Assay Detail
Binding
CHEMBL2066010
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Inhibition of human recombinant AChE assessed as dissociation constant for enzyme-inhibitor-substrate complex using acetylthiocholine substrate preincubated for 5 mins before substrate addition by Ellman's method
9
Total Activities
9
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
Synthesis, design and biological evaluation of novel highly potent tacrine congeners for the treatment of Alzheimer's disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 7.41 | 9.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2064464 | — | — | 1 | 9.50 |
| CHEMBL2064465 | — | — | 1 | 8.43 |
| CHEMBL2064470 | — | — | 1 | 7.61 |
| CHEMBL2064468 | — | — | 1 | 7.32 |
| CHEMBL2064404 | — | — | 1 | 7.12 |
| CHEMBL2064466 | — | — | 1 | 7.07 |
| CHEMBL1677 | TACRINE HYDROCHLORIDE | 4.0 | 1 | 7.00 |
| CHEMBL1256415 | — | — | 1 | 5.20 |
| CHEMBL2064467 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2064464 | — | Ki | = | 0.318 | nM | 9.50 |
| CHEMBL2064465 | — | Ki | = | 3.73 | nM | 8.43 |
| CHEMBL2064470 | — | Ki | = | 24.7 | nM | 7.61 |
| CHEMBL2064468 | — | Ki | = | 47.6 | nM | 7.32 |
| CHEMBL2064404 | — | Ki | = | 76.1 | nM | 7.12 |
| CHEMBL2064466 | — | Ki | = | 85.5 | nM | 7.07 |
| CHEMBL1677 | TACRINE HYDROCHLORIDE | Ki | = | 101.0 | nM | 7.00 |
| CHEMBL1256415 | — | Ki | = | 6340.0 | nM | 5.20 |
| CHEMBL2064467 | — | Ki | - | — | - |