Assay Detail
Binding
CHEMBL4667901
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Inhibition of human SPPL2a expressed in HEK293 cells cotransfected with Gal4 luciferase reporter plasmid and VP16-TNFalpha(1-76)-NTF incubated for 24 hrs by luciferase reporter gene assay based luminescence assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of Orally Active Hydroxyethylamine Based SPPL2a Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 6.76 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4762492 | — | — | 1 | 8.15 |
| CHEMBL4759048 | — | — | 1 | 8.05 |
| CHEMBL4753654 | — | — | 1 | 7.89 |
| CHEMBL4792187 | — | — | 1 | 7.82 |
| CHEMBL4759943 | — | — | 1 | 7.60 |
| CHEMBL4740837 | — | — | 1 | 7.06 |
| CHEMBL4762370 | — | — | 1 | 6.70 |
| CHEMBL4747630 | — | — | 1 | 6.46 |
| CHEMBL4789381 | — | — | 1 | 6.21 |
| CHEMBL4785324 | — | — | 1 | 6.08 |
| CHEMBL4743609 | — | — | 1 | 6.07 |
| CHEMBL4753079 | — | — | 1 | 6.05 |
| CHEMBL4798232 | — | — | 1 | 6.04 |
| CHEMBL4741014 | — | — | 1 | 5.82 |
| CHEMBL4762488 | — | — | 1 | 5.37 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4762492 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4759048 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4753654 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4792187 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4759943 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4740837 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL4762370 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4747630 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL4789381 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL4785324 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL4743609 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL4753079 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL4798232 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL4741014 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4762488 | — | IC50 | = | 4300.0 | nM | 5.37 |