Assay Detail
Binding
CHEMBL3382016
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PCFT (unknown origin) expressed in Chinese hamster R2/PCFT4 cells assessed as reduction in PCFT-mediated [3H]MTX transport at pH 5.5 and 37 degC incubated for 5 mins
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | R2/PCFT4 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Proton-coupled folate transporter (CHEMBL1795188) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Structure-activity profiles of novel 6-substituted pyrrolo[2,3-d]pyrimidine thienoyl antifolates with modified amino acids for cellular uptake by folate receptors α and β and the proton-coupled folate transporter.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 3 | 5.94 | 6.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1834488 | — | — | 1 | 6.48 |
| CHEMBL3335605 | — | — | 1 | 5.80 |
| CHEMBL3335607 | — | — | 1 | 5.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1834488 | — | Ki | = | 330.0 | nM | 6.48 |
| CHEMBL3335605 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL3335607 | — | Ki | = | 2900.0 | nM | 5.54 |