Assay Detail
Binding
CHEMBL644108
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Inhibition of acetylcholinesterase isolated from Human erythrocytes.
20
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
New tacrine-huperzine A hybrids (huprines): highly potent tight-binding acetylcholinesterase inhibitors of interest for the treatment of Alzheimer's disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 8.06 | 9.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL208599 | HUPRINE X | — | 3 | 9.49 |
| CHEMBL140476 | HUPRINE Y | — | 3 | 9.49 |
| CHEMBL357207 | — | — | 1 | 8.86 |
| CHEMBL335355 | — | — | 1 | 8.75 |
| CHEMBL341658 | — | — | 3 | 8.68 |
| CHEMBL143290 | — | — | 1 | 8.66 |
| CHEMBL4524111 | — | — | 1 | 8.34 |
| CHEMBL143094 | — | — | 1 | 8.30 |
| CHEMBL139819 | — | — | 1 | 7.93 |
| CHEMBL142491 | — | — | 1 | 7.53 |
| CHEMBL109869 | — | — | 1 | 7.45 |
| CHEMBL95 | TACRINE | 4.0 | 1 | 6.69 |
| CHEMBL395280 | HUPERZINE A | 2.0 | 1 | 6.58 |
| CHEMBL142816 | — | — | 1 | 6.37 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL208599 | HUPRINE X | IC50 | = | 0.32 | nM | 9.49 |
| CHEMBL140476 | HUPRINE Y | IC50 | = | 0.32 | nM | 9.49 |
| CHEMBL208599 | HUPRINE X | IC50 | = | 0.75 | nM | 9.12 |
| CHEMBL140476 | HUPRINE Y | IC50 | = | 0.78 | nM | 9.11 |
| CHEMBL357207 | — | IC50 | = | 1.39 | nM | 8.86 |
| CHEMBL335355 | — | IC50 | = | 1.76 | nM | 8.75 |
| CHEMBL341658 | — | IC50 | = | 2.11 | nM | 8.68 |
| CHEMBL143290 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL341658 | — | IC50 | = | 3.79 | nM | 8.42 |
| CHEMBL4524111 | — | IC50 | = | 4.58 | nM | 8.34 |
| CHEMBL143094 | — | IC50 | = | 4.96 | nM | 8.30 |
| CHEMBL139819 | — | IC50 | = | 11.7 | nM | 7.93 |
| CHEMBL208599 | HUPRINE X | IC50 | = | 23.1 | nM | 7.64 |
| CHEMBL142491 | — | IC50 | = | 29.5 | nM | 7.53 |
| CHEMBL109869 | — | IC50 | = | 35.4 | nM | 7.45 |
| CHEMBL341658 | — | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL140476 | HUPRINE Y | IC50 | = | 123.0 | nM | 6.91 |
| CHEMBL95 | TACRINE | IC50 | = | 205.0 | nM | 6.69 |
| CHEMBL395280 | HUPERZINE A | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL142816 | — | IC50 | = | 425.0 | nM | 6.37 |