Assay Detail
Binding
CHEMBL4711084
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human BuChE using butyrylthiocholine iodide as substrate preincubated with enzyme for 1 min followed by substrate addition and measured after 10 mins by Ellman's method
30
Total Activities
30
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
Rational design and biological evaluation of a new class of thiazolopyridyl tetrahydroacridines as cholinesterase and GSK-3 dual inhibitors for Alzheimer's disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 6.86 | 8.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4798419 | — | — | 1 | 8.49 |
| CHEMBL4800403 | — | — | 1 | 8.09 |
| CHEMBL4754192 | — | — | 1 | 7.51 |
| CHEMBL4787590 | — | — | 1 | 7.43 |
| CHEMBL95 | TACRINE | 4.0 | 1 | 7.40 |
| CHEMBL4756997 | — | — | 1 | 7.32 |
| CHEMBL4746403 | — | — | 1 | 7.05 |
| CHEMBL4789145 | — | — | 1 | 6.82 |
| CHEMBL4760288 | — | — | 1 | 6.77 |
| CHEMBL4758531 | — | — | 1 | 6.76 |
| CHEMBL4753347 | — | — | 1 | 6.72 |
| CHEMBL4777926 | — | — | 1 | 6.70 |
| CHEMBL4781117 | — | — | 1 | 6.67 |
| CHEMBL4759230 | — | — | 1 | 6.63 |
| CHEMBL4749327 | — | — | 1 | 6.58 |
| CHEMBL4749678 | — | — | 1 | 6.56 |
| CHEMBL4796602 | — | — | 1 | 6.52 |
| CHEMBL4787169 | — | — | 1 | 6.48 |
| CHEMBL4779478 | — | — | 1 | 6.44 |
| CHEMBL4761239 | — | — | 1 | 6.29 |
| CHEMBL4791286 | — | — | 1 | 6.22 |
| CHEMBL4777788 | — | — | 1 | 6.21 |
| CHEMBL4750284 | — | — | 1 | 6.21 |
| CHEMBL4785004 | — | — | 1 | - |
| CHEMBL3410089 | — | — | 1 | - |
| CHEMBL4799661 | — | — | 1 | - |
| CHEMBL4756424 | — | — | 1 | - |
| CHEMBL4744911 | — | — | 1 | - |
| CHEMBL4741219 | — | — | 1 | - |
| CHEMBL4747410 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4798419 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL4800403 | — | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL4754192 | — | IC50 | = | 30.7 | nM | 7.51 |
| CHEMBL4787590 | — | IC50 | = | 37.5 | nM | 7.43 |
| CHEMBL95 | TACRINE | IC50 | = | 39.6 | nM | 7.40 |
| CHEMBL4756997 | — | IC50 | = | 48.3 | nM | 7.32 |
| CHEMBL4746403 | — | IC50 | = | 89.5 | nM | 7.05 |
| CHEMBL4789145 | — | IC50 | = | 149.8 | nM | 6.82 |
| CHEMBL4760288 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4758531 | — | IC50 | = | 173.4 | nM | 6.76 |
| CHEMBL4753347 | — | IC50 | = | 189.8 | nM | 6.72 |
| CHEMBL4777926 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4781117 | — | IC50 | = | 215.9 | nM | 6.67 |
| CHEMBL4759230 | — | IC50 | = | 235.6 | nM | 6.63 |
| CHEMBL4749327 | — | IC50 | = | 262.4 | nM | 6.58 |
| CHEMBL4749678 | — | IC50 | = | 276.7 | nM | 6.56 |
| CHEMBL4796602 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4787169 | — | IC50 | = | 330.1 | nM | 6.48 |
| CHEMBL4779478 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL4761239 | — | IC50 | = | 512.4 | nM | 6.29 |
| CHEMBL4791286 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL4777788 | — | IC50 | = | 612.9 | nM | 6.21 |
| CHEMBL4750284 | — | IC50 | = | 619.4 | nM | 6.21 |
| CHEMBL4785004 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL3410089 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4799661 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4756424 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4744911 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4741219 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4747410 | — | IC50 | > | 1000.0 | nM | - |