Assay Detail
Binding
CHEMBL3097147
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-R-alpha-ethylhistamine from human histamine H3 receptor expressed in HEK293 cells after 45 mins by liquid scintillation spectrometry
3
Total Activities
3
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
Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 3 | 9.77 | 9.90 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL517140 | GSK189254 | 2.0 | 1 | 9.90 |
| CHEMBL1783890 | — | — | 1 | 9.72 |
| CHEMBL3092650 | GSK239512 | 2.0 | 1 | 9.69 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL517140 | GSK189254 | Ki | = | 0.1259 | nM | 9.90 |
| CHEMBL1783890 | — | Ki | = | 0.1905 | nM | 9.72 |
| CHEMBL3092650 | GSK239512 | Ki | = | 0.2042 | nM | 9.69 |