Assay Detail
Binding
CHEMBL960590
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Inhibition of human serum BChE by Ellman's assay
15
Total Activities
15
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
Novel donepezil-based inhibitors of acetyl- and butyrylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 7.17 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL484306 | — | — | 1 | 9.22 |
| CHEMBL3216209 | — | — | 1 | 8.14 |
| CHEMBL3216208 | — | — | 1 | 8.09 |
| CHEMBL2448138 | 9-[(2-{4-[(5,6-Dimethoxy-1-oxoindan-2-yl)methyl]piperidin-1-yl}ethyl)amino]-1,2,3,4-tetrahydroacridine dihydrochloride | — | 1 | 7.91 |
| CHEMBL3216886 | — | — | 1 | 7.91 |
| CHEMBL95 | TACRINE | 4.0 | 1 | 7.62 |
| CHEMBL1677 | TACRINE HYDROCHLORIDE | 4.0 | 1 | 7.36 |
| CHEMBL3216655 | — | — | 1 | 7.18 |
| CHEMBL3217103 | — | — | 1 | 7.14 |
| CHEMBL3216210 | — | — | 1 | 7.05 |
| CHEMBL3216422 | — | — | 1 | 6.87 |
| CHEMBL486698 | — | — | 1 | 6.71 |
| CHEMBL502 | DONEPEZIL | 4.0 | 1 | 6.03 |
| CHEMBL486699 | — | — | 1 | 5.19 |
| CHEMBL1678 | DONEPEZIL HYDROCHLORIDE | 4.0 | 1 | 5.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL484306 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3216209 | — | IC50 | = | 7.25 | nM | 8.14 |
| CHEMBL3216208 | — | IC50 | = | 8.06 | nM | 8.09 |
| CHEMBL2448138 | 9-[(2-{4-[(5,6-Dimethoxy-1-oxoindan-2-yl)methyl]piperidin-1-yl}ethyl)amino]-1,2,3,4-tetrahydroacridine dihydrochloride | IC50 | = | 12.4 | nM | 7.91 |
| CHEMBL3216886 | — | IC50 | = | 12.3 | nM | 7.91 |
| CHEMBL95 | TACRINE | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL1677 | TACRINE HYDROCHLORIDE | IC50 | = | 43.9 | nM | 7.36 |
| CHEMBL3216655 | — | IC50 | = | 66.3 | nM | 7.18 |
| CHEMBL3217103 | — | IC50 | = | 72.7 | nM | 7.14 |
| CHEMBL3216210 | — | IC50 | = | 88.7 | nM | 7.05 |
| CHEMBL3216422 | — | IC50 | = | 136.0 | nM | 6.87 |
| CHEMBL486698 | — | IC50 | = | 196.0 | nM | 6.71 |
| CHEMBL502 | DONEPEZIL | IC50 | = | 930.0 | nM | 6.03 |
| CHEMBL486699 | — | IC50 | = | 6401.0 | nM | 5.19 |
| CHEMBL1678 | DONEPEZIL HYDROCHLORIDE | IC50 | = | 7273.0 | nM | 5.14 |