Assay Detail
Binding
CHEMBL766776
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Displacement of [H-20]phorbol12,13-dibutyrate (PDBU) from Protein kinase C alpha
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. 10. Ultrapotent protein kinase C ligands based on a racemic 5-disubstituted tetrahydro-2-furanone template.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 6.56 | 7.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL94718 | — | — | 1 | 7.62 |
| CHEMBL97661 | — | — | 1 | 7.55 |
| CHEMBL420450 | — | — | 1 | 7.46 |
| CHEMBL49904 | — | — | 1 | 7.11 |
| CHEMBL94492 | — | — | 1 | 7.02 |
| CHEMBL299225 | — | — | 1 | 6.86 |
| CHEMBL94857 | — | — | 1 | 5.19 |
| CHEMBL94549 | — | — | 1 | 5.19 |
| CHEMBL96773 | — | — | 1 | 5.01 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL94718 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL97661 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL420450 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL49904 | — | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL94492 | — | Ki | = | 96.0 | nM | 7.02 |
| CHEMBL299225 | — | Ki | = | 138.0 | nM | 6.86 |
| CHEMBL94857 | — | Ki | = | 6510.0 | nM | 5.19 |
| CHEMBL94549 | — | Ki | = | 6500.0 | nM | 5.19 |
| CHEMBL96773 | — | Ki | = | 9810.0 | nM | 5.01 |