Assay Detail
Binding
CHEMBL4273241
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Inhibition of recombinant human AChE expressed in HEK293 cells using acetylthiocholine iodide as substrate pretreated for 5 mins followed by substrate addition and measured for 5 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 |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Neurogenic and neuroprotective donepezil-flavonoid hybrids with sigma-1 affinity and inhibition of key enzymes in Alzheimer's disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 6.52 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL502 | DONEPEZIL | 4.0 | 1 | 8.00 |
| CHEMBL4277548 | — | — | 1 | 7.68 |
| CHEMBL4284165 | — | — | 1 | 7.64 |
| CHEMBL4285779 | — | — | 1 | 7.48 |
| CHEMBL4292477 | — | — | 1 | 7.39 |
| CHEMBL4287970 | — | — | 1 | 7.34 |
| CHEMBL4284495 | — | — | 1 | 7.25 |
| CHEMBL4291296 | — | — | 1 | 7.04 |
| CHEMBL4286799 | — | — | 1 | 6.96 |
| CHEMBL4294783 | — | — | 1 | 6.96 |
| CHEMBL4283450 | — | — | 1 | 6.77 |
| CHEMBL4293801 | — | — | 1 | 6.77 |
| CHEMBL4285601 | — | — | 1 | 6.52 |
| CHEMBL4294609 | — | — | 1 | 6.52 |
| CHEMBL4284591 | — | — | 1 | 6.50 |
| CHEMBL4291372 | — | — | 1 | 6.43 |
| CHEMBL4282527 | — | — | 1 | 6.35 |
| CHEMBL4277332 | — | — | 1 | 6.24 |
| CHEMBL4289318 | — | — | 1 | 6.21 |
| CHEMBL4292446 | — | — | 1 | 6.18 |
| CHEMBL4294701 | — | — | 1 | 6.06 |
| CHEMBL4287548 | — | — | 1 | 6.06 |
| CHEMBL4290940 | — | — | 1 | 6.01 |
| CHEMBL4285912 | — | — | 1 | 5.94 |
| CHEMBL4295144 | — | — | 1 | 5.84 |
| CHEMBL4290401 | — | — | 1 | 5.79 |
| CHEMBL4283079 | — | — | 1 | 5.63 |
| CHEMBL4287889 | — | — | 1 | 5.44 |
| CHEMBL4280725 | — | — | 1 | 5.38 |
| CHEMBL4286731 | — | — | 1 | 5.13 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL502 | DONEPEZIL | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4277548 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4284165 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4285779 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4292477 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL4287970 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL4284495 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL4291296 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL4286799 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4294783 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4283450 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4293801 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4285601 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4294609 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4284591 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL4291372 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL4282527 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL4277332 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL4289318 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL4292446 | — | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL4294701 | — | IC50 | = | 870.0 | nM | 6.06 |
| CHEMBL4287548 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL4290940 | — | IC50 | = | 970.0 | nM | 6.01 |
| CHEMBL4285912 | — | IC50 | = | 1150.0 | nM | 5.94 |
| CHEMBL4295144 | — | IC50 | = | 1460.0 | nM | 5.84 |
| CHEMBL4290401 | — | IC50 | = | 1640.0 | nM | 5.79 |
| CHEMBL4283079 | — | IC50 | = | 2360.0 | nM | 5.63 |
| CHEMBL4287889 | — | IC50 | = | 3610.0 | nM | 5.44 |
| CHEMBL4280725 | — | IC50 | = | 4130.0 | nM | 5.38 |
| CHEMBL4286731 | — | IC50 | = | 7490.0 | nM | 5.13 |