Assay Detail
Binding
CHEMBL4412002
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of GSK3beta (unknown origin) pre-incubated for 30 mins followed by ULight-GS (Ser641/pSer657) peptide substrate addition and measured after 1 hr by TR-FRET assay
4
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Polycyclic maleimide-based derivatives as first dual modulators of neuronal calcium channels and GSK-3β for Alzheimer's disease treatment.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Inhibition | 3 | - | - |
| IC50 | 1 | 7.94 | 7.94 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL102714 | SB-216763 | — | 1 | 7.94 |
| CHEMBL4590632 | — | — | 1 | - |
| CHEMBL4549511 | — | — | 1 | - |
| CHEMBL4449273 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL102714 | SB-216763 | IC50 | = | 11.4 | nM | 7.94 |
| CHEMBL4590632 | — | Inhibition | - | % | - | |
| CHEMBL4549511 | — | Inhibition | - | % | - | |
| CHEMBL4449273 | — | Inhibition | - | % | - |