Assay Detail
Binding
CHEMBL1787067
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Inhibition of human plasma AChE
9
Total Activities
9
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Plasma |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Quinolizidinyl derivatives of bi- and tricyclic systems as potent inhibitors of acetyl- and butyrylcholinesterase with potential in Alzheimer's disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 5.75 | 7.66 |
| Inhibition | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL502 | DONEPEZIL | 4.0 | 1 | 7.66 |
| CHEMBL95 | TACRINE | 4.0 | 1 | 6.72 |
| CHEMBL659 | GALANTAMINE | 4.0 | 1 | 6.10 |
| CHEMBL636 | RIVASTIGMINE | 4.0 | 1 | 5.38 |
| CHEMBL433041 | EPTASTIGMINE | 2.0 | 1 | 4.66 |
| CHEMBL1782707 | — | — | 1 | 4.00 |
| CHEMBL1080386 | PHENETHYLCYMSERINE | — | 1 | - |
| CHEMBL392577 | — | — | 1 | - |
| CHEMBL1206 | ETHOPROPAZINE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL502 | DONEPEZIL | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL95 | TACRINE | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL659 | GALANTAMINE | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL636 | RIVASTIGMINE | IC50 | = | 4150.0 | nM | 5.38 |
| CHEMBL433041 | EPTASTIGMINE | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL1782707 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL1080386 | PHENETHYLCYMSERINE | IC50 | > | 30000.0 | nM | - |
| CHEMBL392577 | — | Inhibition | - | % | - | |
| CHEMBL1206 | ETHOPROPAZINE | IC50 | = | 260000.0 | nM | - |