Assay Detail
Binding
CHEMBL4433405
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human BACE1 using as 7-Methoxycoumarin-4-acetyl-[Asn670, Leu671]-Amyloid beta/A4 precursor protein 770 fragment 667-676-(2,4-dinitrophenyl) Lys-Arg-Arg amide trifluoroacetate salt as substrate incubated for 2 hrs by FRET based florescence assay
31
Total Activities
31
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
Design and development of multitarget-directed N-Benzylpiperidine analogs as potential candidates for the treatment of Alzheimer's disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 5.58 | 6.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4583534 | — | — | 1 | 6.66 |
| CHEMBL502 | DONEPEZIL | 4.0 | 1 | 6.62 |
| CHEMBL4575167 | — | — | 1 | 6.55 |
| CHEMBL4442580 | — | — | 1 | 6.37 |
| CHEMBL1424080 | — | — | 1 | 6.26 |
| CHEMBL1348834 | — | — | 1 | 6.18 |
| CHEMBL4452092 | — | — | 1 | 6.14 |
| CHEMBL4587156 | — | — | 1 | 5.85 |
| CHEMBL4518938 | — | — | 1 | 5.82 |
| CHEMBL4526950 | — | — | 1 | 5.77 |
| CHEMBL4449445 | — | — | 1 | 5.75 |
| CHEMBL4447514 | — | — | 1 | 5.70 |
| CHEMBL4458653 | — | — | 1 | 5.58 |
| CHEMBL4467620 | — | — | 1 | 5.57 |
| CHEMBL4453051 | — | — | 1 | 5.54 |
| CHEMBL4443695 | — | — | 1 | 5.54 |
| CHEMBL4091169 | — | — | 1 | 5.52 |
| CHEMBL4566242 | — | — | 1 | 5.48 |
| CHEMBL4537808 | — | — | 1 | 5.47 |
| CHEMBL4568615 | — | — | 1 | 5.46 |
| CHEMBL4568264 | — | — | 1 | 5.41 |
| CHEMBL4435826 | — | — | 1 | 5.28 |
| CHEMBL4443013 | — | — | 1 | 5.23 |
| CHEMBL4444849 | — | — | 1 | 5.20 |
| CHEMBL4561792 | — | — | 1 | 5.00 |
| CHEMBL4556855 | — | — | 1 | 5.00 |
| CHEMBL4454571 | — | — | 1 | 4.92 |
| CHEMBL4591283 | — | — | 1 | 4.89 |
| CHEMBL4440283 | — | — | 1 | 4.85 |
| CHEMBL4444968 | — | — | 1 | 4.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4583534 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL502 | DONEPEZIL | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL4575167 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL4442580 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL1424080 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL1348834 | — | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL4452092 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL4587156 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL4518938 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4526950 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4449445 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL4447514 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL4458653 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL4467620 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL4453051 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL4443695 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL4091169 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL4566242 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL4537808 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL4568615 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL4568264 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL4435826 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL4443013 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL4444849 | — | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL4561792 | — | IC50 | = | 9900.0 | nM | 5.00 |
| CHEMBL4556855 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4454571 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL4591283 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL4440283 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL4444968 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL4566555 | — | IC50 | = | 19000.0 | nM | 4.72 |