Assay Detail
Functional
CHEMBL4194635
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Antiproliferative activity against human KB cells expressing human RFC/FR-alpha/PCFT assessed as reduction in cell viability measured after 96 hrs in presence of folic acid by Cell-Titer Blue assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | KB |
| Confidence | 1 — Organism |
| Curated By | Intermediate |
Publication
Tumor Targeting with Novel Pyridyl 6-Substituted Pyrrolo[2,3- d]Pyrimidine Antifolates via Cellular Uptake by Folate Receptor α and the Proton-Coupled Folate Transporter and Inhibition of De Novo Purine Nucleotide Biosynthesis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 7.40 | 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 |
| CHEMBL225072 | PEMETREXED | 4.0 | 1 | 6.49 |
| CHEMBL4214638 | — | — | 1 | 6.43 |
| CHEMBL365307 | — | — | 1 | - |
| CHEMBL4205344 | — | — | 1 | - |
| CHEMBL4209721 | — | — | 1 | - |
| CHEMBL4218109 | — | — | 1 | - |
| CHEMBL4213181 | — | — | 1 | - |
| CHEMBL4205885 | — | — | 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 |
| CHEMBL225072 | PEMETREXED | IC50 | = | 327.0 | nM | 6.49 |
| CHEMBL4214638 | — | IC50 | = | 368.0 | nM | 6.43 |
| CHEMBL365307 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4205344 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4209721 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4218109 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4213181 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4205885 | — | IC50 | > | 1000.0 | nM | - |