Assay Detail
Binding
CHEMBL4376473
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Displacement of [3H]-N-alpha-methylhistamine from human histamine H3 receptor stably expressed in HEK293 cell membrane after 90 mins
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Search for new multi-target compounds against Alzheimer's disease among histamine H3 receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 6.95 | 7.93 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL462605 | PITOLISANT | 4.0 | 1 | 7.93 |
| CHEMBL4475205 | — | — | 1 | 7.22 |
| CHEMBL4529681 | — | — | 1 | 7.07 |
| CHEMBL4455690 | — | — | 1 | 6.80 |
| CHEMBL4454949 | — | — | 1 | 6.74 |
| CHEMBL4474399 | — | — | 1 | 6.64 |
| CHEMBL4560469 | — | — | 1 | 6.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL462605 | PITOLISANT | Ki | = | 11.7 | nM | 7.93 |
| CHEMBL4475205 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL4529681 | — | Ki | = | 84.3 | nM | 7.07 |
| CHEMBL4455690 | — | Ki | = | 159.8 | nM | 6.80 |
| CHEMBL4454949 | — | Ki | = | 181.5 | nM | 6.74 |
| CHEMBL4474399 | — | Ki | = | 228.2 | nM | 6.64 |
| CHEMBL4560469 | — | Ki | = | 522.8 | nM | 6.28 |