Assay Detail
ADMET
CHEMBL4432140
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Cytotoxicity in RFC-null Chinese hamster R2 cells assessed as reduction in cell viability measured after 96 hrs by Cell-Titer Blue fluorescence analysis
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Cricetulus griseus |
| Cell Type | R2 |
| Confidence | 0 — Uncurated / Unknown |
| 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 | 10 | 7.22 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL34412 | LOMETREXOL | 2.0 | 1 | 7.92 |
| CHEMBL225071 | RALTITREXED | 4.0 | 1 | 7.82 |
| CHEMBL225072 | PEMETREXED | 4.0 | 1 | 7.38 |
| CHEMBL34259 | METHOTREXATE | 4.0 | 1 | 6.94 |
| CHEMBL4447805 | — | — | 1 | 6.03 |
| CHEMBL4437824 | — | — | 1 | - |
| CHEMBL4471269 | — | — | 1 | - |
| CHEMBL4444011 | — | — | 1 | - |
| CHEMBL4553188 | — | — | 1 | - |
| CHEMBL4467936 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL34412 | LOMETREXOL | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL225071 | RALTITREXED | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL225072 | PEMETREXED | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL34259 | METHOTREXATE | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL4447805 | — | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL4437824 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4471269 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4444011 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4553188 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4467936 | — | IC50 | > | 1000.0 | nM | - |