Assay Detail
Binding
CHEMBL4003411
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured for 60 to 300 secs by Ellman's method
36
Total Activities
36
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
2,4-Disubstituted quinazolines as amyloid-β aggregation inhibitors with dual cholinesterase inhibition and antioxidant properties: Development and structure-activity relationship (SAR) studies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 36 | 5.25 | 7.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2337271 | DONEPEZIL HYDROCHLORIDE MONOHYDRATE | — | 1 | 7.52 |
| CHEMBL1677 | TACRINE HYDROCHLORIDE | 4.0 | 1 | 6.80 |
| CHEMBL1555 | GALANTAMINE HYDROBROMIDE | 4.0 | 1 | 5.58 |
| CHEMBL4083524 | — | — | 1 | 5.25 |
| CHEMBL4077088 | — | — | 1 | 5.20 |
| CHEMBL1201092 | RIVASTIGMINE TARTRATE | 4.0 | 1 | 5.19 |
| CHEMBL3262251 | — | — | 1 | 5.19 |
| CHEMBL4067481 | — | — | 1 | 5.18 |
| CHEMBL4099790 | — | — | 1 | 5.17 |
| CHEMBL4085114 | — | — | 1 | 5.16 |
| CHEMBL4102655 | — | — | 1 | 5.16 |
| CHEMBL4070462 | — | — | 1 | 5.14 |
| CHEMBL4097374 | — | — | 1 | 5.14 |
| CHEMBL4086248 | — | — | 1 | 5.14 |
| CHEMBL4073193 | — | — | 1 | 5.14 |
| CHEMBL4069444 | — | — | 1 | 5.14 |
| CHEMBL4098421 | — | — | 1 | 5.14 |
| CHEMBL4083601 | — | — | 1 | 5.14 |
| CHEMBL4100046 | — | — | 1 | 5.13 |
| CHEMBL4060016 | — | — | 1 | 5.13 |
| CHEMBL4061837 | — | — | 1 | 5.12 |
| CHEMBL4095445 | — | — | 1 | 5.12 |
| CHEMBL4061746 | — | — | 1 | 5.12 |
| CHEMBL4078382 | — | — | 1 | 5.12 |
| CHEMBL4079345 | — | — | 1 | 5.12 |
| CHEMBL4105088 | — | — | 1 | 5.11 |
| CHEMBL1626455 | — | — | 1 | 5.10 |
| CHEMBL4070380 | — | — | 1 | 5.10 |
| CHEMBL4081013 | — | — | 1 | 5.08 |
| CHEMBL4094911 | — | — | 1 | 5.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2337271 | DONEPEZIL HYDROCHLORIDE MONOHYDRATE | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL1677 | TACRINE HYDROCHLORIDE | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL1555 | GALANTAMINE HYDROBROMIDE | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL4083524 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL4077088 | — | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL1201092 | RIVASTIGMINE TARTRATE | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL3262251 | — | IC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL4067481 | — | IC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL4099790 | — | IC50 | = | 6800.0 | nM | 5.17 |
| CHEMBL4102655 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL4085114 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL4083601 | — | IC50 | = | 7200.0 | nM | 5.14 |
| CHEMBL4098421 | — | IC50 | = | 7300.0 | nM | 5.14 |
| CHEMBL4069444 | — | IC50 | = | 7300.0 | nM | 5.14 |
| CHEMBL4073193 | — | IC50 | = | 7200.0 | nM | 5.14 |
| CHEMBL4070462 | — | IC50 | = | 7200.0 | nM | 5.14 |
| CHEMBL4086248 | — | IC50 | = | 7200.0 | nM | 5.14 |
| CHEMBL4097374 | — | IC50 | = | 7200.0 | nM | 5.14 |
| CHEMBL4100046 | — | IC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL4060016 | — | IC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL4061837 | — | IC50 | = | 7600.0 | nM | 5.12 |
| CHEMBL4095445 | — | IC50 | = | 7600.0 | nM | 5.12 |
| CHEMBL4061746 | — | IC50 | = | 7500.0 | nM | 5.12 |
| CHEMBL4078382 | — | IC50 | = | 7500.0 | nM | 5.12 |
| CHEMBL4079345 | — | IC50 | = | 7500.0 | nM | 5.12 |
| CHEMBL4105088 | — | IC50 | = | 7800.0 | nM | 5.11 |
| CHEMBL4070380 | — | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL1626455 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL4081013 | — | IC50 | = | 8300.0 | nM | 5.08 |
| CHEMBL4094911 | — | IC50 | = | 8500.0 | nM | 5.07 |
| CHEMBL4091385 | — | IC50 | = | 8600.0 | nM | 5.07 |
| CHEMBL4060687 | — | IC50 | = | 8600.0 | nM | 5.07 |
| CHEMBL4091317 | — | IC50 | = | 8500.0 | nM | 5.07 |
| CHEMBL4064773 | — | IC50 | = | 8700.0 | nM | 5.06 |
| CHEMBL4099046 | — | IC50 | = | 8700.0 | nM | 5.06 |
| CHEMBL4096673 | — | IC50 | = | 12500.0 | nM | 4.90 |