Assay Detail
Binding
CHEMBL1040091
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Inhibition of PKCtheta by SPA
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Publication
Discovery of 3-(1H-indol-3-yl)-4-[2-(4-methylpiperazin-1-yl)quinazolin-4-yl]pyrrole-2,5-dione (AEB071), a potent and selective inhibitor of protein kinase C isotypes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 7.51 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL565612 | SOTRASTAURIN | 2.0 | 1 | 9.00 |
| CHEMBL565632 | — | — | 1 | 8.48 |
| CHEMBL568580 | — | — | 1 | 8.32 |
| CHEMBL7463 | GF-109203 | — | 1 | 8.17 |
| CHEMBL566853 | — | — | 1 | 7.28 |
| CHEMBL585500 | — | — | 1 | 7.12 |
| CHEMBL584483 | — | — | 1 | 6.78 |
| CHEMBL566424 | — | — | 1 | 6.59 |
| CHEMBL584817 | — | — | 1 | 5.86 |
| CHEMBL585281 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL565612 | SOTRASTAURIN | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL565632 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL568580 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL7463 | GF-109203 | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL566853 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL585500 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL584483 | — | IC50 | = | 165.0 | nM | 6.78 |
| CHEMBL566424 | — | IC50 | = | 255.0 | nM | 6.59 |
| CHEMBL584817 | — | IC50 | = | 1382.0 | nM | 5.86 |
| CHEMBL585281 | — | IC50 | > | 315.0 | nM | - |