Assay Detail
Binding
CHEMBL5520892
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant ENPP1 expressed in HEK293T cells using cGAMP as substrate at pH 7.5 measured after 3.5 hrs in presence of ATP by luminescence based AMP-glo assay
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293T |
| 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 | 26 | 8.55 | 10.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5566114 | — | — | 1 | 10.05 |
| CHEMBL5556000 | — | — | 1 | 9.80 |
| CHEMBL5560511 | — | — | 1 | 9.52 |
| CHEMBL5561670 | — | — | 1 | 9.32 |
| CHEMBL5566818 | — | — | 1 | 9.25 |
| CHEMBL5558246 | — | — | 1 | 9.18 |
| CHEMBL5558533 | — | — | 1 | 9.14 |
| CHEMBL5556506 | — | — | 1 | 9.10 |
| CHEMBL5567749 | — | — | 1 | 9.03 |
| CHEMBL5527873 | — | — | 1 | 8.85 |
| CHEMBL5556761 | — | — | 1 | 8.75 |
| CHEMBL5568520 | — | — | 1 | 8.67 |
| CHEMBL5563471 | — | — | 1 | 8.62 |
| CHEMBL5557235 | — | — | 1 | 8.39 |
| CHEMBL5568392 | — | — | 1 | 8.39 |
| CHEMBL5564529 | — | — | 1 | 8.21 |
| CHEMBL5567338 | — | — | 1 | 8.21 |
| CHEMBL5555461 | — | — | 1 | 8.07 |
| CHEMBL5562733 | — | — | 1 | 7.90 |
| CHEMBL1783609 | — | — | 1 | 7.78 |
| CHEMBL5542628 | — | — | 1 | 7.72 |
| CHEMBL5556763 | — | — | 1 | 7.47 |
| CHEMBL5565761 | — | — | 1 | 6.94 |
| CHEMBL5555308 | — | — | 1 | 6.80 |
| CHEMBL5560400 | — | — | 1 | - |
| CHEMBL5567993 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5566114 | — | IC50 | = | 0.09 | nM | 10.05 |
| CHEMBL5556000 | — | IC50 | = | 0.16 | nM | 9.80 |
| CHEMBL5560511 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL5561670 | — | IC50 | = | 0.48 | nM | 9.32 |
| CHEMBL5566818 | — | IC50 | = | 0.56 | nM | 9.25 |
| CHEMBL5558246 | — | IC50 | = | 0.66 | nM | 9.18 |
| CHEMBL5558533 | — | IC50 | = | 0.72 | nM | 9.14 |
| CHEMBL5556506 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL5567749 | — | IC50 | = | 0.94 | nM | 9.03 |
| CHEMBL5527873 | — | IC50 | = | 1.41 | nM | 8.85 |
| CHEMBL5556761 | — | IC50 | = | 1.77 | nM | 8.75 |
| CHEMBL5568520 | — | IC50 | = | 2.14 | nM | 8.67 |
| CHEMBL5563471 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL5557235 | — | IC50 | = | 4.03 | nM | 8.39 |
| CHEMBL5568392 | — | IC50 | = | 4.05 | nM | 8.39 |
| CHEMBL5564529 | — | IC50 | = | 6.19 | nM | 8.21 |
| CHEMBL5567338 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL5555461 | — | IC50 | = | 8.46 | nM | 8.07 |
| CHEMBL5562733 | — | IC50 | = | 12.6 | nM | 7.90 |
| CHEMBL1783609 | — | IC50 | = | 16.7 | nM | 7.78 |
| CHEMBL5542628 | — | IC50 | = | 18.94 | nM | 7.72 |
| CHEMBL5556763 | — | IC50 | = | 34.04 | nM | 7.47 |
| CHEMBL5565761 | — | IC50 | = | 114.7 | nM | 6.94 |
| CHEMBL5555308 | — | IC50 | = | 157.1 | nM | 6.80 |
| CHEMBL5560400 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5567993 | — | IC50 | > | 1000.0 | nM | - |