Assay Detail
Binding
CHEMBL3088992
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In situ inhibition of GRAFTase in human KB cells assessed as incorporation of [14C]-glycine into [14C]-formyl GAR preincubated for 30 mins followed by [14C]-glycine addition measured after 15 mins
3
Total Activities
3
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
Tumor-targeting with novel non-benzoyl 6-substituted straight chain pyrrolo[2,3-d]pyrimidine antifolates via cellular uptake by folate receptor α and inhibition of de novo purine nucleotide biosynthesis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 8.27 | 8.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3086865 | — | — | 1 | 8.54 |
| CHEMBL3086866 | — | — | 1 | 8.26 |
| CHEMBL3086867 | — | — | 1 | 8.02 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3086865 | — | IC50 | = | 2.89 | nM | 8.54 |
| CHEMBL3086866 | — | IC50 | = | 5.49 | nM | 8.26 |
| CHEMBL3086867 | — | IC50 | = | 9.62 | nM | 8.02 |