Assay Detail
Binding
CHEMBL4194644
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]MTX uptake at human PCFT expressed in Chinese hamster R2/PCFT4 cells at pH 5.5 measured after 2 mins by Dixon plot analysis
3
Total Activities
3
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 |
|---|---|---|---|
| Ki | 3 | 6.47 | 6.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL225072 | PEMETREXED | 4.0 | 1 | 6.59 |
| CHEMBL4214638 | — | — | 1 | 6.48 |
| CHEMBL365307 | — | — | 1 | 6.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL225072 | PEMETREXED | Ki | = | 259.0 | nM | 6.59 |
| CHEMBL4214638 | — | Ki | = | 332.0 | nM | 6.48 |
| CHEMBL365307 | — | Ki | = | 460.0 | nM | 6.34 |