Assay Detail
Binding
CHEMBL4714598
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human FRalpha expressed in Chinese Hamster MTXRII-OuaR2-4 R2 cells assessed as reduction in cell proliferation after 96 hrs by CellTiter-blue assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | R2 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of 6-substituted thieno[2,3-d]pyrimidine analogs as dual inhibitors of glycinamide ribonucleotide formyltransferase and 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase in de novo purine nucleotide biosynthesis in folate receptor expressing human tumors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 8.71 | 9.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4790375 | — | — | 1 | 9.47 |
| CHEMBL4759798 | — | — | 1 | 9.36 |
| CHEMBL4783397 | — | — | 1 | 9.04 |
| CHEMBL4761741 | — | — | 1 | 8.97 |
| CHEMBL4741259 | — | — | 1 | 8.59 |
| CHEMBL4755197 | — | — | 1 | 8.25 |
| CHEMBL491104 | — | — | 1 | 8.05 |
| CHEMBL4789686 | — | — | 1 | 7.98 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4790375 | — | IC50 | = | 0.34 | nM | 9.47 |
| CHEMBL4759798 | — | IC50 | = | 0.44 | nM | 9.36 |
| CHEMBL4783397 | — | IC50 | = | 0.91 | nM | 9.04 |
| CHEMBL4761741 | — | IC50 | = | 1.08 | nM | 8.97 |
| CHEMBL4741259 | — | IC50 | = | 2.55 | nM | 8.59 |
| CHEMBL4755197 | — | IC50 | = | 5.62 | nM | 8.25 |
| CHEMBL491104 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4789686 | — | IC50 | = | 10.5 | nM | 7.98 |