Assay Detail
Binding
CHEMBL973671
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Displacement of [3H]NAMH from rat full length histamine H3 receptor expressed in rat C6 cells
8
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | C6 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
The alkaloid conessine and analogues as potent histamine H3 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 7.81 | 9.29 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL14638 | CIPROXIFAN | — | 1 | 9.29 |
| CHEMBL451821 | — | — | 1 | 8.59 |
| CHEMBL260374 | THIOPERAMIDE | — | 1 | 8.44 |
| CHEMBL488891 | — | — | 1 | 8.10 |
| CHEMBL191703 | CONESSINE | 2.0 | 2 | 7.91 |
| CHEMBL461024 | CARCININE | — | 1 | 6.53 |
| CHEMBL519889 | — | — | 1 | 6.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL14638 | CIPROXIFAN | Ki | = | 0.5129 | nM | 9.29 |
| CHEMBL451821 | — | Ki | = | 2.57 | nM | 8.59 |
| CHEMBL260374 | THIOPERAMIDE | Ki | = | 3.631 | nM | 8.44 |
| CHEMBL488891 | — | Ki | = | 7.91 | nM | 8.10 |
| CHEMBL191703 | CONESSINE | Ki | = | 12.3 | nM | 7.91 |
| CHEMBL191703 | CONESSINE | Ki | = | 24.5 | nM | 7.61 |
| CHEMBL461024 | CARCININE | Ki | = | 294.0 | nM | 6.53 |
| CHEMBL519889 | — | Ki | = | 1000.0 | nM | 6.00 |