Assay Detail
Binding
CHEMBL5151457
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]Nalpha-methylhistamine from human histamine H3 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis
23
Total Activities
12
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Abolishing Dopamine D<sub>2long</sub>/D<sub>3</sub> Receptor Affinity of Subtype-Selective Carbamoylguanidine-Type Histamine H<sub>2</sub> Receptor Agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 5.38 | 7.59 |
| Kd | 11 | 8.52 | 8.52 |
| pKi | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL90 | HISTAMINE | 4.0 | 2 | 8.52 |
| CHEMBL5209081 | — | — | 2 | 8.52 |
| CHEMBL5207206 | — | — | 2 | 8.52 |
| CHEMBL5170276 | — | — | 2 | 8.52 |
| CHEMBL5209479 | — | — | 2 | 8.52 |
| CHEMBL5209021 | — | — | 2 | 8.52 |
| CHEMBL5184846 | — | — | 2 | 8.52 |
| CHEMBL5174342 | — | — | 2 | 8.52 |
| CHEMBL5208113 | — | — | 2 | 8.52 |
| CHEMBL5192993 | — | — | 2 | 8.52 |
| CHEMBL5194860 | — | — | 2 | 8.52 |
| CHEMBL301265 | PRAMIPEXOLE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5192993 | — | Kd | = | 3.0 | nM | 8.52 |
| CHEMBL5208113 | — | Kd | = | 3.0 | nM | 8.52 |
| CHEMBL5174342 | — | Kd | = | 3.0 | nM | 8.52 |
| CHEMBL5184846 | — | Kd | = | 3.0 | nM | 8.52 |
| CHEMBL5209021 | — | Kd | = | 3.0 | nM | 8.52 |
| CHEMBL5209479 | — | Kd | = | 3.0 | nM | 8.52 |
| CHEMBL5170276 | — | Kd | = | 3.0 | nM | 8.52 |
| CHEMBL5207206 | — | Kd | = | 3.0 | nM | 8.52 |
| CHEMBL5209081 | — | Kd | = | 3.0 | nM | 8.52 |
| CHEMBL90 | HISTAMINE | Kd | = | 3.0 | nM | 8.52 |
| CHEMBL5194860 | — | Kd | = | 3.0 | nM | 8.52 |
| CHEMBL90 | HISTAMINE | Ki | = | 25.7 | nM | 7.59 |
| CHEMBL5194860 | — | Ki | = | 1737.8 | nM | 5.76 |
| CHEMBL5208113 | — | Ki | = | 1949.84 | nM | 5.71 |
| CHEMBL5207206 | — | Ki | = | 6606.93 | nM | 5.18 |
| CHEMBL5192993 | — | Ki | = | 7943.28 | nM | 5.10 |
| CHEMBL5174342 | — | Ki | = | 8317.64 | nM | 5.08 |
| CHEMBL5209021 | — | Ki | = | 8511.38 | nM | 5.07 |
| CHEMBL5184846 | — | Ki | = | 11220.18 | nM | 4.95 |
| CHEMBL5209479 | — | Ki | = | 11481.54 | nM | 4.94 |
| CHEMBL5209081 | — | Ki | = | 11481.54 | nM | 4.94 |
| CHEMBL5170276 | — | Ki | = | 12302.69 | nM | 4.91 |
| CHEMBL301265 | PRAMIPEXOLE | pKi | - | — | - |