Assay Detail
Binding
CHEMBL4194647
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of GARFTase in human KB cells assessed as decrease in [14C]formyl GAR accumulation preincubated for 30 mins followed by [14C]glycine addition measured after 15 hrs in presence of azaserine by ion-exchange chromatographic assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Trifunctional purine biosynthetic protein adenosine-3 (CHEMBL3972) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Tumor Targeting with Novel Pyridyl 6-Substituted Pyrrolo[2,3- d]Pyrimidine Antifolates via Cellular Uptake by Folate Receptor α and the Proton-Coupled Folate Transporter and Inhibition of De Novo Purine Nucleotide Biosynthesis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 8.44 | 8.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4214638 | — | — | 1 | 8.74 |
| CHEMBL4205344 | — | — | 1 | 8.32 |
| CHEMBL365307 | — | — | 1 | 8.25 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4214638 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL4205344 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL365307 | — | IC50 | = | 5.6 | nM | 8.25 |