Assay Detail
Binding
CHEMBL3379803
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Inhibition of human AChE assessed as acetylthiocholine hydrolysis
20
Total Activities
20
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
Syntheses of coumarin-tacrine hybrids as dual-site acetylcholinesterase inhibitors and their activity against butylcholinesterase, Aβ aggregation, and β-secretase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 20 | 7.34 | 7.78 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3326704 | — | — | 1 | 7.78 |
| CHEMBL3326706 | — | — | 1 | 7.61 |
| CHEMBL3326707 | — | — | 1 | 7.52 |
| CHEMBL3326705 | — | — | 1 | 7.51 |
| CHEMBL3326698 | — | — | 1 | 7.46 |
| CHEMBL95 | TACRINE | 4.0 | 1 | 7.45 |
| CHEMBL3326701 | — | — | 1 | 7.45 |
| CHEMBL3326700 | — | — | 1 | 7.41 |
| CHEMBL3326710 | — | — | 1 | 7.38 |
| CHEMBL3326699 | — | — | 1 | 7.35 |
| CHEMBL3327246 | — | — | 1 | 7.29 |
| CHEMBL3326711 | — | — | 1 | 7.26 |
| CHEMBL3326708 | — | — | 1 | 7.25 |
| CHEMBL3326709 | — | — | 1 | 7.22 |
| CHEMBL659 | GALANTAMINE | 4.0 | 1 | 7.21 |
| CHEMBL3327247 | — | — | 1 | 7.18 |
| CHEMBL3326702 | — | — | 1 | 7.16 |
| CHEMBL3326703 | — | — | 1 | 7.12 |
| CHEMBL3327249 | — | — | 1 | 7.11 |
| CHEMBL3327248 | — | — | 1 | 7.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3326704 | — | Ki | = | 16.7 | nM | 7.78 |
| CHEMBL3326706 | — | Ki | = | 24.3 | nM | 7.61 |
| CHEMBL3326707 | — | Ki | = | 30.1 | nM | 7.52 |
| CHEMBL3326705 | — | Ki | = | 30.9 | nM | 7.51 |
| CHEMBL3326698 | — | Ki | = | 34.4 | nM | 7.46 |
| CHEMBL95 | TACRINE | Ki | = | 35.7 | nM | 7.45 |
| CHEMBL3326701 | — | Ki | = | 35.8 | nM | 7.45 |
| CHEMBL3326700 | — | Ki | = | 39.4 | nM | 7.41 |
| CHEMBL3326710 | — | Ki | = | 42.2 | nM | 7.38 |
| CHEMBL3326699 | — | Ki | = | 44.3 | nM | 7.35 |
| CHEMBL3327246 | — | Ki | = | 50.7 | nM | 7.29 |
| CHEMBL3326711 | — | Ki | = | 55.2 | nM | 7.26 |
| CHEMBL3326708 | — | Ki | = | 56.1 | nM | 7.25 |
| CHEMBL3326709 | — | Ki | = | 59.6 | nM | 7.22 |
| CHEMBL659 | GALANTAMINE | Ki | = | 61.9 | nM | 7.21 |
| CHEMBL3327247 | — | Ki | = | 66.1 | nM | 7.18 |
| CHEMBL3326702 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL3326703 | — | Ki | = | 76.1 | nM | 7.12 |
| CHEMBL3327249 | — | Ki | = | 78.2 | nM | 7.11 |
| CHEMBL3327248 | — | Ki | = | 91.1 | nM | 7.04 |