Assay Detail
Functional
CHEMBL2156130
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Inhibition of human Jurkat cell activation assessed as TCR/CD28 stimulated inhibition of IL-2 secretion
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | Jurkat |
| Confidence | 1 — Organism |
| 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 | 4 | 7.33 | 7.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2153748 | — | — | 1 | 7.64 |
| CHEMBL568580 | — | — | 1 | 7.30 |
| CHEMBL565612 | SOTRASTAURIN | 2.0 | 1 | 7.27 |
| CHEMBL2153747 | — | — | 1 | 7.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2153748 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL568580 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL565612 | SOTRASTAURIN | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL2153747 | — | IC50 | = | 79.0 | nM | 7.10 |