Assay Detail
Binding
CHEMBL3632255
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Binding affinity to human FRbeta expressed in Chinese hamster D4 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 | D4 |
| 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 | 6.44 | 6.90 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1834488 | — | — | 1 | 6.90 |
| CHEMBL3628344 | — | — | 1 | 6.25 |
| CHEMBL3628346 | — | — | 1 | 6.18 |
| CHEMBL3628345 | — | — | 1 | - |
| CHEMBL3628347 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1834488 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL3628344 | — | IC50 | = | 557.0 | nM | 6.25 |
| CHEMBL3628346 | — | IC50 | = | 654.0 | nM | 6.18 |
| CHEMBL3628345 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL3628347 | — | IC50 | > | 1000.0 | nM | - |