Assay Detail
Binding
CHEMBL5252014
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of tau 4R1N phosphorylation (unknown origin) at S396 residue transfected in human U2OS cells coexpressing GFP-tagged beta catenin incubated overnight by high content imaging assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | U2OS |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Microtubule-associated protein tau (CHEMBL1293224) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design, Structure-Activity Relationships, and In Vivo Evaluation of Potent and Brain-Penetrant Imidazo[1,2-<i>b</i>]pyridazines as Glycogen Synthase Kinase-3β (GSK-3β) Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 7.17 | 8.04 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5266553 | — | — | 1 | 8.04 |
| CHEMBL5270555 | — | — | 1 | 7.52 |
| CHEMBL5282319 | — | — | 1 | 7.44 |
| CHEMBL5285422 | — | — | 1 | 7.39 |
| CHEMBL5270781 | — | — | 1 | 7.24 |
| CHEMBL5273327 | — | — | 1 | 7.24 |
| CHEMBL5274596 | — | — | 1 | 7.22 |
| CHEMBL5290040 | — | — | 1 | 7.08 |
| CHEMBL5316226 | — | — | 1 | 7.07 |
| CHEMBL5282376 | — | — | 1 | 6.92 |
| CHEMBL5286737 | — | — | 1 | 6.89 |
| CHEMBL5286669 | — | — | 1 | 6.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5266553 | — | IC50 | = | 9.2 | nM | 8.04 |
| CHEMBL5270555 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL5282319 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL5285422 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL5270781 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL5273327 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL5274596 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL5290040 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL5316226 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL5282376 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL5286737 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL5286669 | — | IC50 | = | 910.0 | nM | 6.04 |