Assay Detail
Binding
CHEMBL4424917
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Inhibition of recombinant human BuChE using butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition and measured for 5 mins 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
Highly potent and selective aryl-1,2,3-triazolyl benzylpiperidine inhibitors toward butyrylcholinesterase in Alzheimer's disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 6.37 | 9.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4464964 | — | — | 1 | 9.77 |
| CHEMBL4520568 | — | — | 1 | 8.00 |
| CHEMBL4446441 | — | — | 1 | 7.19 |
| CHEMBL4467345 | — | — | 1 | 6.01 |
| CHEMBL4445099 | — | — | 1 | 5.99 |
| CHEMBL4557745 | — | — | 1 | 5.72 |
| CHEMBL4440392 | — | — | 1 | 5.53 |
| CHEMBL4448634 | — | — | 1 | 5.28 |
| CHEMBL4437391 | — | — | 1 | 5.15 |
| CHEMBL502 | DONEPEZIL | 4.0 | 1 | 5.04 |
| CHEMBL4534345 | — | — | 1 | - |
| CHEMBL4574766 | — | — | 1 | - |
| CHEMBL4438642 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4464964 | — | IC50 | = | 0.17 | nM | 9.77 |
| CHEMBL4520568 | — | IC50 | = | 9.9 | nM | 8.00 |
| CHEMBL4446441 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL4467345 | — | IC50 | = | 970.0 | nM | 6.01 |
| CHEMBL4445099 | — | IC50 | = | 1020.0 | nM | 5.99 |
| CHEMBL4557745 | — | IC50 | = | 1910.0 | nM | 5.72 |
| CHEMBL4440392 | — | IC50 | = | 2950.0 | nM | 5.53 |
| CHEMBL4448634 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL4437391 | — | IC50 | = | 7060.0 | nM | 5.15 |
| CHEMBL502 | DONEPEZIL | IC50 | = | 9140.0 | nM | 5.04 |
| CHEMBL4534345 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4574766 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4438642 | — | IC50 | > | 10000.0 | nM | - |