Assay Detail
Binding
CHEMBL4831996
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant N-terminal His-tagged GSK3beta expressed in Escherichia coli using RRRPASVPPSPSLS RHS(pS)HQRR as substrate incubated for 30 mins in presence of ATP by Kinase-Glo reagent based luminescence assay
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of 2-(cyclopropanecarboxamido)-N-(5-((1-(4-fluorobenzyl)piperidin-4-yl)methoxy)pyridin-3-yl)isonicotinamide as a potent dual AChE/GSK3β inhibitor for the treatment of Alzheimer's disease: Significantly increasing the level of acetylcholine in the brain without affecting that in intestine.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 33 | 6.63 | 7.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4863960 | — | — | 1 | 7.64 |
| CHEMBL102714 | SB-216763 | — | 1 | 7.54 |
| CHEMBL4873612 | — | — | 1 | 7.51 |
| CHEMBL4854209 | — | — | 1 | 7.20 |
| CHEMBL4865061 | — | — | 1 | 7.11 |
| CHEMBL4854572 | — | — | 1 | 7.10 |
| CHEMBL4867249 | — | — | 1 | 7.10 |
| CHEMBL4857955 | — | — | 1 | 7.09 |
| CHEMBL4873162 | — | — | 1 | 7.02 |
| CHEMBL4866150 | — | — | 1 | 7.01 |
| CHEMBL4857680 | — | — | 1 | 6.90 |
| CHEMBL4853675 | — | — | 1 | 6.82 |
| CHEMBL4872690 | — | — | 1 | 6.80 |
| CHEMBL4870746 | — | — | 1 | 6.79 |
| CHEMBL4851865 | — | — | 1 | 6.70 |
| CHEMBL4864059 | — | — | 1 | 6.64 |
| CHEMBL4868956 | — | — | 1 | 6.61 |
| CHEMBL4865615 | — | — | 1 | 6.55 |
| CHEMBL4851835 | — | — | 1 | 6.52 |
| CHEMBL4855714 | — | — | 1 | 6.13 |
| CHEMBL4877175 | — | — | 1 | 6.08 |
| CHEMBL4875903 | — | — | 1 | 5.46 |
| CHEMBL4849828 | — | — | 1 | 5.31 |
| CHEMBL4862811 | — | — | 1 | 5.17 |
| CHEMBL4855201 | — | — | 1 | 5.01 |
| CHEMBL4846646 | — | — | 1 | - |
| CHEMBL4870273 | — | — | 1 | - |
| CHEMBL4846945 | — | — | 1 | - |
| CHEMBL4877556 | — | — | 1 | - |
| CHEMBL4850776 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4863960 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL102714 | SB-216763 | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4873612 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL4854209 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL4865061 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL4854572 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL4867249 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL4857955 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL4873162 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL4866150 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL4857680 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL4853675 | — | IC50 | = | 152.0 | nM | 6.82 |
| CHEMBL4872690 | — | IC50 | = | 157.0 | nM | 6.80 |
| CHEMBL4870746 | — | IC50 | = | 164.0 | nM | 6.79 |
| CHEMBL4851865 | — | IC50 | = | 198.0 | nM | 6.70 |
| CHEMBL4864059 | — | IC50 | = | 231.0 | nM | 6.64 |
| CHEMBL4868956 | — | IC50 | = | 244.0 | nM | 6.61 |
| CHEMBL4865615 | — | IC50 | = | 279.0 | nM | 6.55 |
| CHEMBL4851835 | — | IC50 | = | 305.0 | nM | 6.52 |
| CHEMBL4855714 | — | IC50 | = | 734.0 | nM | 6.13 |
| CHEMBL4877175 | — | IC50 | = | 837.0 | nM | 6.08 |
| CHEMBL4875903 | — | IC50 | = | 3508.0 | nM | 5.46 |
| CHEMBL4849828 | — | IC50 | = | 4935.0 | nM | 5.31 |
| CHEMBL4862811 | — | IC50 | = | 6804.0 | nM | 5.17 |
| CHEMBL4855201 | — | IC50 | = | 9748.0 | nM | 5.01 |
| CHEMBL4846646 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4870273 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4846945 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4877556 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4850776 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4870877 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4859041 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL502 | DONEPEZIL | IC50 | > | 10000.0 | nM | - |