Assay Detail
Functional
CHEMBL1838959
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiproliferative activity against chinese hamster R2 cells expressing human PCFT assessed as inhibition of colony formation after 10 to 14 days
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Cricetulus griseus |
| Cell Type | R2 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Synthesis, biological, and antitumor activity of a highly potent 6-substituted pyrrolo[2,3-d]pyrimidine thienoyl antifolate inhibitor with proton-coupled folate transporter and folate receptor selectivity over the reduced folate carrier that inhibits β-glycinamide ribonucleotide formyltransferase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 8.07 | 8.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1834488 | — | — | 1 | 8.85 |
| CHEMBL225072 | PEMETREXED | 4.0 | 1 | 8.31 |
| CHEMBL590740 | — | — | 1 | 7.57 |
| CHEMBL34412 | LOMETREXOL | 2.0 | 1 | 7.53 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1834488 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL225072 | PEMETREXED | IC50 | = | 4.94 | nM | 8.31 |
| CHEMBL590740 | — | IC50 | = | 27.2 | nM | 7.57 |
| CHEMBL34412 | LOMETREXOL | IC50 | = | 29.7 | nM | 7.53 |