Assay Detail
Binding
CHEMBL759066
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Ability to displace bound [20-3H]-PDBU from a recombinant single isozyme (PKCalpha) in the presence of phosphatidylserine
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
An optimized protein kinase C activating diacylglycerol combining high binding affinity (Ki) with reduced lipophilicity (log P).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 7.11 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL27768 | — | — | 1 | 9.70 |
| CHEMBL170518 | PROSTRATIN | — | 1 | 8.32 |
| CHEMBL294422 | — | — | 1 | 7.61 |
| CHEMBL289230 | — | — | 1 | 7.54 |
| CHEMBL38644 | — | — | 1 | 7.51 |
| CHEMBL55267 | — | — | 1 | 7.48 |
| CHEMBL40482 | — | — | 1 | 7.40 |
| CHEMBL300160 | — | — | 1 | 7.35 |
| CHEMBL59422 | — | — | 1 | 7.30 |
| CHEMBL59376 | — | — | 1 | 7.17 |
| CHEMBL293717 | — | — | 1 | 7.15 |
| CHEMBL57015 | — | — | 1 | 7.14 |
| CHEMBL292417 | — | — | 1 | 7.13 |
| CHEMBL57517 | DIOLEIN | — | 1 | 7.06 |
| CHEMBL56997 | — | — | 1 | 6.96 |
| CHEMBL57400 | — | — | 1 | 6.81 |
| CHEMBL40602 | — | — | 1 | 6.48 |
| CHEMBL57211 | — | — | 1 | 5.98 |
| CHEMBL292383 | — | — | 1 | 5.85 |
| CHEMBL293709 | — | — | 1 | 5.75 |
| CHEMBL57105 | — | — | 1 | 5.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL27768 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL170518 | PROSTRATIN | Ki | = | 4.8 | nM | 8.32 |
| CHEMBL294422 | — | Ki | = | 24.6 | nM | 7.61 |
| CHEMBL289230 | — | Ki | = | 28.6 | nM | 7.54 |
| CHEMBL38644 | — | Ki | = | 31.1 | nM | 7.51 |
| CHEMBL55267 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL40482 | — | Ki | = | 39.9 | nM | 7.40 |
| CHEMBL300160 | — | Ki | = | 44.5 | nM | 7.35 |
| CHEMBL59422 | — | Ki | = | 50.4 | nM | 7.30 |
| CHEMBL59376 | — | Ki | = | 68.3 | nM | 7.17 |
| CHEMBL293717 | — | Ki | = | 71.0 | nM | 7.15 |
| CHEMBL57015 | — | Ki | = | 73.0 | nM | 7.14 |
| CHEMBL292417 | — | Ki | = | 74.9 | nM | 7.13 |
| CHEMBL57517 | DIOLEIN | Ki | = | 87.2 | nM | 7.06 |
| CHEMBL56997 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL57400 | — | Ki | = | 154.0 | nM | 6.81 |
| CHEMBL40602 | — | Ki | = | 330.0 | nM | 6.48 |
| CHEMBL57211 | — | Ki | = | 1050.0 | nM | 5.98 |
| CHEMBL292383 | — | Ki | = | 1409.0 | nM | 5.85 |
| CHEMBL293709 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL57105 | — | Ki | = | 2400.0 | nM | 5.62 |