Assay Detail
Functional
CHEMBL3387477
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Cytotoxicity against human KB cells assessed as cell growth inhibition incubated up to 96 hrs by Celltiter-blue cell viability assay
9
Total Activities
9
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
Structure-activity profiles of novel 6-substituted pyrrolo[2,3-d]pyrimidine thienoyl antifolates with modified amino acids for cellular uptake by folate receptors α and β and the proton-coupled folate transporter.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 8.25 | 9.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1834488 | — | — | 1 | 9.59 |
| CHEMBL225071 | RALTITREXED | 4.0 | 1 | 8.23 |
| CHEMBL34259 | METHOTREXATE | 4.0 | 1 | 8.22 |
| CHEMBL3335605 | — | — | 1 | 8.05 |
| CHEMBL225072 | PEMETREXED | 4.0 | 1 | 7.17 |
| CHEMBL3335607 | — | — | 1 | - |
| CHEMBL3335606 | — | — | 1 | - |
| CHEMBL3335604 | — | — | 1 | - |
| CHEMBL3335603 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1834488 | — | IC50 | = | 0.26 | nM | 9.59 |
| CHEMBL225071 | RALTITREXED | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL34259 | METHOTREXATE | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3335605 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL225072 | PEMETREXED | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL3335607 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL3335606 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL3335604 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL3335603 | — | IC50 | > | 1000.0 | nM | - |