Assay Detail
Binding
CHEMBL760366
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Displacement of [20-3H]-PDBU ligand from recombinant protein kinase C (baculovirus)
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Conformationally constrained analogues of diacylglycerol. 18. The incorporation of a hydroxamate moiety into diacylglycerol-lactones reduces lipophilicity and helps discriminate between sn-1 and sn-2 binding modes to protein kinase C (PK-C). Implications for isozyme specificity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 7.40 | 8.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL137288 | — | — | 1 | 8.57 |
| CHEMBL290876 | — | — | 1 | 8.54 |
| CHEMBL96766 | — | — | 1 | 8.54 |
| CHEMBL138171 | — | — | 1 | 8.35 |
| CHEMBL137386 | — | — | 1 | 8.35 |
| CHEMBL135779 | — | — | 1 | 8.32 |
| CHEMBL94505 | — | — | 1 | 8.27 |
| CHEMBL137597 | — | — | 1 | 8.16 |
| CHEMBL137701 | — | — | 1 | 8.08 |
| CHEMBL136760 | — | — | 1 | 7.95 |
| CHEMBL136786 | — | — | 1 | 6.37 |
| CHEMBL439979 | — | — | 1 | 5.90 |
| CHEMBL336926 | — | — | 1 | 5.36 |
| CHEMBL137484 | — | — | 1 | 5.32 |
| CHEMBL138279 | — | — | 1 | 4.98 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL137288 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL290876 | — | Ki | = | 2.89 | nM | 8.54 |
| CHEMBL96766 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL138171 | — | Ki | = | 4.46 | nM | 8.35 |
| CHEMBL137386 | — | Ki | = | 4.51 | nM | 8.35 |
| CHEMBL135779 | — | Ki | = | 4.81 | nM | 8.32 |
| CHEMBL94505 | — | Ki | = | 5.42 | nM | 8.27 |
| CHEMBL137597 | — | Ki | = | 6.87 | nM | 8.16 |
| CHEMBL137701 | — | Ki | = | 8.32 | nM | 8.08 |
| CHEMBL136760 | — | Ki | = | 11.25 | nM | 7.95 |
| CHEMBL136786 | — | Ki | = | 429.7 | nM | 6.37 |
| CHEMBL439979 | — | Ki | = | 1260.0 | nM | 5.90 |
| CHEMBL336926 | — | Ki | = | 4330.0 | nM | 5.36 |
| CHEMBL137484 | — | Ki | = | 4840.0 | nM | 5.32 |
| CHEMBL138279 | — | Ki | = | 10430.0 | nM | 4.98 |