Assay Detail
Binding
CHEMBL4329059
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Displacement of [3H]-N-alpha-methylhistamine from human H3 receptor expressed in CHO-K1 cell membranes after 60 mins by microbeta2 scintillation counting analysis
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
4-tert-Pentylphenoxyalkyl derivatives - Histamine H<sub>3</sub> receptor ligands and monoamine oxidase B inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 6.79 | 7.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4173079 | — | — | 1 | 7.43 |
| CHEMBL4561401 | — | — | 1 | 7.20 |
| CHEMBL4560631 | — | — | 1 | 7.00 |
| CHEMBL4449671 | — | — | 1 | 6.85 |
| CHEMBL4473751 | — | — | 1 | 6.83 |
| CHEMBL4522715 | — | — | 1 | 6.53 |
| CHEMBL4435585 | — | — | 1 | 6.36 |
| CHEMBL4530407 | — | — | 1 | 6.12 |
| CHEMBL4557594 | — | — | 1 | - |
| CHEMBL887 | RASAGILINE | 4.0 | 1 | - |
| CHEMBL396778 | SAFINAMIDE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4173079 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL4561401 | — | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL4560631 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL4449671 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL4473751 | — | Ki | = | 147.0 | nM | 6.83 |
| CHEMBL4522715 | — | Ki | = | 298.0 | nM | 6.53 |
| CHEMBL4435585 | — | Ki | = | 437.0 | nM | 6.36 |
| CHEMBL4530407 | — | Ki | = | 753.0 | nM | 6.12 |
| CHEMBL4557594 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL887 | RASAGILINE | Ki | - | — | - | |
| CHEMBL396778 | SAFINAMIDE | Ki | - | — | - |