Assay Detail
Binding
CHEMBL654885
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Inhibition of butyrylcholinesterase (BChE) in human serum
25
Total Activities
19
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
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 | 25 | 6.78 | 7.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL208599 | HUPRINE X | — | 3 | 7.80 |
| CHEMBL341658 | — | — | 3 | 7.49 |
| CHEMBL143094 | — | — | 1 | 7.49 |
| CHEMBL95 | TACRINE | 4.0 | 1 | 7.36 |
| CHEMBL325338 | — | — | 1 | 7.10 |
| CHEMBL142491 | — | — | 1 | 6.96 |
| CHEMBL322281 | — | — | 1 | 6.90 |
| CHEMBL140476 | HUPRINE Y | — | 3 | 6.82 |
| CHEMBL4524111 | — | — | 1 | 6.71 |
| CHEMBL335355 | — | — | 1 | 6.71 |
| CHEMBL322343 | — | — | 1 | 6.68 |
| CHEMBL139819 | — | — | 1 | 6.48 |
| CHEMBL109870 | — | — | 1 | 6.35 |
| CHEMBL322106 | — | — | 1 | 6.29 |
| CHEMBL109869 | — | — | 1 | 6.26 |
| CHEMBL142816 | — | — | 1 | 6.12 |
| CHEMBL143290 | — | — | 1 | 6.02 |
| CHEMBL357207 | — | — | 1 | 5.92 |
| CHEMBL395280 | HUPERZINE A | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL208599 | HUPRINE X | IC50 | = | 15.8 | nM | 7.80 |
| CHEMBL341658 | — | IC50 | = | 32.4 | nM | 7.49 |
| CHEMBL143094 | — | IC50 | = | 32.6 | nM | 7.49 |
| CHEMBL95 | TACRINE | IC50 | = | 43.9 | nM | 7.36 |
| CHEMBL341658 | — | IC50 | = | 57.4 | nM | 7.24 |
| CHEMBL208599 | HUPRINE X | IC50 | = | 58.3 | nM | 7.23 |
| CHEMBL325338 | — | IC50 | = | 79.3 | nM | 7.10 |
| CHEMBL142491 | — | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL322281 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL140476 | HUPRINE Y | IC50 | = | 153.0 | nM | 6.82 |
| CHEMBL208599 | HUPRINE X | IC50 | = | 159.0 | nM | 6.80 |
| CHEMBL341658 | — | IC50 | = | 185.0 | nM | 6.73 |
| CHEMBL4524111 | — | IC50 | = | 197.0 | nM | 6.71 |
| CHEMBL335355 | — | IC50 | = | 194.0 | nM | 6.71 |
| CHEMBL322343 | — | IC50 | = | 208.0 | nM | 6.68 |
| CHEMBL140476 | HUPRINE Y | IC50 | = | 236.0 | nM | 6.63 |
| CHEMBL140476 | HUPRINE Y | IC50 | = | 247.0 | nM | 6.61 |
| CHEMBL139819 | — | IC50 | = | 331.0 | nM | 6.48 |
| CHEMBL109870 | — | IC50 | = | 449.0 | nM | 6.35 |
| CHEMBL322106 | — | IC50 | = | 512.0 | nM | 6.29 |
| CHEMBL109869 | — | IC50 | = | 543.0 | nM | 6.26 |
| CHEMBL142816 | — | IC50 | = | 762.0 | nM | 6.12 |
| CHEMBL143290 | — | IC50 | = | 963.0 | nM | 6.02 |
| CHEMBL357207 | — | IC50 | = | 1210.0 | nM | 5.92 |
| CHEMBL395280 | HUPERZINE A | IC50 | > | 10000.0 | nM | - |