Assay Detail
Functional
CHEMBL2161984
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Growth inhibition of human KB cells endogenously expressing RFC/FRalpha/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 | 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 | 13 | 8.43 | 9.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2158681 | — | — | 1 | 9.77 |
| CHEMBL1834488 | — | — | 1 | 9.59 |
| CHEMBL2158682 | — | — | 1 | 9.57 |
| CHEMBL590740 | — | — | 1 | 9.26 |
| CHEMBL2158680 | — | — | 1 | 7.45 |
| CHEMBL2158678 | — | — | 1 | 6.77 |
| CHEMBL2158679 | — | — | 1 | 6.57 |
| CHEMBL2158677 | — | — | 1 | - |
| CHEMBL2158676 | — | — | 1 | - |
| CHEMBL2158675 | — | — | 1 | - |
| CHEMBL2158616 | — | — | 1 | - |
| CHEMBL2158684 | — | — | 1 | - |
| CHEMBL2158683 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2158681 | — | IC50 | = | 0.17 | nM | 9.77 |
| CHEMBL1834488 | — | IC50 | = | 0.26 | nM | 9.59 |
| CHEMBL2158682 | — | IC50 | = | 0.27 | nM | 9.57 |
| CHEMBL590740 | — | IC50 | = | 0.55 | nM | 9.26 |
| CHEMBL2158680 | — | IC50 | = | 35.3 | nM | 7.45 |
| CHEMBL2158678 | — | IC50 | = | 171.0 | nM | 6.77 |
| CHEMBL2158679 | — | IC50 | = | 267.0 | nM | 6.57 |
| 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 | - |