Assay Detail
Binding
CHEMBL4194629
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Binding affinity to human FR-alpha receptor expressed in Chinese hamster RT16 cells assessed as antiproliferative activity measured as reduction in cell viability after 96 hrs by Cell-Titer Blue assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Tumor Targeting with Novel Pyridyl 6-Substituted Pyrrolo[2,3- d]Pyrimidine Antifolates via Cellular Uptake by Folate Receptor α and the Proton-Coupled Folate Transporter and Inhibition of De Novo Purine Nucleotide Biosynthesis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 7.53 | 8.90 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4214638 | — | — | 1 | 8.90 |
| CHEMBL4213181 | — | — | 1 | 8.35 |
| CHEMBL365307 | — | — | 1 | 8.20 |
| CHEMBL4205344 | — | — | 1 | 7.82 |
| CHEMBL225071 | RALTITREXED | 4.0 | 1 | 7.82 |
| CHEMBL225072 | PEMETREXED | 4.0 | 1 | 7.38 |
| CHEMBL34259 | METHOTREXATE | 4.0 | 1 | 6.94 |
| CHEMBL1201746 | PRALATREXATE | 4.0 | 1 | 6.78 |
| CHEMBL4209721 | — | — | 1 | 6.73 |
| CHEMBL4218109 | — | — | 1 | 6.35 |
| CHEMBL4205885 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4214638 | — | IC50 | = | 1.27 | nM | 8.90 |
| CHEMBL4213181 | — | IC50 | = | 4.43 | nM | 8.35 |
| CHEMBL365307 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL4205344 | — | IC50 | = | 15.02 | nM | 7.82 |
| CHEMBL225071 | RALTITREXED | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL225072 | PEMETREXED | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL34259 | METHOTREXATE | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL1201746 | PRALATREXATE | IC50 | = | 168.0 | nM | 6.78 |
| CHEMBL4209721 | — | IC50 | = | 186.0 | nM | 6.73 |
| CHEMBL4218109 | — | IC50 | = | 449.0 | nM | 6.35 |
| CHEMBL4205885 | — | IC50 | > | 1000.0 | nM | - |