Assay Detail
Functional
CHEMBL3106437
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Cytotoxicity against chinese hamster R2 cells expressing human PCFT4 after 96 hrs by CellTitre-Blue fluorescence assay
13
Total Activities
13
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
Discovery of 5-substituted pyrrolo[2,3-d]pyrimidine antifolates as dual-acting inhibitors of glycinamide ribonucleotide formyltransferase and 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase in de novo purine nucleotide biosynthesis: implications of inhibiting 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase to ampk activation and antitumor activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 6.98 | 7.65 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL225072 | PEMETREXED | 4.0 | 1 | 7.65 |
| CHEMBL192632 | — | — | 1 | 7.64 |
| CHEMBL34412 | LOMETREXOL | 2.0 | 1 | 7.42 |
| CHEMBL225071 | RALTITREXED | 4.0 | 1 | 7.00 |
| CHEMBL34259 | METHOTREXATE | 4.0 | 1 | 6.92 |
| CHEMBL365307 | — | — | 1 | 6.67 |
| CHEMBL374172 | — | — | 1 | 6.48 |
| CHEMBL3104645 | — | — | 1 | 6.08 |
| CHEMBL502528 | — | — | 1 | - |
| CHEMBL526928 | — | — | 1 | - |
| CHEMBL2426247 | — | — | 1 | - |
| CHEMBL2426246 | — | — | 1 | - |
| CHEMBL3105240 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL225072 | PEMETREXED | IC50 | = | 22.3 | nM | 7.65 |
| CHEMBL192632 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL34412 | LOMETREXOL | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL225071 | RALTITREXED | IC50 | = | 99.5 | nM | 7.00 |
| CHEMBL34259 | METHOTREXATE | IC50 | = | 120.5 | nM | 6.92 |
| CHEMBL365307 | — | IC50 | = | 213.0 | nM | 6.67 |
| CHEMBL374172 | — | IC50 | = | 329.0 | nM | 6.48 |
| CHEMBL3104645 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL502528 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL526928 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2426247 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2426246 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL3105240 | — | IC50 | > | 1000.0 | nM | - |