Assay Detail
Binding
CHEMBL2066006
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Inhibition of human recombinant AChE using acetylthiocholine substrate preincubated for 5 mins before substrate addition by Ellman's method
11
Total Activities
11
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 |
|---|---|---|---|
| IC50 | 11 | 7.12 | 8.35 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2064471 | — | — | 1 | 8.35 |
| CHEMBL2064465 | — | — | 1 | 8.30 |
| CHEMBL2064464 | — | — | 1 | 7.83 |
| CHEMBL2064468 | — | — | 1 | 7.39 |
| CHEMBL2064404 | — | — | 1 | 7.29 |
| CHEMBL2064466 | — | — | 1 | 7.15 |
| CHEMBL2064470 | — | — | 1 | 7.07 |
| CHEMBL2064469 | — | — | 1 | 6.71 |
| CHEMBL1677 | TACRINE HYDROCHLORIDE | 4.0 | 1 | 6.30 |
| CHEMBL1256415 | — | — | 1 | 4.82 |
| CHEMBL2064467 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2064471 | — | IC50 | = | 4.49 | nM | 8.35 |
| CHEMBL2064465 | — | IC50 | = | 4.97 | nM | 8.30 |
| CHEMBL2064464 | — | IC50 | = | 14.9 | nM | 7.83 |
| CHEMBL2064468 | — | IC50 | = | 40.7 | nM | 7.39 |
| CHEMBL2064404 | — | IC50 | = | 51.7 | nM | 7.29 |
| CHEMBL2064466 | — | IC50 | = | 70.3 | nM | 7.15 |
| CHEMBL2064470 | — | IC50 | = | 84.8 | nM | 7.07 |
| CHEMBL2064469 | — | IC50 | = | 194.0 | nM | 6.71 |
| CHEMBL1677 | TACRINE HYDROCHLORIDE | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL1256415 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL2064467 | — | IC50 | - | — | - |