Assay Detail
Functional
CHEMBL3106435
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Cytotoxicity against human KB cells expressing human RFC/FRalpha/PCFT after 96 hrs by CellTitre-Blue fluorescence assay
6
Total Activities
6
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
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 | 6 | 7.74 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL225072 | PEMETREXED | 4.0 | 1 | 8.00 |
| CHEMBL3104645 | — | — | 1 | 7.90 |
| CHEMBL2426246 | — | — | 1 | 7.76 |
| CHEMBL374172 | — | — | 1 | 7.30 |
| CHEMBL3105240 | — | — | 1 | - |
| CHEMBL2426247 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL225072 | PEMETREXED | IC50 | = | 9.94 | nM | 8.00 |
| CHEMBL3104645 | — | IC50 | = | 12.7 | nM | 7.90 |
| CHEMBL2426246 | — | IC50 | = | 17.3 | nM | 7.76 |
| CHEMBL374172 | — | IC50 | = | 49.5 | nM | 7.30 |
| CHEMBL3105240 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2426247 | — | IC50 | > | 1000.0 | nM | - |