Assay Detail
Binding
CHEMBL2156016
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PKCtheta 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 | 8.22 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2151411 | — | — | 1 | 10.00 |
| CHEMBL1996510 | — | — | 1 | 9.30 |
| CHEMBL2153750 | — | — | 1 | 9.22 |
| CHEMBL565612 | SOTRASTAURIN | 2.0 | 1 | 9.00 |
| CHEMBL2151415 | — | — | 1 | 8.92 |
| CHEMBL2153751 | — | — | 1 | 8.92 |
| CHEMBL2153748 | — | — | 1 | 8.68 |
| CHEMBL2153749 | — | — | 1 | 8.54 |
| CHEMBL2151413 | — | — | 1 | 8.42 |
| CHEMBL568580 | — | — | 1 | 8.32 |
| CHEMBL2153752 | — | — | 1 | 8.29 |
| CHEMBL2151412 | — | — | 1 | 8.24 |
| CHEMBL2151410 | — | — | 1 | 8.15 |
| CHEMBL2153755 | — | — | 1 | 8.11 |
| CHEMBL2151408 | — | — | 1 | 8.08 |
| CHEMBL2151409 | — | — | 1 | 8.01 |
| CHEMBL2151414 | — | — | 1 | 7.58 |
| CHEMBL2153747 | — | — | 1 | 7.51 |
| CHEMBL2151406 | — | — | 1 | 7.17 |
| CHEMBL2153753 | — | — | 1 | 7.15 |
| CHEMBL2151407 | — | — | 1 | 6.66 |
| CHEMBL2153756 | — | — | 1 | 6.50 |
| CHEMBL2153754 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2151411 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL1996510 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL2153750 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL565612 | SOTRASTAURIN | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL2151415 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL2153751 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL2153748 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL2153749 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL2151413 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL568580 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL2153752 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL2151412 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL2151410 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL2153755 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL2151408 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL2151409 | — | IC50 | = | 9.8 | nM | 8.01 |
| CHEMBL2151414 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL2153747 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL2151406 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL2153753 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL2151407 | — | IC50 | = | 221.0 | nM | 6.66 |
| CHEMBL2153756 | — | IC50 | = | 316.0 | nM | 6.50 |
| CHEMBL2153754 | — | IC50 | > | 316.0 | nM | - |