Assay Detail
Functional
CHEMBL695015
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Histamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atrium
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Cavia porcellus |
| Tissue | Cardiac atrium |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Synthesis and pharmacological activity of fluorescent histamine H2 receptor antagonists related to potentidine.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 16 | 6.32 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL45728 | — | — | 1 | 7.96 |
| CHEMBL902 | FAMOTIDINE | 4.0 | 1 | 7.74 |
| CHEMBL45725 | — | — | 1 | 7.59 |
| CHEMBL46043 | — | — | 1 | 7.49 |
| CHEMBL295682 | — | — | 1 | 7.43 |
| CHEMBL46102 | ROXATIDINE ACETATE | -1.0 | 1 | 7.41 |
| CHEMBL1790041 | RANITIDINE | 4.0 | 1 | 6.77 |
| CHEMBL47917 | — | — | 1 | 6.74 |
| CHEMBL30 | CIMETIDINE | 4.0 | 1 | 6.00 |
| CHEMBL48885 | — | — | 1 | 5.96 |
| CHEMBL291192 | — | — | 1 | 5.74 |
| CHEMBL295252 | — | — | 1 | 5.71 |
| CHEMBL297324 | — | — | 1 | 5.05 |
| CHEMBL47979 | — | — | 1 | 5.00 |
| CHEMBL45907 | — | — | 1 | 4.35 |
| CHEMBL297627 | — | — | 1 | 4.18 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL45728 | — | Kd | = | 10.96 | nM | 7.96 |
| CHEMBL902 | FAMOTIDINE | Kd | = | 18.2 | nM | 7.74 |
| CHEMBL45725 | — | Kd | = | 25.7 | nM | 7.59 |
| CHEMBL46043 | — | Kd | = | 32.36 | nM | 7.49 |
| CHEMBL295682 | — | Kd | = | 37.15 | nM | 7.43 |
| CHEMBL46102 | ROXATIDINE ACETATE | Kd | = | 38.9 | nM | 7.41 |
| CHEMBL1790041 | RANITIDINE | Kd | = | 169.82 | nM | 6.77 |
| CHEMBL47917 | — | Kd | = | 181.97 | nM | 6.74 |
| CHEMBL30 | CIMETIDINE | Kd | = | 1000.0 | nM | 6.00 |
| CHEMBL48885 | — | Kd | = | 1096.48 | nM | 5.96 |
| CHEMBL291192 | — | Kd | = | 1819.7 | nM | 5.74 |
| CHEMBL295252 | — | Kd | = | 1949.84 | nM | 5.71 |
| CHEMBL297324 | — | Kd | = | 8912.51 | nM | 5.05 |
| CHEMBL47979 | — | Kd | = | 10000.0 | nM | 5.00 |
| CHEMBL45907 | — | Kd | = | 44668.36 | nM | 4.35 |
| CHEMBL297627 | — | Kd | = | 66069.34 | nM | 4.18 |