Assay Detail
Functional
CHEMBL2161982
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Growth inhibition of Chinese hamster R2 cells expressing human PCFT incubated for 96 hrs by CellTiter-blue cell viability assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Cricetulus griseus |
| Cell Type | R2 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
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 | 13 | 7.61 | 8.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1834488 | — | — | 1 | 8.48 |
| CHEMBL2158681 | — | — | 1 | 7.38 |
| CHEMBL590740 | — | — | 1 | 7.36 |
| CHEMBL2158682 | — | — | 1 | 7.20 |
| CHEMBL2158678 | — | — | 1 | - |
| CHEMBL2158677 | — | — | 1 | - |
| CHEMBL2158676 | — | — | 1 | - |
| CHEMBL2158675 | — | — | 1 | - |
| CHEMBL2158616 | — | — | 1 | - |
| CHEMBL2158684 | — | — | 1 | - |
| CHEMBL2158683 | — | — | 1 | - |
| CHEMBL2158680 | — | — | 1 | - |
| CHEMBL2158679 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1834488 | — | IC50 | = | 3.34 | nM | 8.48 |
| CHEMBL2158681 | — | IC50 | = | 41.54 | nM | 7.38 |
| CHEMBL590740 | — | IC50 | = | 43.4 | nM | 7.36 |
| CHEMBL2158682 | — | IC50 | = | 63.82 | nM | 7.20 |
| CHEMBL2158678 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2158677 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2158676 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2158675 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2158616 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2158684 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2158683 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2158680 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2158679 | — | IC50 | > | 1000.0 | nM | - |