Assay Detail
Binding
CHEMBL4309285
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 antiproliferative activity measured as reduction in cell growth after 96 hrs by Cell-Titer Blue assay
13
Total Activities
13
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
Fluorine-Substituted Pyrrolo[2,3- d]Pyrimidine Analogues with Tumor Targeting 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 | 13 | 8.92 | 9.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4445651 | — | — | 1 | 9.85 |
| CHEMBL1834488 | — | — | 1 | 9.51 |
| CHEMBL3628344 | — | — | 1 | 9.48 |
| CHEMBL4465095 | — | — | 1 | 9.44 |
| CHEMBL4540298 | — | — | 1 | 9.24 |
| CHEMBL4557278 | — | — | 1 | 9.16 |
| CHEMBL4538151 | — | — | 1 | 8.95 |
| CHEMBL4214638 | — | — | 1 | 8.89 |
| CHEMBL4441626 | — | — | 1 | 8.85 |
| CHEMBL2158681 | — | — | 1 | 8.60 |
| CHEMBL192632 | — | — | 1 | 8.39 |
| CHEMBL365307 | — | — | 1 | 8.20 |
| CHEMBL225072 | PEMETREXED | 4.0 | 1 | 7.38 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4445651 | — | IC50 | = | 0.14 | nM | 9.85 |
| CHEMBL1834488 | — | IC50 | = | 0.31 | nM | 9.51 |
| CHEMBL3628344 | — | IC50 | = | 0.33 | nM | 9.48 |
| CHEMBL4465095 | — | IC50 | = | 0.36 | nM | 9.44 |
| CHEMBL4540298 | — | IC50 | = | 0.58 | nM | 9.24 |
| CHEMBL4557278 | — | IC50 | = | 0.69 | nM | 9.16 |
| CHEMBL4538151 | — | IC50 | = | 1.12 | nM | 8.95 |
| CHEMBL4214638 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4441626 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL2158681 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL192632 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL365307 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL225072 | PEMETREXED | IC50 | = | 42.0 | nM | 7.38 |