Assay Detail
Binding
CHEMBL5032903
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H] N-alpha methylhistamine from human recombinant histamine H3 receptor expressed in HEK293 cells measured after 90 mins
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
Adenosine A<sub>2A</sub>R/A<sub>1</sub>R Antagonists Enabling Additional H<sub>3</sub>R Antagonism for the Treatment of Parkinson's Disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 8.22 | 9.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5089580 | — | — | 1 | 9.55 |
| CHEMBL5093850 | — | — | 1 | 9.51 |
| CHEMBL5072724 | — | — | 1 | 9.31 |
| CHEMBL5093935 | — | — | 1 | 9.22 |
| CHEMBL5094415 | — | — | 1 | 8.64 |
| CHEMBL5084903 | — | — | 1 | 8.35 |
| CHEMBL5094263 | — | — | 1 | 7.96 |
| CHEMBL5088622 | — | — | 1 | 7.96 |
| CHEMBL2297871 | — | — | 1 | 7.96 |
| CHEMBL5082920 | — | — | 1 | 7.77 |
| CHEMBL5081556 | — | — | 1 | 7.51 |
| CHEMBL5087059 | — | — | 1 | 7.44 |
| CHEMBL5082650 | — | — | 1 | 7.28 |
| CHEMBL14638 | CIPROXIFAN | — | 1 | 6.65 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5089580 | — | Ki | = | 0.28 | nM | 9.55 |
| CHEMBL5093850 | — | Ki | = | 0.31 | nM | 9.51 |
| CHEMBL5072724 | — | Ki | = | 0.49 | nM | 9.31 |
| CHEMBL5093935 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL5094415 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL5084903 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL5094263 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL5088622 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL2297871 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL5082920 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL5081556 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL5087059 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL5082650 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL14638 | CIPROXIFAN | Ki | = | 224.0 | nM | 6.65 |