Assay Detail
Binding
CHEMBL4824378
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human full length GSK3beta expressed in baculovirus in Sf9 insect cells using YRRAAVPPSPSLSRHSSPHQ(pS)EDEEE as substrate by ADP-Glo kinase assay
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, synthesis and biological evaluation of harmine derivatives as potent GSK-3β/DYRK1A dual inhibitors for the treatment of Alzheimer's disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 6.03 | 7.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL388978 | STAUROSPORINE | — | 1 | 7.52 |
| CHEMBL322970 | — | — | 1 | 7.27 |
| CHEMBL4849247 | — | — | 1 | 7.15 |
| CHEMBL4846517 | — | — | 1 | 6.84 |
| CHEMBL4872945 | — | — | 1 | 6.70 |
| CHEMBL4873680 | — | — | 1 | 6.40 |
| CHEMBL4871399 | — | — | 1 | 5.32 |
| CHEMBL4854952 | — | — | 1 | 5.29 |
| CHEMBL4845857 | — | — | 1 | 5.18 |
| CHEMBL4878234 | — | — | 1 | 5.12 |
| CHEMBL4869592 | — | — | 1 | 5.09 |
| CHEMBL269538 | HARMINE | 1.0 | 1 | 4.49 |
| CHEMBL4859020 | — | — | 1 | - |
| CHEMBL4875836 | — | — | 1 | - |
| CHEMBL4854983 | — | — | 1 | - |
| CHEMBL4878139 | — | — | 1 | - |
| CHEMBL4848873 | — | — | 1 | - |
| CHEMBL4870826 | — | — | 1 | - |
| CHEMBL4863925 | — | — | 1 | - |
| CHEMBL4868963 | — | — | 1 | - |
| CHEMBL4875404 | — | — | 1 | - |
| CHEMBL4866620 | — | — | 1 | - |
| CHEMBL4861340 | — | — | 1 | - |
| CHEMBL4861480 | — | — | 1 | - |
| CHEMBL4860218 | — | — | 1 | - |
| CHEMBL4856645 | — | — | 1 | - |
| CHEMBL4873051 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL388978 | STAUROSPORINE | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL322970 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL4849247 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL4846517 | — | IC50 | = | 144.0 | nM | 6.84 |
| CHEMBL4872945 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4873680 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL4871399 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL4854952 | — | IC50 | = | 5150.0 | nM | 5.29 |
| CHEMBL4845857 | — | IC50 | = | 6590.0 | nM | 5.18 |
| CHEMBL4878234 | — | IC50 | = | 7620.0 | nM | 5.12 |
| CHEMBL4869592 | — | IC50 | = | 8100.0 | nM | 5.09 |
| CHEMBL269538 | HARMINE | IC50 | = | 32100.0 | nM | 4.49 |
| CHEMBL4859020 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4875836 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4854983 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4878139 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4848873 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4870826 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4863925 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4868963 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4875404 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4866620 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4861340 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4861480 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4860218 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4856645 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4873051 | — | IC50 | > | 10000.0 | nM | - |