | EC50 | > | 20000.0 | nM | - |