Assay Detail
Binding
CHEMBL4433277
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Displacement of [3H]-N-alpha-methylhistamine from human recombinant full length H3R expressed in HEK293 cell membranes incubated for 90 mins by liquid scintillation counting method
14
Total Activities
14
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
Biphenyloxy-alkyl-piperidine and azepane derivatives as histamine H<sub>3</sub> receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 7.12 | 7.93 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL462605 | PITOLISANT | 4.0 | 1 | 7.93 |
| CHEMBL4445028 | — | — | 1 | 7.75 |
| CHEMBL4540849 | — | — | 1 | 7.60 |
| CHEMBL4586133 | — | — | 1 | 7.47 |
| CHEMBL4585724 | — | — | 1 | 7.12 |
| CHEMBL4450520 | — | — | 1 | 7.05 |
| CHEMBL4469232 | — | — | 1 | 7.04 |
| CHEMBL4437238 | — | — | 1 | 6.94 |
| CHEMBL4514837 | — | — | 1 | 6.91 |
| CHEMBL4159018 | — | — | 1 | 6.88 |
| CHEMBL4552629 | — | — | 1 | 6.82 |
| CHEMBL4465338 | — | — | 1 | 6.80 |
| CHEMBL4553559 | — | — | 1 | 6.80 |
| CHEMBL4467138 | — | — | 1 | 6.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL462605 | PITOLISANT | Ki | = | 11.7 | nM | 7.93 |
| CHEMBL4445028 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL4540849 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL4586133 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL4585724 | — | Ki | = | 76.0 | nM | 7.12 |
| CHEMBL4450520 | — | Ki | = | 89.0 | nM | 7.05 |
| CHEMBL4469232 | — | Ki | = | 92.0 | nM | 7.04 |
| CHEMBL4437238 | — | Ki | = | 115.0 | nM | 6.94 |
| CHEMBL4514837 | — | Ki | = | 122.0 | nM | 6.91 |
| CHEMBL4159018 | — | Ki | = | 131.0 | nM | 6.88 |
| CHEMBL4552629 | — | Ki | = | 151.0 | nM | 6.82 |
| CHEMBL4465338 | — | Ki | = | 159.0 | nM | 6.80 |
| CHEMBL4553559 | — | Ki | = | 157.0 | nM | 6.80 |
| CHEMBL4467138 | — | Ki | = | 266.0 | nM | 6.58 |