Assay Detail
Binding
CHEMBL4688567
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human N-terminal His6-tagged GSK3beta H350L mutant expressed in baculovirus infected Sf21 cells using prephosphorylated polypeptide as substrate incubated for 1 min followed by substrate addition and measured after 30 mins by Kinase-Glo luminescence assay
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf21 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of potent glycogen synthase kinase 3/cholinesterase inhibitors with neuroprotection as potential therapeutic agent for Alzheimer's disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 7.67 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4747992 | — | — | 1 | 8.52 |
| CHEMBL4792678 | — | — | 1 | 8.30 |
| CHEMBL4755445 | — | — | 1 | 8.30 |
| CHEMBL4752296 | — | — | 1 | 8.15 |
| CHEMBL4794823 | — | — | 1 | 8.10 |
| CHEMBL4776811 | — | — | 1 | 8.05 |
| CHEMBL4756451 | — | — | 1 | 8.00 |
| CHEMBL4787873 | — | — | 1 | 7.96 |
| CHEMBL4753139 | — | — | 1 | 7.85 |
| CHEMBL4748993 | — | — | 1 | 7.82 |
| CHEMBL4748792 | — | — | 1 | 7.80 |
| CHEMBL4796437 | — | — | 1 | 7.72 |
| CHEMBL102714 | SB-216763 | — | 1 | 7.70 |
| CHEMBL4795876 | — | — | 1 | 7.58 |
| CHEMBL4792741 | — | — | 1 | 7.58 |
| CHEMBL4742138 | — | — | 1 | 7.57 |
| CHEMBL4764558 | — | — | 1 | 7.42 |
| CHEMBL4746460 | — | — | 1 | 7.39 |
| CHEMBL4791089 | — | — | 1 | 7.35 |
| CHEMBL4785551 | — | — | 1 | 7.31 |
| CHEMBL4741669 | — | — | 1 | 7.21 |
| CHEMBL4753478 | — | — | 1 | 7.03 |
| CHEMBL4749550 | — | — | 1 | 6.71 |
| CHEMBL4759253 | — | — | 1 | 6.58 |
| CHEMBL502 | DONEPEZIL | 4.0 | 1 | - |
| CHEMBL95 | TACRINE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4747992 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4792678 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4755445 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4752296 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4794823 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4776811 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4756451 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4787873 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4753139 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4748993 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4748792 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4796437 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL102714 | SB-216763 | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4795876 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4792741 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4742138 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4764558 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL4746460 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL4791089 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL4785551 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL4741669 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL4753478 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL4749550 | — | IC50 | = | 193.0 | nM | 6.71 |
| CHEMBL4759253 | — | IC50 | = | 261.0 | nM | 6.58 |
| CHEMBL502 | DONEPEZIL | IC50 | > | 1000.0 | nM | - |
| CHEMBL95 | TACRINE | IC50 | > | 1000.0 | nM | - |