Assay Detail
Binding
CHEMBL3394956
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [20-3H] phorbol 12, 13-dibutylate from recombinant PKCalpha (unknown origin) in presence of nuclear membrane mimetic lipid mixture
22
Total Activities
22
Compounds Tested
2
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 C epsilon selective diacylglycerol lactones (DAG-lactones).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 7.27 | 7.81 |
| Kd | 1 | 8.84 | 8.84 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL27768 | — | — | 1 | 8.84 |
| CHEMBL3393748 | — | — | 1 | 7.81 |
| CHEMBL3393741 | — | — | 1 | 7.61 |
| CHEMBL3393754 | — | — | 1 | 7.59 |
| CHEMBL3393654 | — | — | 1 | 7.58 |
| CHEMBL3393753 | — | — | 1 | 7.51 |
| CHEMBL3393749 | — | — | 1 | 7.41 |
| CHEMBL3393750 | — | — | 1 | 7.36 |
| CHEMBL3393742 | — | — | 1 | 7.36 |
| CHEMBL3393751 | — | — | 1 | 7.35 |
| CHEMBL137386 | — | — | 1 | 7.34 |
| CHEMBL230048 | — | — | 1 | 7.24 |
| CHEMBL3393743 | — | — | 1 | 7.22 |
| CHEMBL3393752 | — | — | 1 | 7.22 |
| CHEMBL3393755 | — | — | 1 | 7.14 |
| CHEMBL3393757 | — | — | 1 | 7.08 |
| CHEMBL3393747 | — | — | 1 | 7.00 |
| CHEMBL3393744 | — | — | 1 | 6.99 |
| CHEMBL3393746 | — | — | 1 | 6.97 |
| CHEMBL3393756 | — | — | 1 | 6.96 |
| CHEMBL3393745 | — | — | 1 | 6.94 |
| CHEMBL3393758 | — | — | 1 | 6.93 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL27768 | — | Kd | = | 1.44 | nM | 8.84 |
| CHEMBL3393748 | — | Ki | = | 15.4 | nM | 7.81 |
| CHEMBL3393741 | — | Ki | = | 24.7 | nM | 7.61 |
| CHEMBL3393754 | — | Ki | = | 25.7 | nM | 7.59 |
| CHEMBL3393654 | — | Ki | = | 26.2 | nM | 7.58 |
| CHEMBL3393753 | — | Ki | = | 31.1 | nM | 7.51 |
| CHEMBL3393749 | — | Ki | = | 38.7 | nM | 7.41 |
| CHEMBL3393750 | — | Ki | = | 43.8 | nM | 7.36 |
| CHEMBL3393742 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL3393751 | — | Ki | = | 44.8 | nM | 7.35 |
| CHEMBL137386 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL230048 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL3393743 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL3393752 | — | Ki | = | 60.8 | nM | 7.22 |
| CHEMBL3393755 | — | Ki | = | 73.0 | nM | 7.14 |
| CHEMBL3393757 | — | Ki | = | 84.1 | nM | 7.08 |
| CHEMBL3393747 | — | Ki | = | 99.0 | nM | 7.00 |
| CHEMBL3393744 | — | Ki | = | 103.0 | nM | 6.99 |
| CHEMBL3393746 | — | Ki | = | 106.0 | nM | 6.97 |
| CHEMBL3393756 | — | Ki | = | 110.3 | nM | 6.96 |
| CHEMBL3393745 | — | Ki | = | 116.0 | nM | 6.94 |
| CHEMBL3393758 | — | Ki | = | 117.0 | nM | 6.93 |