Assay Detail
Binding
CHEMBL769174
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Inhibition of protein kinase C (PKC) in rat brain
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
Inhibitors of protein kinase C. 2. Substituted bisindolylmaleimides with improved potency and selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.24 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6291 | BISINDOLYLMALEIMIDE IX | — | 1 | 8.00 |
| CHEMBL267386 | — | — | 1 | 7.72 |
| CHEMBL6279 | — | — | 1 | 7.58 |
| CHEMBL268888 | — | — | 1 | 7.55 |
| CHEMBL6332 | — | — | 1 | 7.51 |
| CHEMBL429244 | — | — | 1 | 7.46 |
| CHEMBL267126 | — | — | 1 | 7.39 |
| CHEMBL268769 | — | — | 1 | 7.35 |
| CHEMBL6274 | — | — | 1 | 7.33 |
| CHEMBL266483 | — | — | 1 | 7.26 |
| CHEMBL268529 | — | — | 1 | 7.19 |
| CHEMBL269264 | — | — | 1 | 7.12 |
| CHEMBL6235 | — | — | 1 | 7.12 |
| CHEMBL6331 | — | — | 1 | 7.03 |
| CHEMBL6205 | — | — | 1 | 6.89 |
| CHEMBL441172 | — | — | 1 | 6.77 |
| CHEMBL6199 | — | — | 1 | 6.55 |
| CHEMBL268292 | — | — | 1 | 6.47 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6291 | BISINDOLYLMALEIMIDE IX | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL267386 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL6279 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL268888 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL6332 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL429244 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL267126 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL268769 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL6274 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL266483 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL268529 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL269264 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL6235 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL6331 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL6205 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL441172 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL6199 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL268292 | — | IC50 | = | 340.0 | nM | 6.47 |