Assay Detail
Binding
CHEMBL3379808
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Inhibition of human recombinant AChE pre-incubated for 5 mins before acetylthiocholine substrate addition by Ellman's method
13
Total Activities
13
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 and biological evaluation of novel tacrine derivatives and tacrine-coumarin hybrids as cholinesterase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 6.29 | 7.81 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3322160 | — | — | 1 | 7.81 |
| CHEMBL3322141 | — | — | 1 | 7.58 |
| CHEMBL3322142 | — | — | 1 | 7.03 |
| CHEMBL3322157 | — | — | 1 | 6.98 |
| CHEMBL3322140 | — | — | 1 | 6.63 |
| CHEMBL3322159 | — | — | 1 | 6.56 |
| CHEMBL3322156 | — | — | 1 | 6.40 |
| CHEMBL95 | TACRINE | 4.0 | 1 | 6.30 |
| CHEMBL3322155 | — | — | 1 | 6.24 |
| CHEMBL3322158 | — | — | 1 | 5.54 |
| CHEMBL3322161 | — | — | 1 | 5.09 |
| CHEMBL1256415 | — | — | 1 | 4.82 |
| CHEMBL3322162 | — | — | 1 | 4.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3322160 | — | IC50 | = | 15.4 | nM | 7.81 |
| CHEMBL3322141 | — | IC50 | = | 26.3 | nM | 7.58 |
| CHEMBL3322142 | — | IC50 | = | 94.2 | nM | 7.03 |
| CHEMBL3322157 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL3322140 | — | IC50 | = | 233.0 | nM | 6.63 |
| CHEMBL3322159 | — | IC50 | = | 277.0 | nM | 6.56 |
| CHEMBL3322156 | — | IC50 | = | 398.0 | nM | 6.40 |
| CHEMBL95 | TACRINE | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL3322155 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL3322158 | — | IC50 | = | 2910.0 | nM | 5.54 |
| CHEMBL3322161 | — | IC50 | = | 8170.0 | nM | 5.09 |
| CHEMBL1256415 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL3322162 | — | IC50 | = | 15700.0 | nM | 4.80 |