Assay Detail
Binding
CHEMBL768985
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Displacement of [20-3H]phorbol-12,13-dibutyrate (PDBu) from a recombinant protein kinase C alpha with phosphatidylserine
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 | Expert |
Publication
Conformationally constrained analogues of diacylglycerol. 21. A solid-phase method of synthesis of diacylglycerol lactones as a prelude to a combinatorial approach for the synthesis of protein kinase C isozyme-specific ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 7.56 | 7.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL112543 | — | — | 1 | 7.85 |
| CHEMBL109354 | — | — | 1 | 7.72 |
| CHEMBL110256 | — | — | 1 | 7.69 |
| CHEMBL442009 | — | — | 1 | 7.64 |
| CHEMBL111711 | — | — | 1 | 7.59 |
| CHEMBL112401 | — | — | 1 | 7.55 |
| CHEMBL109997 | — | — | 1 | 7.36 |
| CHEMBL321665 | — | — | 1 | 7.36 |
| CHEMBL321189 | — | — | 1 | 7.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL112543 | — | Ki | = | 14.1 | nM | 7.85 |
| CHEMBL109354 | — | Ki | = | 19.1 | nM | 7.72 |
| CHEMBL110256 | — | Ki | = | 20.3 | nM | 7.69 |
| CHEMBL442009 | — | Ki | = | 22.7 | nM | 7.64 |
| CHEMBL111711 | — | Ki | = | 25.7 | nM | 7.59 |
| CHEMBL112401 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL109997 | — | Ki | = | 43.3 | nM | 7.36 |
| CHEMBL321665 | — | Ki | = | 43.8 | nM | 7.36 |
| CHEMBL321189 | — | Ki | = | 48.0 | nM | 7.32 |