Assay Detail
Binding
CHEMBL4309294
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human PCFT expressed in Chinese hamster R2/PCFT4 cells assessed as reduction in [3H]MTX uptake at pH 5.5 measured over 2 mins by Dixon plot analysis
12
Total Activities
12
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
Fluorine-Substituted Pyrrolo[2,3- d]Pyrimidine Analogues with Tumor Targeting 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 | 12 | 6.61 | 7.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4445651 | — | — | 1 | 7.16 |
| CHEMBL225072 | PEMETREXED | 4.0 | 1 | 6.92 |
| CHEMBL1834488 | — | — | 1 | 6.85 |
| CHEMBL4540298 | — | — | 1 | 6.77 |
| CHEMBL4214638 | — | — | 1 | 6.62 |
| CHEMBL4465095 | — | — | 1 | 6.60 |
| CHEMBL4538151 | — | — | 1 | 6.58 |
| CHEMBL3628344 | — | — | 1 | 6.55 |
| CHEMBL2158681 | — | — | 1 | 6.44 |
| CHEMBL365307 | — | — | 1 | 6.34 |
| CHEMBL4557278 | — | — | 1 | 6.34 |
| CHEMBL192632 | — | — | 1 | 6.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4445651 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL225072 | PEMETREXED | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL1834488 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL4540298 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL4214638 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL4465095 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL4538151 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL3628344 | — | Ki | = | 280.0 | nM | 6.55 |
| CHEMBL2158681 | — | Ki | = | 360.0 | nM | 6.44 |
| CHEMBL365307 | — | Ki | = | 460.0 | nM | 6.34 |
| CHEMBL4557278 | — | Ki | = | 460.0 | nM | 6.34 |
| CHEMBL192632 | — | Ki | = | 630.0 | nM | 6.20 |