Assay Detail
Binding
CHEMBL5338147
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition and measured every min for 10 mins by Ellman's method
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Equus caballus |
| Tissue | Serum |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, synthesis and preliminary biological evaluation of rivastigmine-INDY hybrids as multitarget ligands against Alzheimer's disease by targeting butyrylcholinesterase and DYRK1A/CLK1 kinases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 6.23 | 8.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL95 | TACRINE | 4.0 | 1 | 8.72 |
| CHEMBL5402840 | — | — | 1 | 7.57 |
| CHEMBL5396284 | — | — | 1 | 7.17 |
| CHEMBL5417812 | — | — | 1 | 6.81 |
| CHEMBL5408824 | — | — | 1 | 6.36 |
| CHEMBL5402721 | — | — | 1 | 6.33 |
| CHEMBL5408141 | — | — | 1 | 6.15 |
| CHEMBL5397089 | — | — | 1 | 6.12 |
| CHEMBL5398338 | — | — | 1 | 6.09 |
| CHEMBL5398767 | — | — | 1 | 5.79 |
| CHEMBL5407180 | — | — | 1 | 5.70 |
| CHEMBL5428725 | — | — | 1 | 5.66 |
| CHEMBL5407164 | — | — | 1 | 5.22 |
| CHEMBL5434888 | — | — | 1 | 4.92 |
| CHEMBL5414144 | — | — | 1 | 4.89 |
| CHEMBL5440931 | — | — | 1 | - |
| CHEMBL5412852 | — | — | 1 | - |
| CHEMBL5400482 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL95 | TACRINE | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL5402840 | — | IC50 | = | 26.7 | nM | 7.57 |
| CHEMBL5396284 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL5417812 | — | IC50 | = | 154.0 | nM | 6.81 |
| CHEMBL5408824 | — | IC50 | = | 439.0 | nM | 6.36 |
| CHEMBL5402721 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL5408141 | — | IC50 | = | 703.0 | nM | 6.15 |
| CHEMBL5397089 | — | IC50 | = | 761.0 | nM | 6.12 |
| CHEMBL5398338 | — | IC50 | = | 821.0 | nM | 6.09 |
| CHEMBL5398767 | — | IC50 | = | 1640.0 | nM | 5.79 |
| CHEMBL5407180 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL5428725 | — | IC50 | = | 2195.0 | nM | 5.66 |
| CHEMBL5407164 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL5434888 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL5414144 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL5440931 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5412852 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5400482 | — | IC50 | > | 10000.0 | nM | - |