Assay Detail
Binding
CHEMBL2156012
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Inhibition of PKCbeta-1 by scintillation proximity assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Structure-activity relationship and pharmacokinetic studies of sotrastaurin (AEB071), a promising novel medicine for prevention of graft rejection and treatment of psoriasis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 8.24 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2151411 | — | — | 1 | 9.70 |
| CHEMBL1996510 | — | — | 1 | 9.22 |
| CHEMBL2153750 | — | — | 1 | 8.92 |
| CHEMBL2151415 | — | — | 1 | 8.85 |
| CHEMBL568580 | — | — | 1 | 8.74 |
| CHEMBL565612 | SOTRASTAURIN | 2.0 | 1 | 8.70 |
| CHEMBL2153748 | — | — | 1 | 8.70 |
| CHEMBL2153749 | — | — | 1 | 8.42 |
| CHEMBL2153755 | — | — | 1 | 8.30 |
| CHEMBL2151412 | — | — | 1 | 8.29 |
| CHEMBL2153747 | — | — | 1 | 8.28 |
| CHEMBL2151410 | — | — | 1 | 8.22 |
| CHEMBL2151408 | — | — | 1 | 8.19 |
| CHEMBL2151409 | — | — | 1 | 8.11 |
| CHEMBL2151413 | — | — | 1 | 8.11 |
| CHEMBL2151414 | — | — | 1 | 7.66 |
| CHEMBL2153751 | — | — | 1 | 7.64 |
| CHEMBL2151407 | — | — | 1 | 7.32 |
| CHEMBL2153752 | — | — | 1 | 6.85 |
| CHEMBL2153756 | — | — | 1 | 6.52 |
| CHEMBL2151406 | — | — | 1 | - |
| CHEMBL2153754 | — | — | 1 | - |
| CHEMBL2153753 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2151411 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL1996510 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL2153750 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL2151415 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL568580 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL565612 | SOTRASTAURIN | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL2153748 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL2153749 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL2153755 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL2151412 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL2153747 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL2151410 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL2151408 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL2151409 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL2151413 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL2151414 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL2153751 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL2151407 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL2153752 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL2153756 | — | IC50 | = | 304.0 | nM | 6.52 |
| CHEMBL2151406 | — | IC50 | > | 316.0 | nM | - |
| CHEMBL2153754 | — | IC50 | > | 316.0 | nM | - |
| CHEMBL2153753 | — | IC50 | > | 316.0 | nM | - |