Assay Detail
Binding
CHEMBL3387469
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of RFC (unknown origin) expressed in Chinese hamster PC43-10 cells assessed as cell growth inhibition incubated up to 96 hrs by Celltiter-blue cell viability assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | PC43-10 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
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 |
|---|---|---|---|
| IC50 | 9 | 7.50 | 8.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL225071 | RALTITREXED | 4.0 | 1 | 8.20 |
| CHEMBL34259 | METHOTREXATE | 4.0 | 1 | 7.92 |
| CHEMBL1834488 | — | — | 1 | 7.00 |
| CHEMBL225072 | PEMETREXED | 4.0 | 1 | 6.86 |
| CHEMBL3335607 | — | — | 1 | - |
| CHEMBL3335606 | — | — | 1 | - |
| CHEMBL3335605 | — | — | 1 | - |
| CHEMBL3335604 | — | — | 1 | - |
| CHEMBL3335603 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL225071 | RALTITREXED | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL34259 | METHOTREXATE | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL1834488 | — | IC50 | = | 101.0 | nM | 7.00 |
| CHEMBL225072 | PEMETREXED | IC50 | = | 138.0 | nM | 6.86 |
| CHEMBL3335607 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL3335606 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL3335605 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL3335604 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL3335603 | — | IC50 | > | 1000.0 | nM | - |