Assay Detail
Binding
CHEMBL5134833
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Inhibition of NanoLuc-PKN2 (ser646-cys984)(unknown origin) expressed in HEK293 cells by cell-based NanoBRET target engagement assay
4
Total Activities
4
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
Development of dihydropyrrolopyridinone-based PKN2/PRK2 chemical tools to enable drug discovery.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 5.38 | 5.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL250870 | — | — | 1 | 5.68 |
| CHEMBL5182936 | — | — | 1 | 5.55 |
| CHEMBL225519 | — | — | 1 | 5.32 |
| CHEMBL250871 | — | — | 1 | 4.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL250870 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL5182936 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL225519 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL250871 | — | IC50 | = | 11000.0 | nM | 4.96 |