Assay Detail
Binding
CHEMBL644099
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Anticholinesterase activity against erythrocyte acetylcholinesterase (AChE) in humans.
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Syntheses and anticholinesterase activities of (3aS)-N1, N8-bisnorphenserine, (3aS)-N1,N8-bisnorphysostigmine, their antipodal isomers, and other potential metabolites of phenserine.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 6.65 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL309667 | — | — | 1 | 7.96 |
| CHEMBL80247 | — | — | 1 | 7.86 |
| CHEMBL74089 | — | — | 1 | 7.68 |
| CHEMBL419470 | — | — | 1 | 7.66 |
| CHEMBL54727 | — | — | 1 | 7.62 |
| CHEMBL94 | PHYSOSTIGMINE | 3.0 | 1 | 7.55 |
| CHEMBL418917 | — | — | 1 | 7.39 |
| CHEMBL431784 | — | — | 1 | 7.25 |
| CHEMBL80221 | — | — | 1 | 6.79 |
| CHEMBL309351 | — | — | 1 | 6.64 |
| CHEMBL76241 | — | — | 1 | 6.48 |
| CHEMBL77896 | — | — | 1 | 5.96 |
| CHEMBL75743 | — | — | 1 | 5.83 |
| CHEMBL75919 | — | — | 1 | 5.46 |
| CHEMBL440497 | — | — | 1 | 5.45 |
| CHEMBL76640 | (+)-PHYSOSTIGMINE | — | 1 | 5.00 |
| CHEMBL76135 | — | — | 1 | 4.39 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL309667 | — | IC50 | = | 10.9 | nM | 7.96 |
| CHEMBL80247 | — | IC50 | = | 13.8 | nM | 7.86 |
| CHEMBL74089 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL419470 | — | IC50 | = | 22.1 | nM | 7.66 |
| CHEMBL54727 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL94 | PHYSOSTIGMINE | IC50 | = | 27.9 | nM | 7.55 |
| CHEMBL418917 | — | IC50 | = | 40.8 | nM | 7.39 |
| CHEMBL431784 | — | IC50 | = | 56.7 | nM | 7.25 |
| CHEMBL80221 | — | IC50 | = | 161.0 | nM | 6.79 |
| CHEMBL309351 | — | IC50 | = | 231.0 | nM | 6.64 |
| CHEMBL76241 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL77896 | — | IC50 | = | 1090.0 | nM | 5.96 |
| CHEMBL75743 | — | IC50 | = | 1490.0 | nM | 5.83 |
| CHEMBL75919 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL440497 | — | IC50 | = | 3560.0 | nM | 5.45 |
| CHEMBL76640 | (+)-PHYSOSTIGMINE | IC50 | = | 9890.0 | nM | 5.00 |
| CHEMBL76135 | — | IC50 | = | 41130.0 | nM | 4.39 |