Assay Detail
Binding
CHEMBL5501446
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Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition and measured after 10 mins by DTNB based Ellman's method
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Equus caballus |
| 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 | 23 | 5.92 | 7.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL95 | TACRINE | 4.0 | 1 | 7.52 |
| CHEMBL5557312 | — | — | 1 | 7.19 |
| CHEMBL5558492 | — | — | 1 | 6.79 |
| CHEMBL5555131 | — | — | 1 | 6.40 |
| CHEMBL5556474 | — | — | 1 | 6.37 |
| CHEMBL5532251 | — | — | 1 | 6.33 |
| CHEMBL5557952 | — | — | 1 | 6.28 |
| CHEMBL5517704 | — | — | 1 | 6.14 |
| CHEMBL5532599 | — | — | 1 | 6.12 |
| CHEMBL5555332 | — | — | 1 | 6.04 |
| CHEMBL5542859 | — | — | 1 | 6.00 |
| CHEMBL5556994 | — | — | 1 | 5.75 |
| CHEMBL5559422 | — | — | 1 | 5.73 |
| CHEMBL5505916 | — | — | 1 | 5.72 |
| CHEMBL5557601 | — | — | 1 | 5.68 |
| CHEMBL502 | DONEPEZIL | 4.0 | 1 | 5.64 |
| CHEMBL5532253 | — | — | 1 | 5.58 |
| CHEMBL5532065 | — | — | 1 | 5.31 |
| CHEMBL5517644 | — | — | 1 | 5.26 |
| CHEMBL5512595 | — | — | 1 | 5.24 |
| CHEMBL5542336 | — | — | 1 | 5.18 |
| CHEMBL5532475 | — | — | 1 | 5.00 |
| CHEMBL5512467 | — | — | 1 | 5.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL95 | TACRINE | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL5557312 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL5558492 | — | IC50 | = | 163.0 | nM | 6.79 |
| CHEMBL5555131 | — | IC50 | = | 396.0 | nM | 6.40 |
| CHEMBL5556474 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL5532251 | — | IC50 | = | 466.0 | nM | 6.33 |
| CHEMBL5557952 | — | IC50 | = | 528.0 | nM | 6.28 |
| CHEMBL5517704 | — | IC50 | = | 717.0 | nM | 6.14 |
| CHEMBL5532599 | — | IC50 | = | 765.0 | nM | 6.12 |
| CHEMBL5555332 | — | IC50 | = | 906.0 | nM | 6.04 |
| CHEMBL5542859 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL5556994 | — | IC50 | = | 1780.0 | nM | 5.75 |
| CHEMBL5559422 | — | IC50 | = | 1860.0 | nM | 5.73 |
| CHEMBL5505916 | — | IC50 | = | 1920.0 | nM | 5.72 |
| CHEMBL5557601 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL502 | DONEPEZIL | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL5532253 | — | IC50 | = | 2640.0 | nM | 5.58 |
| CHEMBL5532065 | — | IC50 | = | 4920.0 | nM | 5.31 |
| CHEMBL5517644 | — | IC50 | = | 5520.0 | nM | 5.26 |
| CHEMBL5512595 | — | IC50 | = | 5790.0 | nM | 5.24 |
| CHEMBL5542336 | — | IC50 | = | 6590.0 | nM | 5.18 |
| CHEMBL5532475 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL5512467 | — | IC50 | = | 10000.0 | nM | 5.00 |