Assay Detail
Functional
CHEMBL2161347
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of colony formation of human KB cells endogenously expressing RFC/FRalpha/PCFT incubated for 14 days by methylene blue staining based clonogenicty assay
4
Total Activities
4
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 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 | 9.25 | 9.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2158682 | — | — | 1 | 9.80 |
| CHEMBL590740 | — | — | 1 | 9.70 |
| CHEMBL2158681 | — | — | 1 | 9.41 |
| CHEMBL34259 | METHOTREXATE | 4.0 | 1 | 8.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2158682 | — | IC50 | = | 0.16 | nM | 9.80 |
| CHEMBL590740 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL2158681 | — | IC50 | = | 0.39 | nM | 9.41 |
| CHEMBL34259 | METHOTREXATE | IC50 | = | 8.5 | nM | 8.07 |