Assay Detail
Binding
CHEMBL3412692
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 cell growth inhibition after 96 hrs by CellTiter-Blue assay
8
Total Activities
8
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
Novel 5-substituted pyrrolo[2,3-d]pyrimidines as dual inhibitors of glycinamide ribonucleotide formyltransferase and 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase and as potential antitumor agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 7.16 | 7.88 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL225072 | PEMETREXED | 4.0 | 1 | 7.88 |
| CHEMBL590740 | — | — | 1 | 7.36 |
| CHEMBL3409336 | — | — | 1 | 7.24 |
| CHEMBL3407519 | — | — | 1 | 7.10 |
| CHEMBL3409335 | — | — | 1 | 6.85 |
| CHEMBL3409334 | — | — | 1 | 6.51 |
| CHEMBL2426245 | — | — | 1 | - |
| CHEMBL3409337 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL225072 | PEMETREXED | IC50 | = | 13.2 | nM | 7.88 |
| CHEMBL590740 | — | IC50 | = | 43.4 | nM | 7.36 |
| CHEMBL3409336 | — | IC50 | = | 57.4 | nM | 7.24 |
| CHEMBL3407519 | — | IC50 | = | 80.2 | nM | 7.10 |
| CHEMBL3409335 | — | IC50 | = | 141.0 | nM | 6.85 |
| CHEMBL3409334 | — | IC50 | = | 312.0 | nM | 6.51 |
| CHEMBL2426245 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL3409337 | — | IC50 | > | 1000.0 | nM | - |