Assay Detail
Binding
CHEMBL684979
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Inhibition of Glycogen synthase kinase-3beta (GSK3-beta)
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Oryctolagus cuniculus |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Synthesis and discovery of macrocyclic polyoxygenated bis-7-azaindolylmaleimides as a novel series of potent and highly selective glycogen synthase kinase-3beta inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 7.04 | 7.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL340935 | INDOLYLYLMALEIMIDE 1 | — | 1 | 7.77 |
| CHEMBL336179 | — | — | 1 | 7.58 |
| CHEMBL340776 | — | — | 1 | 7.47 |
| CHEMBL337642 | — | — | 1 | 7.32 |
| CHEMBL130774 | — | — | 1 | 7.29 |
| CHEMBL131035 | — | — | 1 | 6.87 |
| CHEMBL334555 | — | — | 1 | 6.86 |
| CHEMBL340259 | INDOLYLYLMALEIMIDE 2 | — | 1 | 6.66 |
| CHEMBL131254 | — | — | 1 | 6.39 |
| CHEMBL132223 | — | — | 1 | 6.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL340935 | INDOLYLYLMALEIMIDE 1 | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL336179 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL340776 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL337642 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL130774 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL131035 | — | IC50 | = | 136.0 | nM | 6.87 |
| CHEMBL334555 | — | IC50 | = | 138.0 | nM | 6.86 |
| CHEMBL340259 | INDOLYLYLMALEIMIDE 2 | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL131254 | — | IC50 | = | 403.0 | nM | 6.39 |
| CHEMBL132223 | — | IC50 | = | 620.0 | nM | 6.21 |