Assay Detail
Binding
CHEMBL4821429
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human BACE1 expressed in baculovirus expression system using Rh-EVNLDAEFK-quencher as substrate incubated for 60 mins by FRET assay
19
Total Activities
19
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
Discovery of multifunctional anti-Alzheimer's agents with a unique mechanism of action including inhibition of the enzyme butyrylcholinesterase and γ-aminobutyric acid transporters.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 5.14 | 7.34 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL378225 | — | — | 1 | 7.34 |
| CHEMBL4857933 | — | — | 1 | 5.68 |
| CHEMBL4868077 | — | — | 1 | 5.47 |
| CHEMBL4876288 | — | — | 1 | 5.34 |
| CHEMBL4874266 | — | — | 1 | 5.23 |
| CHEMBL4858894 | — | — | 1 | 5.22 |
| CHEMBL4851448 | — | — | 1 | 5.21 |
| CHEMBL4861746 | — | — | 1 | 5.18 |
| CHEMBL4877574 | — | — | 1 | 5.08 |
| CHEMBL4856694 | — | — | 1 | 5.07 |
| CHEMBL4873410 | — | — | 1 | 5.05 |
| CHEMBL4857355 | — | — | 1 | 4.81 |
| CHEMBL4845832 | — | — | 1 | 4.76 |
| CHEMBL4847981 | — | — | 1 | 4.63 |
| CHEMBL4860617 | — | — | 1 | 4.47 |
| CHEMBL4869613 | — | — | 1 | 4.45 |
| CHEMBL4860825 | — | — | 1 | 4.38 |
| CHEMBL502 | DONEPEZIL | 4.0 | 1 | - |
| CHEMBL95 | TACRINE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL378225 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL4857933 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL4868077 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL4876288 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL4874266 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL4858894 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL4851448 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL4861746 | — | IC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL4877574 | — | IC50 | = | 8300.0 | nM | 5.08 |
| CHEMBL4856694 | — | IC50 | = | 8600.0 | nM | 5.07 |
| CHEMBL4873410 | — | IC50 | = | 8900.0 | nM | 5.05 |
| CHEMBL4857355 | — | IC50 | = | 15400.0 | nM | 4.81 |
| CHEMBL4845832 | — | IC50 | = | 17400.0 | nM | 4.76 |
| CHEMBL4847981 | — | IC50 | = | 23400.0 | nM | 4.63 |
| CHEMBL4860617 | — | IC50 | = | 33600.0 | nM | 4.47 |
| CHEMBL4869613 | — | IC50 | = | 35400.0 | nM | 4.45 |
| CHEMBL4860825 | — | IC50 | = | 41600.0 | nM | 4.38 |
| CHEMBL502 | DONEPEZIL | IC50 | - | — | - | |
| CHEMBL95 | TACRINE | IC50 | - | — | - |