Assay Detail
Binding
CHEMBL3379809
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Inhibition of human BuChE pre-incubated for 5 mins before butylthiocholine 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 | 5.94 | 7.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL95 | TACRINE | 4.0 | 1 | 7.64 |
| CHEMBL3322142 | — | — | 1 | 6.64 |
| CHEMBL3322141 | — | — | 1 | 6.57 |
| CHEMBL3322160 | — | — | 1 | 6.48 |
| CHEMBL3322140 | — | — | 1 | 6.12 |
| CHEMBL3322159 | — | — | 1 | 6.08 |
| CHEMBL3322161 | — | — | 1 | 5.85 |
| CHEMBL3322155 | — | — | 1 | 5.69 |
| CHEMBL3322157 | — | — | 1 | 5.65 |
| CHEMBL3322156 | — | — | 1 | 5.62 |
| CHEMBL3322162 | — | — | 1 | 5.25 |
| CHEMBL3322158 | — | — | 1 | 4.90 |
| CHEMBL1256415 | — | — | 1 | 4.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL95 | TACRINE | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3322142 | — | IC50 | = | 228.0 | nM | 6.64 |
| CHEMBL3322141 | — | IC50 | = | 267.0 | nM | 6.57 |
| CHEMBL3322160 | — | IC50 | = | 328.0 | nM | 6.48 |
| CHEMBL3322140 | — | IC50 | = | 765.0 | nM | 6.12 |
| CHEMBL3322159 | — | IC50 | = | 827.0 | nM | 6.08 |
| CHEMBL3322161 | — | IC50 | = | 1420.0 | nM | 5.85 |
| CHEMBL3322155 | — | IC50 | = | 2030.0 | nM | 5.69 |
| CHEMBL3322157 | — | IC50 | = | 2230.0 | nM | 5.65 |
| CHEMBL3322156 | — | IC50 | = | 2380.0 | nM | 5.62 |
| CHEMBL3322162 | — | IC50 | = | 5620.0 | nM | 5.25 |
| CHEMBL3322158 | — | IC50 | = | 12600.0 | nM | 4.90 |
| CHEMBL1256415 | — | IC50 | = | 21000.0 | nM | 4.68 |