Assay Detail
Binding
CHEMBL1006408
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of GARFTase in human KB cells assessed as inhibition of [14C]glycine incorporation into [14C]formylGAR in presence of azaserine
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | KB |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Trifunctional purine biosynthetic protein adenosine-3 (CHEMBL3972) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and discovery of high affinity folate receptor-specific glycinamide ribonucleotide formyltransferase inhibitors with antitumor activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 7.92 | 8.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL365307 | — | — | 1 | 8.17 |
| CHEMBL502528 | — | — | 1 | 8.14 |
| CHEMBL526928 | — | — | 1 | 8.07 |
| CHEMBL34412 | LOMETREXOL | 2.0 | 1 | 7.85 |
| CHEMBL192632 | — | — | 1 | 7.75 |
| CHEMBL225072 | PEMETREXED | 4.0 | 1 | 7.52 |
| CHEMBL498800 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL365307 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL502528 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL526928 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL34412 | LOMETREXOL | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL192632 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL225072 | PEMETREXED | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL498800 | — | IC50 | > | 1000.0 | nM | - |