Assay Detail
Binding
CHEMBL4432143
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human FR-beta receptor expressed in Chinese hamster D4 cells assessed as antiproliferative activity measured as reduction in cell viability after 96 hrs by Cell-Titer Blue fluorescence analysis
6
Total Activities
6
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 6-Substituted Pyrrolo [2,3-d] Pyrimidine Antifolates with Heteroatom Bridge Substitutions 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 | 6 | 9.12 | 9.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4467936 | — | — | 1 | 9.47 |
| CHEMBL4553188 | — | — | 1 | 9.35 |
| CHEMBL4471269 | — | — | 1 | 9.28 |
| CHEMBL4437824 | — | — | 1 | 9.21 |
| CHEMBL4444011 | — | — | 1 | 8.80 |
| CHEMBL4447805 | — | — | 1 | 8.59 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4467936 | — | IC50 | = | 0.34 | nM | 9.47 |
| CHEMBL4553188 | — | IC50 | = | 0.45 | nM | 9.35 |
| CHEMBL4471269 | — | IC50 | = | 0.53 | nM | 9.28 |
| CHEMBL4437824 | — | IC50 | = | 0.62 | nM | 9.21 |
| CHEMBL4444011 | — | IC50 | = | 1.57 | nM | 8.80 |
| CHEMBL4447805 | — | IC50 | = | 2.59 | nM | 8.59 |