Assay Detail
Functional
CHEMBL4432147
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Antiproliferative activity against human KB cells expressing human RFC/FR-alpha/PCFT assessed as reduction in cell viability measured after 96 hrs in presence of folic acid by Cell-Titer Blue fluorescence analysis
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | KB |
| Confidence | 1 — Organism |
| 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 | 7 | 6.34 | 7.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1834488 | — | — | 1 | 7.00 |
| CHEMBL4437824 | — | — | 1 | 6.18 |
| CHEMBL4447805 | — | — | 1 | 6.15 |
| CHEMBL4553188 | — | — | 1 | 6.03 |
| CHEMBL4471269 | — | — | 1 | - |
| CHEMBL4444011 | — | — | 1 | - |
| CHEMBL4467936 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1834488 | — | IC50 | = | 101.0 | nM | 7.00 |
| CHEMBL4437824 | — | IC50 | = | 666.0 | nM | 6.18 |
| CHEMBL4447805 | — | IC50 | = | 704.0 | nM | 6.15 |
| CHEMBL4553188 | — | IC50 | = | 924.0 | nM | 6.03 |
| CHEMBL4471269 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4444011 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4467936 | — | IC50 | > | 1000.0 | nM | - |