Assay Detail
Binding
CHEMBL4269385
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Inhibition of AChE in Swiss Webster mouse cerebral homogenate using acetylthiocholine iodide as substrate preincubated for 10 mins followed substrate addition measured after 10 mins by Ellman's method
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, synthesis, cholinesterase inhibition and molecular modelling study of novel tacrine hybrids with carbohydrate derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 7.90 | 8.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL32823 | — | — | 1 | 8.72 |
| CHEMBL4280262 | — | — | 1 | 8.66 |
| CHEMBL4287482 | — | — | 1 | 8.32 |
| CHEMBL4283717 | — | — | 1 | 8.29 |
| CHEMBL4282214 | — | — | 1 | 8.12 |
| CHEMBL4287068 | — | — | 1 | 8.06 |
| CHEMBL4294287 | — | — | 1 | 7.99 |
| CHEMBL95 | TACRINE | 4.0 | 1 | 7.46 |
| CHEMBL4276832 | — | — | 1 | 7.18 |
| CHEMBL4279148 | — | — | 1 | 7.07 |
| CHEMBL4290902 | — | — | 1 | 7.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL32823 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL4280262 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL4287482 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL4283717 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL4282214 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL4287068 | — | IC50 | = | 8.7 | nM | 8.06 |
| CHEMBL4294287 | — | IC50 | = | 10.2 | nM | 7.99 |
| CHEMBL95 | TACRINE | IC50 | = | 34.3 | nM | 7.46 |
| CHEMBL4276832 | — | IC50 | = | 65.5 | nM | 7.18 |
| CHEMBL4279148 | — | IC50 | = | 84.4 | nM | 7.07 |
| CHEMBL4290902 | — | IC50 | = | 89.9 | nM | 7.05 |