Assay Detail
Binding
CHEMBL4309290
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Binding affinity to human FR2 expressed in human HeLa R1-11 cells assessed as antiproliferative activity measured as reduction in cell growth after 96 hrs by Cell-Titer Blue assay
12
Total Activities
12
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 | 12 | 7.86 | 8.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4465095 | — | — | 1 | 8.55 |
| CHEMBL4445651 | — | — | 1 | 8.51 |
| CHEMBL4538151 | — | — | 1 | 8.28 |
| CHEMBL4214638 | — | — | 1 | 8.18 |
| CHEMBL3628344 | — | — | 1 | 8.12 |
| CHEMBL4540298 | — | — | 1 | 8.11 |
| CHEMBL365307 | — | — | 1 | 7.94 |
| CHEMBL192632 | — | — | 1 | 7.91 |
| CHEMBL4557278 | — | — | 1 | 7.66 |
| CHEMBL1834488 | — | — | 1 | 7.52 |
| CHEMBL2158681 | — | — | 1 | 7.45 |
| CHEMBL225072 | PEMETREXED | 4.0 | 1 | 6.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4465095 | — | IC50 | = | 2.84 | nM | 8.55 |
| CHEMBL4445651 | — | IC50 | = | 3.11 | nM | 8.51 |
| CHEMBL4538151 | — | IC50 | = | 5.22 | nM | 8.28 |
| CHEMBL4214638 | — | IC50 | = | 6.54 | nM | 8.18 |
| CHEMBL3628344 | — | IC50 | = | 7.57 | nM | 8.12 |
| CHEMBL4540298 | — | IC50 | = | 7.78 | nM | 8.11 |
| CHEMBL365307 | — | IC50 | = | 11.6 | nM | 7.94 |
| CHEMBL192632 | — | IC50 | = | 12.2 | nM | 7.91 |
| CHEMBL4557278 | — | IC50 | = | 21.7 | nM | 7.66 |
| CHEMBL1834488 | — | IC50 | = | 30.2 | nM | 7.52 |
| CHEMBL2158681 | — | IC50 | = | 35.3 | nM | 7.45 |
| CHEMBL225072 | PEMETREXED | IC50 | = | 863.0 | nM | 6.06 |