Assay Detail
Binding
CHEMBL3129496
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant MAO-A using tyramine as substrate preincubated for 30 mins followed by substrate addition measured for 1 hr by fluorometric assay
21
Total Activities
16
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, synthesis, pharmacological evaluation, QSAR analysis, molecular modeling and ADMET of novel donepezil-indolyl hybrids as multipotent cholinesterase/monoamine oxidase inhibitors for the potential treatment of Alzheimer's disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 5.95 | 8.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1929421 | — | — | 1 | 8.38 |
| CHEMBL3127967 | — | — | 2 | 8.26 |
| CHEMBL3127968 | — | — | 2 | 6.01 |
| CHEMBL3127970 | — | — | 1 | 5.82 |
| CHEMBL3127976 | — | — | 1 | 5.37 |
| CHEMBL3127966 | — | — | 1 | 5.36 |
| CHEMBL3127978 | — | — | 2 | 4.00 |
| CHEMBL3127977 | — | — | 2 | 4.00 |
| CHEMBL3124971 | — | — | 2 | 4.00 |
| CHEMBL3127975 | — | — | 1 | - |
| CHEMBL3127974 | — | — | 1 | - |
| CHEMBL3127973 | — | — | 1 | - |
| CHEMBL3127972 | — | — | 1 | - |
| CHEMBL3127971 | — | — | 1 | - |
| CHEMBL3127969 | — | — | 1 | - |
| CHEMBL502 | DONEPEZIL | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1929421 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL3127967 | — | IC50 | = | 5.495 | nM | 8.26 |
| CHEMBL3127967 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL3127968 | — | IC50 | = | 980.0 | nM | 6.01 |
| CHEMBL3127968 | — | IC50 | = | 979.49 | nM | 6.01 |
| CHEMBL3127970 | — | IC50 | = | 1530.0 | nM | 5.82 |
| CHEMBL3127976 | — | IC50 | = | 4260.0 | nM | 5.37 |
| CHEMBL3127966 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL3127978 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL3127977 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL3124971 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL3127977 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3127974 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3127975 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3127978 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL502 | DONEPEZIL | IC50 | = | 850000.0 | nM | - |
| CHEMBL3127969 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3124971 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3127971 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3127972 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3127973 | — | IC50 | > | 100000.0 | nM | - |