Assay Detail
Binding
CHEMBL5520893
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of ENPP1 in human MDA-MB-231 cells using p-Nph-5'-TMP as substrate at pH 9.5 measured after 60 mins by spectrophotometry based analysis
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | MDA-MB-231 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Ectonucleotide pyrophosphatase/phosphodiesterase family member 1 (CHEMBL5925) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of Pyrido[2,3-<i>d</i>]pyrimidin-7-one Derivatives as Highly Potent and Efficacious Ectonucleotide Pyrophosphatase/Phosphodiesterase 1 (ENPP1) Inhibitors for Cancer Treatment.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 7.39 | 8.06 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5566114 | — | — | 1 | 8.06 |
| CHEMBL1783609 | — | — | 1 | 7.71 |
| CHEMBL5556000 | — | — | 1 | 7.51 |
| CHEMBL5560511 | — | — | 1 | 7.45 |
| CHEMBL5566818 | — | — | 1 | 7.38 |
| CHEMBL5556506 | — | — | 1 | 7.33 |
| CHEMBL5561670 | — | — | 1 | 7.23 |
| CHEMBL5558246 | — | — | 1 | 7.20 |
| CHEMBL5567749 | — | — | 1 | 7.12 |
| CHEMBL5558533 | — | — | 1 | 6.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5566114 | — | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL1783609 | — | IC50 | = | 19.3 | nM | 7.71 |
| CHEMBL5556000 | — | IC50 | = | 30.8 | nM | 7.51 |
| CHEMBL5560511 | — | IC50 | = | 35.6 | nM | 7.45 |
| CHEMBL5566818 | — | IC50 | = | 42.2 | nM | 7.38 |
| CHEMBL5556506 | — | IC50 | = | 47.3 | nM | 7.33 |
| CHEMBL5561670 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL5558246 | — | IC50 | = | 63.3 | nM | 7.20 |
| CHEMBL5567749 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL5558533 | — | IC50 | = | 120.1 | nM | 6.92 |