Assay Detail
Binding
CHEMBL4309287
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to human PCFT expressed in Chinese hamster R2/PCFT4 cells assessed as antiproliferative activity measured as reduction in cell growth after 96 hrs by Cell-Titer Blue assay
13
Total Activities
13
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 |
|---|---|---|---|
| IC50 | 13 | 7.77 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4445651 | — | — | 1 | 8.82 |
| CHEMBL1834488 | — | — | 1 | 8.48 |
| CHEMBL4538151 | — | — | 1 | 8.42 |
| CHEMBL3628344 | — | — | 1 | 8.27 |
| CHEMBL4465095 | — | — | 1 | 8.22 |
| CHEMBL225072 | PEMETREXED | 4.0 | 1 | 8.08 |
| CHEMBL192632 | — | — | 1 | 7.64 |
| CHEMBL4540298 | — | — | 1 | 7.64 |
| CHEMBL4214638 | — | — | 1 | 7.52 |
| CHEMBL2158681 | — | — | 1 | 7.38 |
| CHEMBL4557278 | — | — | 1 | 7.17 |
| CHEMBL4441626 | — | — | 1 | 6.68 |
| CHEMBL365307 | — | — | 1 | 6.67 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4445651 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL1834488 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL4538151 | — | IC50 | = | 3.82 | nM | 8.42 |
| CHEMBL3628344 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL4465095 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL225072 | PEMETREXED | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL192632 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4540298 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4214638 | — | IC50 | = | 30.4 | nM | 7.52 |
| CHEMBL2158681 | — | IC50 | = | 41.5 | nM | 7.38 |
| CHEMBL4557278 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL4441626 | — | IC50 | = | 207.0 | nM | 6.68 |
| CHEMBL365307 | — | IC50 | = | 213.0 | nM | 6.67 |