Assay Detail
Binding
CHEMBL3632253
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to human FRalpha expressed in Chinese hamster RT16 cells assessed as cell growth inhibition after 96 hrs by CellTiter-Blue assay in presence of 200 nM folic acid
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | RT16 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
6-Substituted Pyrrolo[2,3-d]pyrimidine Thienoyl Regioisomers as Targeted Antifolates for Folate Receptor α and the Proton-Coupled Folate Transporter in Human Tumors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 6.46 | 6.76 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1834488 | — | — | 1 | 6.76 |
| CHEMBL3628344 | — | — | 1 | 6.31 |
| CHEMBL3628346 | — | — | 1 | 6.30 |
| CHEMBL3628345 | — | — | 1 | - |
| CHEMBL3628347 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1834488 | — | IC50 | = | 173.0 | nM | 6.76 |
| CHEMBL3628344 | — | IC50 | = | 494.0 | nM | 6.31 |
| CHEMBL3628346 | — | IC50 | = | 506.0 | nM | 6.30 |
| CHEMBL3628345 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL3628347 | — | IC50 | > | 1000.0 | nM | - |