Assay Detail
Binding
CHEMBL5501445
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition and measured after 10 mins by DTNB-reagent based Ellman's method
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Electrophorus electricus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Novel 6-alkyl-bridged 4-arylalkylpiperazin-1-yl derivatives of azepino[4,3-b]indol-1(2H)-one as potent BChE-selective inhibitors showing protective effects against neurodegenerative insults.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 5.72 | 7.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL502 | DONEPEZIL | 4.0 | 1 | 7.68 |
| CHEMBL95 | TACRINE | 4.0 | 1 | 6.54 |
| CHEMBL5555131 | — | — | 1 | 6.40 |
| CHEMBL5532253 | — | — | 1 | 5.83 |
| CHEMBL5556474 | — | — | 1 | 5.74 |
| CHEMBL5555332 | — | — | 1 | 5.31 |
| CHEMBL5557312 | — | — | 1 | 5.23 |
| CHEMBL5542336 | — | — | 1 | 5.18 |
| CHEMBL5559422 | — | — | 1 | 5.15 |
| CHEMBL5557601 | — | — | 1 | 5.04 |
| CHEMBL5512467 | — | — | 1 | 4.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL502 | DONEPEZIL | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL95 | TACRINE | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL5555131 | — | IC50 | = | 402.0 | nM | 6.40 |
| CHEMBL5532253 | — | IC50 | = | 1480.0 | nM | 5.83 |
| CHEMBL5556474 | — | IC50 | = | 1830.0 | nM | 5.74 |
| CHEMBL5555332 | — | IC50 | = | 4940.0 | nM | 5.31 |
| CHEMBL5557312 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL5542336 | — | IC50 | = | 6570.0 | nM | 5.18 |
| CHEMBL5559422 | — | IC50 | = | 7060.0 | nM | 5.15 |
| CHEMBL5557601 | — | IC50 | = | 9100.0 | nM | 5.04 |
| CHEMBL5512467 | — | IC50 | = | 15000.0 | nM | 4.82 |