Assay Detail
Functional
CHEMBL5057269
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Antagonist activity at histamine H3 receptor (unknown origin)
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Histamine H<sub>3</sub> receptor antagonists with peptidomimetic (keto)piperazine structures to inhibit Aβ oligomerisation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 2 | 8.65 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4527011 | — | — | 1 | 8.70 |
| CHEMBL462605 | PITOLISANT | 4.0 | 1 | 8.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4527011 | — | Ki | = | 1.995 | nM | 8.70 |
| CHEMBL462605 | PITOLISANT | Ki | = | 2.512 | nM | 8.60 |