Assay Detail
Functional
CHEMBL3088999
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Growth inhibition of human KB cells expressing human RFC/FRalpha/PCFT after 96 hrs by CellTiter-blue assay in presence of folic acid
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | KB |
| 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 | 13 | 7.61 | 8.71 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1201746 | PRALATREXATE | 4.0 | 1 | 8.71 |
| CHEMBL34259 | METHOTREXATE | 4.0 | 1 | 7.70 |
| CHEMBL225071 | RALTITREXED | 4.0 | 1 | 7.66 |
| CHEMBL34412 | LOMETREXOL | 2.0 | 1 | 7.51 |
| CHEMBL225072 | PEMETREXED | 4.0 | 1 | 6.49 |
| CHEMBL3086867 | — | — | 1 | - |
| CHEMBL3086866 | — | — | 1 | - |
| CHEMBL3086865 | — | — | 1 | - |
| CHEMBL3086864 | — | — | 1 | - |
| CHEMBL3086863 | — | — | 1 | - |
| CHEMBL3086673 | — | — | 1 | - |
| CHEMBL3086868 | — | — | 1 | - |
| CHEMBL3086869 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1201746 | PRALATREXATE | IC50 | = | 1.94 | nM | 8.71 |
| CHEMBL34259 | METHOTREXATE | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL225071 | RALTITREXED | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL34412 | LOMETREXOL | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL225072 | PEMETREXED | IC50 | = | 327.0 | nM | 6.49 |
| 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 | - |
| CHEMBL3086869 | — | IC50 | > | 1000.0 | nM | - |