Assay Detail
Binding
CHEMBL4433438
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human H3R expressed in methylhistamine-induced human H3-bla U2OS cells incubated for 30 mins by beta-lactamase complementation technology
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | U2OS |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, synthesis, and evaluation of isoflavone analogs as multifunctional agents for the treatment of Alzheimer's disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 6.14 | 6.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4568293 | — | — | 1 | 6.57 |
| CHEMBL4552051 | — | — | 1 | 6.39 |
| CHEMBL4554976 | — | — | 1 | 6.37 |
| CHEMBL4516496 | — | — | 1 | 6.28 |
| CHEMBL4439461 | — | — | 1 | 6.14 |
| CHEMBL260374 | THIOPERAMIDE | — | 1 | 5.99 |
| CHEMBL4554072 | — | — | 1 | 5.71 |
| CHEMBL4586884 | — | — | 1 | 5.68 |
| CHEMBL4471251 | — | — | 1 | - |
| CHEMBL4476554 | — | — | 1 | - |
| CHEMBL4450260 | — | — | 1 | - |
| CHEMBL4445115 | — | — | 1 | - |
| CHEMBL4583406 | — | — | 1 | - |
| CHEMBL4438929 | — | — | 1 | - |
| CHEMBL4555824 | — | — | 1 | - |
| CHEMBL4543223 | — | — | 1 | - |
| CHEMBL502 | DONEPEZIL | 4.0 | 1 | - |
| CHEMBL636 | RIVASTIGMINE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4568293 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4552051 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL4554976 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL4516496 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL4439461 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL260374 | THIOPERAMIDE | IC50 | = | 1030.0 | nM | 5.99 |
| CHEMBL4554072 | — | IC50 | = | 1940.0 | nM | 5.71 |
| CHEMBL4586884 | — | IC50 | = | 2070.0 | nM | 5.68 |
| CHEMBL4471251 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4476554 | — | IC50 | - | — | - | |
| CHEMBL4450260 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4445115 | — | IC50 | - | — | - | |
| CHEMBL4583406 | — | IC50 | - | — | - | |
| CHEMBL4438929 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4555824 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4543223 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL502 | DONEPEZIL | IC50 | - | — | - | |
| CHEMBL636 | RIVASTIGMINE | IC50 | - | — | - |