Assay Detail
Functional
CHEMBL1003015
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Antiproliferative activity against human KB cells expressing human reduced folate carrier/folate receptor alpha after 96 hrs by celltiter-blue cell viability assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | KB |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Synthesis and biological activity of a novel series of 6-substituted thieno[2,3-d]pyrimidine antifolate inhibitors of purine biosynthesis with selectivity for high affinity folate receptors over the reduced folate carrier and proton-coupled folate transporter for cellular entry.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 7.34 | 8.31 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL491104 | — | — | 1 | 8.31 |
| CHEMBL490934 | — | — | 1 | 7.64 |
| CHEMBL491129 | — | — | 1 | 6.88 |
| CHEMBL491298 | — | — | 1 | 6.51 |
| CHEMBL522455 | — | — | 1 | - |
| CHEMBL522126 | — | — | 1 | - |
| CHEMBL491299 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL491104 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL490934 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL491129 | — | IC50 | = | 132.0 | nM | 6.88 |
| CHEMBL491298 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL522455 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL522126 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL491299 | — | IC50 | > | 1000.0 | nM | - |