Assay Detail
Binding
CHEMBL4307302
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Inhibition of human recombinant AChE expressed in HEK293 cells using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition by spectrophotometry analysis
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
A novel class of multitarget anti-Alzheimer benzohomoadamantane‒chlorotacrine hybrids modulating cholinesterases and glutamate NMDA receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 8.75 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4471659 | — | — | 1 | 9.52 |
| CHEMBL4462369 | — | — | 1 | 8.89 |
| CHEMBL4558495 | — | — | 1 | 8.85 |
| CHEMBL4438626 | — | — | 1 | 8.85 |
| CHEMBL4469343 | — | — | 1 | 8.70 |
| CHEMBL4591167 | — | — | 1 | 8.60 |
| CHEMBL292314 | — | — | 1 | 7.84 |
| CHEMBL807 | MEMANTINE | 4.0 | 1 | - |
| CHEMBL3259988 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4471659 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4462369 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4558495 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL4438626 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL4469343 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4591167 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL292314 | — | IC50 | = | 14.5 | nM | 7.84 |
| CHEMBL807 | MEMANTINE | IC50 | - | — | - | |
| CHEMBL3259988 | — | IC50 | - | — | - |