Assay Detail
Functional
CHEMBL833438
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Inhibitory concentration to inhibit Ser396 phosphorylation of tau, a natural substrate of GSK-3 in SY5Y cells
13
Total Activities
13
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
The development of potent and selective bisarylmaleimide GSK3 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 7.95 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL181031 | BISARYLMALEIMIDE 1 | — | 1 | 9.52 |
| CHEMBL362588 | — | — | 1 | 8.80 |
| CHEMBL178737 | — | — | 1 | 8.59 |
| CHEMBL368246 | — | — | 1 | 8.30 |
| CHEMBL181339 | — | — | 1 | 8.11 |
| CHEMBL178851 | — | — | 1 | 8.06 |
| CHEMBL361007 | — | — | 1 | 7.96 |
| CHEMBL362814 | — | — | 1 | 7.92 |
| CHEMBL179725 | — | — | 1 | 7.89 |
| CHEMBL181464 | — | — | 1 | 7.42 |
| CHEMBL369572 | — | — | 1 | 7.28 |
| CHEMBL361948 | — | — | 1 | 6.96 |
| CHEMBL369316 | — | — | 1 | 6.53 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL181031 | BISARYLMALEIMIDE 1 | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL362588 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL178737 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL368246 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL181339 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL178851 | — | IC50 | = | 8.7 | nM | 8.06 |
| CHEMBL361007 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL362814 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL179725 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL181464 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL369572 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL361948 | — | IC50 | = | 111.0 | nM | 6.96 |
| CHEMBL369316 | — | IC50 | = | 297.0 | nM | 6.53 |