Assay Detail
Binding
CHEMBL4714600
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human PCFT expressed in Chinese Hamster MTXRII-OuaR2-4 R2 cells assessed as reduction in cell proliferation 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 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Proton-coupled folate transporter (CHEMBL1795188) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of 6-substituted thieno[2,3-d]pyrimidine analogs as dual inhibitors of glycinamide ribonucleotide formyltransferase and 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase in de novo purine nucleotide biosynthesis in folate receptor expressing human tumors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 6.80 | 7.09 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4761741 | — | — | 1 | 7.09 |
| CHEMBL4759798 | — | — | 1 | 6.97 |
| CHEMBL4755197 | — | — | 1 | 6.34 |
| CHEMBL4783397 | — | — | 1 | - |
| CHEMBL4790375 | — | — | 1 | - |
| CHEMBL4789686 | — | — | 1 | - |
| CHEMBL4741259 | — | — | 1 | - |
| CHEMBL491104 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4761741 | — | IC50 | = | 80.45 | nM | 7.09 |
| CHEMBL4759798 | — | IC50 | = | 107.29 | nM | 6.97 |
| CHEMBL4755197 | — | IC50 | = | 460.21 | nM | 6.34 |
| CHEMBL4783397 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4790375 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4789686 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4741259 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL491104 | — | IC50 | > | 1000.0 | nM | - |