Assay Detail
Binding
CHEMBL5136430
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human SPPL2A expressed in human U2OS cells assessed as nuclear mask transferring to EGFP channel using EGFP-labeled TNFalpha (aa1-76) NTF as substrate and measured after 24 hrs by Hoechst staining based translocation assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | U2OS |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Diazepinone Compounds as Sppl2a Inhibitors for Treating Autoimmune Diseases and Lymphomas.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 9.17 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5204104 | — | — | 1 | 9.52 |
| CHEMBL5203663 | — | — | 1 | 9.30 |
| CHEMBL5182068 | — | — | 1 | 9.22 |
| CHEMBL5171841 | — | — | 1 | 9.00 |
| CHEMBL5197736 | — | — | 1 | 9.00 |
| CHEMBL5199989 | — | — | 1 | 9.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5204104 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL5203663 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL5182068 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL5171841 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5197736 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5199989 | — | IC50 | = | 1.0 | nM | 9.00 |