Assay Detail
Binding
CHEMBL4432157
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 5 mins by Dixon plot analysis
8
Total Activities
8
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 6-Substituted Pyrrolo [2,3-d] Pyrimidine Antifolates with Heteroatom Bridge Substitutions 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 | 8 | 6.23 | 7.03 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL225072 | PEMETREXED | 4.0 | 1 | 7.03 |
| CHEMBL192632 | — | — | 1 | 6.66 |
| CHEMBL4447805 | — | — | 1 | 6.19 |
| CHEMBL4471269 | — | — | 1 | 6.14 |
| CHEMBL4553188 | — | — | 1 | 6.10 |
| CHEMBL4437824 | — | — | 1 | 6.07 |
| CHEMBL4467936 | — | — | 1 | 5.83 |
| CHEMBL4444011 | — | — | 1 | 5.78 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL225072 | PEMETREXED | Ki | = | 94.0 | nM | 7.03 |
| CHEMBL192632 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL4447805 | — | Ki | = | 640.0 | nM | 6.19 |
| CHEMBL4471269 | — | Ki | = | 730.0 | nM | 6.14 |
| CHEMBL4553188 | — | Ki | = | 800.0 | nM | 6.10 |
| CHEMBL4437824 | — | Ki | = | 850.0 | nM | 6.07 |
| CHEMBL4467936 | — | Ki | = | 1480.0 | nM | 5.83 |
| CHEMBL4444011 | — | Ki | = | 1680.0 | nM | 5.78 |