Assay Detail
Binding
CHEMBL1787069
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Inhibition of human plasma BChE
10
Total Activities
10
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 | 9 | 6.87 | 8.30 |
| Ki | 1 | 8.46 | 8.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL392577 | — | — | 1 | 8.46 |
| CHEMBL433041 | EPTASTIGMINE | 2.0 | 1 | 8.30 |
| CHEMBL1080386 | PHENETHYLCYMSERINE | — | 1 | 8.22 |
| CHEMBL1782707 | — | — | 1 | 8.05 |
| CHEMBL636 | RIVASTIGMINE | 4.0 | 1 | 7.43 |
| CHEMBL95 | TACRINE | 4.0 | 1 | 7.33 |
| CHEMBL1206 | ETHOPROPAZINE | 4.0 | 1 | 6.52 |
| CHEMBL1782730 | — | — | 1 | 5.47 |
| CHEMBL502 | DONEPEZIL | 4.0 | 1 | 5.38 |
| CHEMBL659 | GALANTAMINE | 4.0 | 1 | 5.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL392577 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL433041 | EPTASTIGMINE | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1080386 | PHENETHYLCYMSERINE | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL1782707 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL636 | RIVASTIGMINE | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL95 | TACRINE | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL1206 | ETHOPROPAZINE | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL1782730 | — | IC50 | = | 3370.0 | nM | 5.47 |
| CHEMBL502 | DONEPEZIL | IC50 | = | 4150.0 | nM | 5.38 |
| CHEMBL659 | GALANTAMINE | IC50 | = | 7300.0 | nM | 5.14 |