Assay Detail
Binding
CHEMBL4432144
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 antiproliferative activity measured as reduction in cell viability after 96 hrs by Cell-Titer Blue fluorescence analysis
6
Total Activities
6
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 |
|---|---|---|---|
| IC50 | 6 | 7.00 | 7.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4447805 | — | — | 1 | 7.24 |
| CHEMBL4444011 | — | — | 1 | 7.09 |
| CHEMBL4437824 | — | — | 1 | 7.06 |
| CHEMBL4471269 | — | — | 1 | 7.05 |
| CHEMBL4553188 | — | — | 1 | 6.96 |
| CHEMBL4467936 | — | — | 1 | 6.57 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4447805 | — | IC50 | = | 57.5 | nM | 7.24 |
| CHEMBL4444011 | — | IC50 | = | 81.7 | nM | 7.09 |
| CHEMBL4437824 | — | IC50 | = | 87.4 | nM | 7.06 |
| CHEMBL4471269 | — | IC50 | = | 88.5 | nM | 7.05 |
| CHEMBL4553188 | — | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL4467936 | — | IC50 | = | 267.0 | nM | 6.57 |