Assay Detail
Functional
CHEMBL830848
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of Glycogen synthase kinase-3 beta dependent Tau protein serine-396 phosphorylation in human SY5Y cells
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | SY5Y |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Substituted 3-imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino-[6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as highly selective and potent inhibitors of glycogen synthase kinase-3.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 8.28 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL362558 | LY-2090314 | 2.0 | 1 | 9.15 |
| CHEMBL362588 | — | — | 1 | 8.80 |
| CHEMBL178737 | — | — | 1 | 8.59 |
| CHEMBL362814 | — | — | 1 | 7.92 |
| CHEMBL363058 | — | — | 1 | 7.82 |
| CHEMBL186290 | — | — | 1 | 7.39 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL362558 | LY-2090314 | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL362588 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL178737 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL362814 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL363058 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL186290 | — | IC50 | = | 41.0 | nM | 7.39 |