Assay Detail
Binding
CHEMBL1780758
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]PDBu from human recombinant PKCalpha after 20 mins by liquid scintillation counting
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design and synthesis of protein kinase Cα activators based on 'out of pocket' interactions.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 6.85 | 8.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL279115 | PHORBOL MYRISTATE ACETATE | 2.0 | 1 | 8.19 |
| CHEMBL1778819 | — | — | 1 | 7.37 |
| CHEMBL1778822 | — | — | 1 | 6.22 |
| CHEMBL1778821 | — | — | 1 | 5.63 |
| CHEMBL1778820 | — | — | 1 | - |
| CHEMBL1778823 | — | — | 1 | - |
| CHEMBL1778824 | — | — | 1 | - |
| CHEMBL1778825 | — | — | 1 | - |
| CHEMBL1778826 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL279115 | PHORBOL MYRISTATE ACETATE | Ki | = | 6.4 | nM | 8.19 |
| CHEMBL1778819 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL1778822 | — | Ki | = | 600.0 | nM | 6.22 |
| CHEMBL1778821 | — | Ki | = | 2340.0 | nM | 5.63 |
| CHEMBL1778820 | — | Ki | > | 3000.0 | nM | - |
| CHEMBL1778823 | — | Ki | > | 20000.0 | nM | - |
| CHEMBL1778824 | — | Ki | > | 20000.0 | nM | - |
| CHEMBL1778825 | — | Ki | > | 20000.0 | nM | - |
| CHEMBL1778826 | — | Ki | > | 20000.0 | nM | - |