Assay Detail
Binding
CHEMBL830137
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Displacement of [20-3H]-phorbol 12,13-dibutyrate (PDBU) from recombinant Protein kinase C alpha (C1a/C1b domain) in presence of phosphatidyl serine
15
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Macrocyclic diacylglycerol-bis-lactones as conformationally constrained analogues of diacylglycerol-lactones. Interactions with protein kinase C.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 7.36 | 8.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL96766 | — | — | 1 | 8.54 |
| CHEMBL362890 | — | — | 1 | 8.22 |
| CHEMBL185859 | — | — | 1 | 7.99 |
| CHEMBL187067 | — | — | 1 | 7.92 |
| CHEMBL359571 | — | — | 1 | 7.66 |
| CHEMBL184340 | — | — | 1 | 7.62 |
| CHEMBL186067 | — | — | 1 | 7.55 |
| CHEMBL2114288 | — | — | 2 | 7.46 |
| CHEMBL361050 | — | — | 1 | 7.28 |
| CHEMBL49904 | — | — | 1 | 7.11 |
| CHEMBL364849 | — | — | 1 | 6.97 |
| CHEMBL299225 | — | — | 1 | 6.86 |
| CHEMBL186395 | — | — | 1 | 6.00 |
| CHEMBL184615 | — | — | 1 | 5.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL96766 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL362890 | — | Ki | = | 6.07 | nM | 8.22 |
| CHEMBL185859 | — | Ki | = | 10.29 | nM | 7.99 |
| CHEMBL187067 | — | Ki | = | 12.16 | nM | 7.92 |
| CHEMBL359571 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL184340 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL186067 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL2114288 | — | Ki | = | 35.09 | nM | 7.46 |
| CHEMBL2114288 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL361050 | — | Ki | = | 52.7 | nM | 7.28 |
| CHEMBL49904 | — | Ki | = | 77.85 | nM | 7.11 |
| CHEMBL364849 | — | Ki | = | 107.2 | nM | 6.97 |
| CHEMBL299225 | — | Ki | = | 138.0 | nM | 6.86 |
| CHEMBL186395 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL184615 | — | Ki | = | 1800.0 | nM | 5.75 |