Assay Detail
Functional
CHEMBL3089002
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Growth inhibition of Chinese hamster R2 cells expressing human PCFT4 after 96 hrs by CellTiter-blue assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Cricetulus griseus |
| Cell Type | R2 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Tumor-targeting with novel non-benzoyl 6-substituted straight chain pyrrolo[2,3-d]pyrimidine antifolates via cellular uptake by folate receptor α and inhibition of de novo purine nucleotide biosynthesis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 7.25 | 7.88 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL225072 | PEMETREXED | 4.0 | 1 | 7.88 |
| CHEMBL192632 | — | — | 1 | 7.64 |
| CHEMBL34412 | LOMETREXOL | 2.0 | 1 | 7.42 |
| CHEMBL1201746 | PRALATREXATE | 4.0 | 1 | 7.24 |
| CHEMBL225071 | RALTITREXED | 4.0 | 1 | 7.00 |
| CHEMBL34259 | METHOTREXATE | 4.0 | 1 | 6.92 |
| CHEMBL365307 | — | — | 1 | 6.67 |
| CHEMBL502528 | — | — | 1 | - |
| CHEMBL3086867 | — | — | 1 | - |
| CHEMBL3086866 | — | — | 1 | - |
| CHEMBL3086865 | — | — | 1 | - |
| CHEMBL3086864 | — | — | 1 | - |
| CHEMBL3086863 | — | — | 1 | - |
| CHEMBL3086673 | — | — | 1 | - |
| CHEMBL3086868 | — | — | 1 | - |
| CHEMBL526928 | — | — | 1 | - |
| CHEMBL3086869 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL225072 | PEMETREXED | IC50 | = | 13.2 | nM | 7.88 |
| CHEMBL192632 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL34412 | LOMETREXOL | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL1201746 | PRALATREXATE | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL225071 | RALTITREXED | IC50 | = | 99.5 | nM | 7.00 |
| CHEMBL34259 | METHOTREXATE | IC50 | = | 121.0 | nM | 6.92 |
| CHEMBL365307 | — | IC50 | = | 213.0 | nM | 6.67 |
| CHEMBL502528 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL3086867 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL3086866 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL3086865 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL3086864 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL3086863 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL3086673 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL3086868 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL526928 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL3086869 | — | IC50 | > | 1000.0 | nM | - |