Assay Detail
Functional
CHEMBL973689
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Antagonist activity at histamine H3 receptor in guinea pig ileum assessed as inhibition of (R)-alpha-methylhistamine-induced response
5
Total Activities
5
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Cavia porcellus |
| Tissue | Ileum |
| 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 |
|---|---|---|---|
| IC50 | 2 | 6.19 | 6.30 |
| Kd | 2 | 7.50 | 8.44 |
| pKb | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL260374 | THIOPERAMIDE | — | 1 | 8.44 |
| CHEMBL191703 | CONESSINE | 2.0 | 1 | 6.55 |
| CHEMBL380697 | APLYSAMINE | — | 1 | 6.30 |
| CHEMBL15075 | VERONGAMINE | — | 1 | 6.08 |
| CHEMBL14638 | CIPROXIFAN | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL260374 | THIOPERAMIDE | Kd | = | 3.631 | nM | 8.44 |
| CHEMBL191703 | CONESSINE | Kd | = | 281.84 | nM | 6.55 |
| CHEMBL380697 | APLYSAMINE | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL15075 | VERONGAMINE | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL14638 | CIPROXIFAN | pKb | = | 8.12 | — | - |