Assay Detail
Binding
CHEMBL654411
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Inhibition of butyrylcholinesterase (BChE) activity in human serum
17
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Serum |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Synthesis, in vitro pharmacology, and molecular modeling of very potent tacrine-huperzine A hybrids as acetylcholinesterase inhibitors of potential interest for the treatment of Alzheimer's disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 6.70 | 7.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL95 | TACRINE | 4.0 | 1 | 7.36 |
| CHEMBL325338 | — | — | 3 | 7.20 |
| CHEMBL322281 | — | — | 3 | 7.05 |
| CHEMBL322343 | — | — | 3 | 6.94 |
| CHEMBL4524111 | — | — | 3 | 6.86 |
| CHEMBL109870 | — | — | 1 | 6.35 |
| CHEMBL322106 | — | — | 1 | 6.29 |
| CHEMBL109869 | — | — | 1 | 6.26 |
| CHEMBL395280 | HUPERZINE A | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL95 | TACRINE | IC50 | = | 43.9 | nM | 7.36 |
| CHEMBL325338 | — | IC50 | = | 63.3 | nM | 7.20 |
| CHEMBL325338 | — | IC50 | = | 79.3 | nM | 7.10 |
| CHEMBL322281 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL325338 | — | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL322343 | — | IC50 | = | 115.0 | nM | 6.94 |
| CHEMBL322281 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL4524111 | — | IC50 | = | 138.0 | nM | 6.86 |
| CHEMBL4524111 | — | IC50 | = | 197.0 | nM | 6.71 |
| CHEMBL322343 | — | IC50 | = | 208.0 | nM | 6.68 |
| CHEMBL322281 | — | IC50 | = | 316.0 | nM | 6.50 |
| CHEMBL322343 | — | IC50 | = | 347.0 | nM | 6.46 |
| CHEMBL109870 | — | IC50 | = | 449.0 | nM | 6.35 |
| CHEMBL322106 | — | IC50 | = | 512.0 | nM | 6.29 |
| CHEMBL109869 | — | IC50 | = | 543.0 | nM | 6.26 |
| CHEMBL4524111 | — | IC50 | = | 2930.0 | nM | 5.53 |
| CHEMBL395280 | HUPERZINE A | IC50 | > | 100000.0 | nM | - |