Assay Detail
Functional
CHEMBL1067635
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Growth inhibition of human IGROV1 cells expressing RFC, FRalpha and PCFT after 96 hrs
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | IGROV-1 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Synthesis and antitumor activity of a novel series of 6-substituted pyrrolo[2,3-d]pyrimidine thienoyl antifolate inhibitors of purine biosynthesis with selectivity for high affinity folate receptors and the proton-coupled folate transporter over the reduced folate carrier for cellular entry.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 8.18 | 9.01 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL590740 | — | — | 1 | 9.01 |
| CHEMBL590985 | TALOTREXIN | 2.0 | 1 | 8.46 |
| CHEMBL365307 | — | — | 1 | 8.44 |
| CHEMBL491104 | — | — | 1 | 8.23 |
| CHEMBL605580 | — | — | 1 | 6.75 |
| CHEMBL601009 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL590740 | — | IC50 | = | 0.97 | nM | 9.01 |
| CHEMBL590985 | TALOTREXIN | IC50 | = | 3.47 | nM | 8.46 |
| CHEMBL365307 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL491104 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL605580 | — | IC50 | = | 176.0 | nM | 6.75 |
| CHEMBL601009 | — | IC50 | > | 1000.0 | nM | - |