Assay Detail
Binding
CHEMBL4711086
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human N-terminal His6-tagged GSK-3beta H350L mutant expressed in baculovirus infected Sf21 cells using GSM as substrate incubated for 30 mins in presence of ATP by kinase-glo luminescence assay
31
Total Activities
31
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
Rational design and biological evaluation of a new class of thiazolopyridyl tetrahydroacridines as cholinesterase and GSK-3 dual inhibitors for Alzheimer's disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 7.30 | 8.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4747410 | — | — | 1 | 8.19 |
| CHEMBL4744911 | — | — | 1 | 7.84 |
| CHEMBL3410089 | — | — | 1 | 7.76 |
| CHEMBL102714 | SB-216763 | — | 1 | 7.70 |
| CHEMBL4779478 | — | — | 1 | 7.68 |
| CHEMBL4789145 | — | — | 1 | 7.66 |
| CHEMBL4756424 | — | — | 1 | 7.58 |
| CHEMBL4799661 | — | — | 1 | 7.51 |
| CHEMBL4787590 | — | — | 1 | 7.43 |
| CHEMBL4785004 | — | — | 1 | 7.41 |
| CHEMBL4749327 | — | — | 1 | 7.39 |
| CHEMBL4756997 | — | — | 1 | 7.38 |
| CHEMBL4753347 | — | — | 1 | 7.37 |
| CHEMBL4741219 | — | — | 1 | 7.33 |
| CHEMBL4791286 | — | — | 1 | 7.29 |
| CHEMBL4798419 | — | — | 1 | 7.21 |
| CHEMBL4800403 | — | — | 1 | 7.21 |
| CHEMBL4777788 | — | — | 1 | 7.20 |
| CHEMBL4760288 | — | — | 1 | 7.19 |
| CHEMBL4787169 | — | — | 1 | 7.14 |
| CHEMBL4796602 | — | — | 1 | 7.14 |
| CHEMBL4754192 | — | — | 1 | 7.09 |
| CHEMBL4777926 | — | — | 1 | 7.08 |
| CHEMBL4758531 | — | — | 1 | 7.03 |
| CHEMBL4781117 | — | — | 1 | 6.99 |
| CHEMBL4761239 | — | — | 1 | 6.94 |
| CHEMBL4749678 | — | — | 1 | 6.88 |
| CHEMBL4750284 | — | — | 1 | 6.88 |
| CHEMBL4759230 | — | — | 1 | 6.78 |
| CHEMBL4746403 | — | — | 1 | 6.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4747410 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL4744911 | — | IC50 | = | 14.6 | nM | 7.84 |
| CHEMBL3410089 | — | IC50 | = | 17.2 | nM | 7.76 |
| CHEMBL102714 | SB-216763 | IC50 | = | 19.8 | nM | 7.70 |
| CHEMBL4779478 | — | IC50 | = | 20.8 | nM | 7.68 |
| CHEMBL4789145 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4756424 | — | IC50 | = | 26.3 | nM | 7.58 |
| CHEMBL4799661 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL4787590 | — | IC50 | = | 37.1 | nM | 7.43 |
| CHEMBL4785004 | — | IC50 | = | 39.3 | nM | 7.41 |
| CHEMBL4749327 | — | IC50 | = | 41.1 | nM | 7.39 |
| CHEMBL4756997 | — | IC50 | = | 41.6 | nM | 7.38 |
| CHEMBL4753347 | — | IC50 | = | 42.6 | nM | 7.37 |
| CHEMBL4741219 | — | IC50 | = | 46.7 | nM | 7.33 |
| CHEMBL4791286 | — | IC50 | = | 51.7 | nM | 7.29 |
| CHEMBL4798419 | — | IC50 | = | 62.2 | nM | 7.21 |
| CHEMBL4800403 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL4777788 | — | IC50 | = | 62.6 | nM | 7.20 |
| CHEMBL4760288 | — | IC50 | = | 64.3 | nM | 7.19 |
| CHEMBL4787169 | — | IC50 | = | 71.6 | nM | 7.14 |
| CHEMBL4796602 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL4754192 | — | IC50 | = | 80.7 | nM | 7.09 |
| CHEMBL4777926 | — | IC50 | = | 83.9 | nM | 7.08 |
| CHEMBL4758531 | — | IC50 | = | 92.8 | nM | 7.03 |
| CHEMBL4781117 | — | IC50 | = | 103.6 | nM | 6.99 |
| CHEMBL4761239 | — | IC50 | = | 114.4 | nM | 6.94 |
| CHEMBL4749678 | — | IC50 | = | 130.4 | nM | 6.88 |
| CHEMBL4750284 | — | IC50 | = | 132.4 | nM | 6.88 |
| CHEMBL4759230 | — | IC50 | = | 165.3 | nM | 6.78 |
| CHEMBL4746403 | — | IC50 | = | 239.3 | nM | 6.62 |
| CHEMBL95 | TACRINE | IC50 | > | 1000.0 | nM | - |