Assay Detail
Binding
CHEMBL4688568
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Inhibition of human recombinant AChE expressed in HEK293 cells using acetylthiocholine iodide as substrate incubated for 10 mins by Ellman's method
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| 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 | 25 | 5.39 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL502 | DONEPEZIL | 4.0 | 1 | 8.30 |
| CHEMBL95 | TACRINE | 4.0 | 1 | 6.72 |
| CHEMBL4747992 | — | — | 1 | 6.51 |
| CHEMBL4794823 | — | — | 1 | 6.42 |
| CHEMBL4796437 | — | — | 1 | 6.14 |
| CHEMBL4748993 | — | — | 1 | 5.88 |
| CHEMBL4753478 | — | — | 1 | 5.82 |
| CHEMBL4776811 | — | — | 1 | 5.52 |
| CHEMBL4742138 | — | — | 1 | 5.43 |
| CHEMBL4764558 | — | — | 1 | 5.35 |
| CHEMBL4795876 | — | — | 1 | 5.33 |
| CHEMBL4792678 | — | — | 1 | 5.22 |
| CHEMBL4749550 | — | — | 1 | 5.18 |
| CHEMBL4759253 | — | — | 1 | 5.11 |
| CHEMBL4748792 | — | — | 1 | 5.10 |
| CHEMBL4753139 | — | — | 1 | 5.05 |
| CHEMBL4755445 | — | — | 1 | 4.71 |
| CHEMBL4756451 | — | — | 1 | 4.37 |
| CHEMBL4752296 | — | — | 1 | 4.14 |
| CHEMBL4741669 | — | — | 1 | 4.10 |
| CHEMBL4791089 | — | — | 1 | 4.09 |
| CHEMBL4746460 | — | — | 1 | 4.01 |
| CHEMBL4787873 | — | — | 1 | - |
| CHEMBL4785551 | — | — | 1 | - |
| CHEMBL4792741 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL502 | DONEPEZIL | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL95 | TACRINE | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL4747992 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL4794823 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL4796437 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL4748993 | — | IC50 | = | 1320.0 | nM | 5.88 |
| CHEMBL4753478 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4776811 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL4742138 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL4764558 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL4795876 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL4792678 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL4749550 | — | IC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL4759253 | — | IC50 | = | 7800.0 | nM | 5.11 |
| CHEMBL4748792 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL4753139 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL4755445 | — | IC50 | = | 19500.0 | nM | 4.71 |
| CHEMBL4756451 | — | IC50 | = | 42800.0 | nM | 4.37 |
| CHEMBL4752296 | — | IC50 | = | 73000.0 | nM | 4.14 |
| CHEMBL4741669 | — | IC50 | = | 80000.0 | nM | 4.10 |
| CHEMBL4791089 | — | IC50 | = | 82000.0 | nM | 4.09 |
| CHEMBL4746460 | — | IC50 | = | 97000.0 | nM | 4.01 |
| CHEMBL4787873 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL4785551 | — | IC50 | = | 394000.0 | nM | - |
| CHEMBL4792741 | — | IC50 | > | 1000000.0 | nM | - |