Assay Detail
Binding
CHEMBL3396875
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Displacement of [20-3H] phorbol 12, 13-dibutylate from recombinant PKCalpha (unknown origin) in presence of 100 ug/ml 100% phosphatidylserine
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 | 7.92 | 8.56 |
| Kd | 1 | 9.55 | 9.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL27768 | — | — | 1 | 9.55 |
| CHEMBL3393748 | — | — | 1 | 8.56 |
| CHEMBL3393741 | — | — | 1 | 8.36 |
| CHEMBL230048 | — | — | 1 | 8.32 |
| CHEMBL3393654 | — | — | 1 | 8.15 |
| CHEMBL3393753 | — | — | 1 | 8.14 |
| CHEMBL137386 | — | — | 1 | 8.08 |
| CHEMBL3393754 | — | — | 1 | 8.08 |
| CHEMBL3393752 | — | — | 1 | 8.08 |
| CHEMBL3393750 | — | — | 1 | 8.06 |
| CHEMBL3393751 | — | — | 1 | 8.01 |
| CHEMBL3393743 | — | — | 1 | 7.99 |
| CHEMBL3393749 | — | — | 1 | 7.90 |
| CHEMBL3393745 | — | — | 1 | 7.88 |
| CHEMBL3393742 | — | — | 1 | 7.81 |
| CHEMBL3393744 | — | — | 1 | 7.78 |
| CHEMBL3393758 | — | — | 1 | 7.61 |
| CHEMBL3393756 | — | — | 1 | 7.57 |
| CHEMBL3393747 | — | — | 1 | 7.51 |
| CHEMBL3393757 | — | — | 1 | 7.50 |
| CHEMBL3393755 | — | — | 1 | 7.48 |
| CHEMBL3393746 | — | — | 1 | 7.36 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL27768 | — | Kd | = | 0.28 | nM | 9.55 |
| CHEMBL3393748 | — | Ki | = | 2.78 | nM | 8.56 |
| CHEMBL3393741 | — | Ki | = | 4.33 | nM | 8.36 |
| CHEMBL230048 | — | Ki | = | 4.74 | nM | 8.32 |
| CHEMBL3393654 | — | Ki | = | 7.05 | nM | 8.15 |
| CHEMBL3393753 | — | Ki | = | 7.2 | nM | 8.14 |
| CHEMBL137386 | — | Ki | = | 8.3 | nM | 8.08 |
| CHEMBL3393754 | — | Ki | = | 8.26 | nM | 8.08 |
| CHEMBL3393752 | — | Ki | = | 8.31 | nM | 8.08 |
| CHEMBL3393750 | — | Ki | = | 8.7 | nM | 8.06 |
| CHEMBL3393751 | — | Ki | = | 9.8 | nM | 8.01 |
| CHEMBL3393743 | — | Ki | = | 10.2 | nM | 7.99 |
| CHEMBL3393749 | — | Ki | = | 12.6 | nM | 7.90 |
| CHEMBL3393745 | — | Ki | = | 13.2 | nM | 7.88 |
| CHEMBL3393742 | — | Ki | = | 15.4 | nM | 7.81 |
| CHEMBL3393744 | — | Ki | = | 16.5 | nM | 7.78 |
| CHEMBL3393758 | — | Ki | = | 24.5 | nM | 7.61 |
| CHEMBL3393756 | — | Ki | = | 26.7 | nM | 7.57 |
| CHEMBL3393747 | — | Ki | = | 30.8 | nM | 7.51 |
| CHEMBL3393757 | — | Ki | = | 31.6 | nM | 7.50 |
| CHEMBL3393755 | — | Ki | = | 33.1 | nM | 7.48 |
| CHEMBL3393746 | — | Ki | = | 43.9 | nM | 7.36 |