Assay Detail
Binding
CHEMBL2161359
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of GARFTase in human IGROV1 cells assessed as reduction in [14C]glycine incorporation into [14C]formyl GAR incubated for 15 hrs in complete folate free RPMI medium in presence of 2 nM leucovorin
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | IGROV-1 |
| 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 biological activity of 6-substituted pyrrolo[2,3-d]pyrimidine thienoyl regioisomers as inhibitors of de novo purine biosynthesis with selectivity for cellular uptake by high affinity folate receptors and the proton-coupled folate transporter over the reduced folate carrier.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 8.54 | 8.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2158681 | — | — | 1 | 8.75 |
| CHEMBL2158682 | — | — | 1 | 8.69 |
| CHEMBL590740 | — | — | 1 | 8.46 |
| CHEMBL34412 | LOMETREXOL | 2.0 | 1 | 8.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2158681 | — | IC50 | = | 1.79 | nM | 8.75 |
| CHEMBL2158682 | — | IC50 | = | 2.03 | nM | 8.69 |
| CHEMBL590740 | — | IC50 | = | 3.46 | nM | 8.46 |
| CHEMBL34412 | LOMETREXOL | IC50 | = | 5.77 | nM | 8.24 |