Assay Detail
Binding
CHEMBL4624209
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of GARFTase in human KB cells expressing RFC/FRalpha/PCFT assessed as reduction in cell growth after 96 hrs in presence of folic acid by Cell-Titer Blue assay
9
Total Activities
9
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
Design, synthesis and biological evaluation of novel pyrrolo[2,3-d]pyrimidine as tumor-targeting agents with selectivity for tumor uptake by high affinity folate receptors over the reduced folate carrier.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 6.15 | 6.18 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4437824 | — | — | 1 | 6.18 |
| CHEMBL4643623 | — | — | 1 | 6.12 |
| CHEMBL192632 | — | — | 1 | - |
| CHEMBL365307 | — | — | 1 | - |
| CHEMBL4636872 | — | — | 1 | - |
| CHEMBL4645676 | — | — | 1 | - |
| CHEMBL4641908 | — | — | 1 | - |
| CHEMBL4638232 | — | — | 1 | - |
| CHEMBL4642637 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4437824 | — | IC50 | = | 666.0 | nM | 6.18 |
| CHEMBL4643623 | — | IC50 | = | 757.0 | nM | 6.12 |
| CHEMBL192632 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL365307 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4636872 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4645676 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4641908 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4638232 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4642637 | — | IC50 | > | 1000.0 | nM | - |