Assay Detail
Binding
CHEMBL694994
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In vitro inhibition of Histamine H2 receptor by measuring its ability to block the histamine-stimulated adenylate cyclase of guinea pig hippocampal homogenate
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Hippocampus |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Inhibitors of gastric acid secretion: 3,4-diamino-1,2,5-thiadiazole 1-oxides and 1,1-dioxides as urea equivalents in a series of histamine H2-receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 5 | 7.48 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL306465 | — | — | 1 | 8.40 |
| CHEMBL8982 | — | — | 1 | 8.20 |
| CHEMBL63299 | — | — | 1 | 8.20 |
| CHEMBL1790041 | RANITIDINE | 4.0 | 1 | 6.30 |
| CHEMBL30 | CIMETIDINE | 4.0 | 1 | 6.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL306465 | — | Ki | = | 3.981 | nM | 8.40 |
| CHEMBL8982 | — | Ki | = | 6.31 | nM | 8.20 |
| CHEMBL63299 | — | Ki | = | 6.31 | nM | 8.20 |
| CHEMBL1790041 | RANITIDINE | Ki | = | 501.19 | nM | 6.30 |
| CHEMBL30 | CIMETIDINE | Ki | = | 501.19 | nM | 6.30 |