Assay Detail
Binding
CHEMBL872399
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Inhibition of [3H]PDBu binding to recombinant protein kinase C alpha was determined at pH 7.4, 37 degree C for 5 min
7
Total Activities
7
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 (DAG). 25. Exploration of the sn-1 and sn-2 carbonyl functionality reveals the essential role of the sn-1 carbonyl at the lipid interface in the binding of DAG-lactones to protein kinase C.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 6.84 | 8.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL96766 | — | — | 1 | 8.54 |
| CHEMBL137386 | — | — | 1 | 8.49 |
| CHEMBL370130 | — | — | 1 | 7.62 |
| CHEMBL434938 | — | — | 1 | 6.95 |
| CHEMBL194257 | — | — | 1 | 6.21 |
| CHEMBL194357 | — | — | 1 | 5.23 |
| CHEMBL363418 | — | — | 1 | 4.84 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL96766 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL137386 | — | Ki | = | 3.25 | nM | 8.49 |
| CHEMBL370130 | — | Ki | = | 23.7 | nM | 7.62 |
| CHEMBL434938 | — | Ki | = | 113.0 | nM | 6.95 |
| CHEMBL194257 | — | Ki | = | 622.0 | nM | 6.21 |
| CHEMBL194357 | — | Ki | = | 5874.0 | nM | 5.23 |
| CHEMBL363418 | — | Ki | = | 14290.0 | nM | 4.84 |