Assay Detail
ADMET
CHEMBL4194628
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Cytotoxicity in RFC-null Chinese hamster R2 cells assessed as reduction in cell viability measured after 96 hrs by Cell-Titer Blue assay
11
Total Activities
11
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 Pyridyl 6-Substituted Pyrrolo[2,3- d]Pyrimidine Antifolates 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 | 11 | 6.73 | 7.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL225071 | RALTITREXED | 4.0 | 1 | 7.82 |
| CHEMBL34259 | METHOTREXATE | 4.0 | 1 | 6.94 |
| CHEMBL1201746 | PRALATREXATE | 4.0 | 1 | 6.09 |
| CHEMBL225072 | PEMETREXED | 4.0 | 1 | 6.07 |
| CHEMBL365307 | — | — | 1 | - |
| CHEMBL4205344 | — | — | 1 | - |
| CHEMBL4214638 | — | — | 1 | - |
| CHEMBL4209721 | — | — | 1 | - |
| CHEMBL4218109 | — | — | 1 | - |
| CHEMBL4213181 | — | — | 1 | - |
| CHEMBL4205885 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL225071 | RALTITREXED | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL34259 | METHOTREXATE | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL1201746 | PRALATREXATE | IC50 | = | 819.0 | nM | 6.09 |
| CHEMBL225072 | PEMETREXED | IC50 | = | 849.0 | nM | 6.07 |
| CHEMBL365307 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4205344 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4214638 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4209721 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4218109 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4213181 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4205885 | — | IC50 | > | 1000.0 | nM | - |