Assay Detail
Binding
CHEMBL4194632
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to human PCFT expressed in Chinese hamster R2/PCFT4 cells assessed as antiproliferative activity measured as reduction in cell viability after 96 hrs by Cell-Titer Blue assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Proton-coupled folate transporter (CHEMBL1795188) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 7.16 | 7.88 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL225072 | PEMETREXED | 4.0 | 1 | 7.88 |
| CHEMBL4214638 | — | — | 1 | 7.24 |
| 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 |
| CHEMBL4205344 | — | — | 1 | - |
| CHEMBL4209721 | — | — | 1 | - |
| CHEMBL4218109 | — | — | 1 | - |
| CHEMBL4213181 | — | — | 1 | - |
| CHEMBL4205885 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL225072 | PEMETREXED | IC50 | = | 13.2 | nM | 7.88 |
| CHEMBL4214638 | — | IC50 | = | 57.6 | nM | 7.24 |
| 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 |
| 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 | - |