Assay Detail
Binding
CHEMBL3772143
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human BuChE using S-butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured after 60 to 300 sec by Ellman's method
32
Total Activities
32
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
Tricyclic phenothiazine and phenoselenazine derivatives as potential multi-targeting agents to treat Alzheimer's disease
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 32 | 4.99 | 7.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL95 | TACRINE | 4.0 | 1 | 7.40 |
| CHEMBL3769834 | — | — | 1 | 5.52 |
| CHEMBL502 | DONEPEZIL | 4.0 | 1 | 5.44 |
| CHEMBL3770516 | — | — | 1 | 5.44 |
| CHEMBL3770479 | — | — | 1 | 5.42 |
| CHEMBL51085 | EBSELEN | 3.0 | 1 | 5.34 |
| CHEMBL3769862 | — | — | 1 | 5.33 |
| CHEMBL3770203 | — | — | 1 | 5.31 |
| CHEMBL3770803 | — | — | 1 | 5.30 |
| CHEMBL3770866 | — | — | 1 | 5.30 |
| CHEMBL1801816 | — | — | 1 | 5.28 |
| CHEMBL828 | PHENOTHIAZINE | 2.0 | 1 | 5.24 |
| CHEMBL3769555 | — | — | 1 | 5.24 |
| CHEMBL3770978 | — | — | 1 | 5.04 |
| CHEMBL1801815 | — | — | 1 | 5.03 |
| CHEMBL3769833 | — | — | 1 | 5.02 |
| CHEMBL3769576 | — | — | 1 | 4.96 |
| CHEMBL3769811 | — | — | 1 | 4.96 |
| CHEMBL1411769 | — | — | 1 | 4.72 |
| CHEMBL3769537 | — | — | 1 | 4.71 |
| CHEMBL3770569 | — | — | 1 | 4.64 |
| CHEMBL1327885 | — | — | 1 | 4.59 |
| CHEMBL3770206 | — | — | 1 | 4.51 |
| CHEMBL3770071 | — | — | 1 | 4.49 |
| CHEMBL3771233 | — | — | 1 | 4.42 |
| CHEMBL394753 | — | — | 1 | 4.42 |
| CHEMBL3770577 | — | — | 1 | 4.40 |
| CHEMBL3770356 | — | — | 1 | 4.35 |
| CHEMBL240047 | — | — | 1 | 4.29 |
| CHEMBL239618 | — | — | 1 | 4.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL95 | TACRINE | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3769834 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL502 | DONEPEZIL | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL3770516 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL3770479 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL51085 | EBSELEN | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL3769862 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL3770203 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL3770803 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL3770866 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL1801816 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL828 | PHENOTHIAZINE | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL3769555 | — | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL3770978 | — | IC50 | = | 9100.0 | nM | 5.04 |
| CHEMBL1801815 | — | IC50 | = | 9300.0 | nM | 5.03 |
| CHEMBL3769833 | — | IC50 | = | 9600.0 | nM | 5.02 |
| CHEMBL3769576 | — | IC50 | = | 11100.0 | nM | 4.96 |
| CHEMBL3769811 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL1411769 | — | IC50 | = | 19200.0 | nM | 4.72 |
| CHEMBL3769537 | — | IC50 | = | 19300.0 | nM | 4.71 |
| CHEMBL3770569 | — | IC50 | = | 22700.0 | nM | 4.64 |
| CHEMBL1327885 | — | IC50 | = | 25500.0 | nM | 4.59 |
| CHEMBL3770206 | — | IC50 | = | 30800.0 | nM | 4.51 |
| CHEMBL3770071 | — | IC50 | = | 32600.0 | nM | 4.49 |
| CHEMBL3771233 | — | IC50 | = | 38000.0 | nM | 4.42 |
| CHEMBL394753 | — | IC50 | = | 38300.0 | nM | 4.42 |
| CHEMBL3770577 | — | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL3770356 | — | IC50 | = | 45000.0 | nM | 4.35 |
| CHEMBL240047 | — | IC50 | = | 51000.0 | nM | 4.29 |
| CHEMBL239618 | — | IC50 | = | 53000.0 | nM | 4.28 |
| CHEMBL659 | GALANTAMINE | IC50 | = | 66500.0 | nM | 4.18 |
| CHEMBL239400 | — | IC50 | > | 100000.0 | nM | - |