Assay Detail
Binding
CHEMBL695010
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In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Synthesis and antiulcer activity of N-substituted N'-[3-[3-(piperidinomethyl)phenoxy]propyl]ureas: histamine H2-receptor antagonists with a potent mucosal protective activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 29 | 6.58 | 7.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL311206 | DALCOTIDINE | 2.0 | 1 | 7.39 |
| CHEMBL81545 | — | — | 1 | 7.36 |
| CHEMBL82654 | — | — | 1 | 7.36 |
| CHEMBL432167 | — | — | 1 | 7.32 |
| CHEMBL78519 | — | — | 1 | 7.09 |
| CHEMBL78339 | — | — | 1 | 7.07 |
| CHEMBL81750 | — | — | 1 | 7.02 |
| CHEMBL82599 | — | — | 1 | 7.01 |
| CHEMBL902 | FAMOTIDINE | 4.0 | 1 | 7.00 |
| CHEMBL80046 | — | — | 1 | 6.90 |
| CHEMBL81506 | — | — | 1 | 6.81 |
| CHEMBL81039 | — | — | 1 | 6.80 |
| CHEMBL79974 | — | — | 1 | 6.77 |
| CHEMBL80084 | — | — | 1 | 6.70 |
| CHEMBL30 | CIMETIDINE | 4.0 | 1 | 6.58 |
| CHEMBL311978 | — | — | 1 | 6.57 |
| CHEMBL81758 | — | — | 1 | 6.54 |
| CHEMBL309659 | — | — | 1 | 6.50 |
| CHEMBL80105 | — | — | 1 | 6.46 |
| CHEMBL82430 | — | — | 1 | 6.31 |
| CHEMBL311272 | — | — | 1 | 6.20 |
| CHEMBL81520 | — | — | 1 | 6.20 |
| CHEMBL312419 | — | — | 1 | 6.20 |
| CHEMBL316154 | — | — | 1 | 6.11 |
| CHEMBL80069 | — | — | 1 | 6.09 |
| CHEMBL312601 | — | — | 1 | 5.77 |
| CHEMBL81597 | — | — | 1 | 5.68 |
| CHEMBL313060 | — | — | 1 | 5.65 |
| CHEMBL79507 | — | — | 1 | 5.36 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL311206 | DALCOTIDINE | Kd | = | 40.74 | nM | 7.39 |
| CHEMBL81545 | — | Kd | = | 43.65 | nM | 7.36 |
| CHEMBL82654 | — | Kd | = | 43.65 | nM | 7.36 |
| CHEMBL432167 | — | Kd | = | 47.86 | nM | 7.32 |
| CHEMBL78519 | — | Kd | = | 81.28 | nM | 7.09 |
| CHEMBL78339 | — | Kd | = | 85.11 | nM | 7.07 |
| CHEMBL81750 | — | Kd | = | 95.5 | nM | 7.02 |
| CHEMBL82599 | — | Kd | = | 97.72 | nM | 7.01 |
| CHEMBL902 | FAMOTIDINE | Kd | = | 100.0 | nM | 7.00 |
| CHEMBL80046 | — | Kd | = | 125.89 | nM | 6.90 |
| CHEMBL81506 | — | Kd | = | 154.88 | nM | 6.81 |
| CHEMBL81039 | — | Kd | = | 158.49 | nM | 6.80 |
| CHEMBL79974 | — | Kd | = | 169.82 | nM | 6.77 |
| CHEMBL80084 | — | Kd | = | 199.53 | nM | 6.70 |
| CHEMBL30 | CIMETIDINE | Kd | = | 263.03 | nM | 6.58 |
| CHEMBL311978 | — | Kd | = | 269.15 | nM | 6.57 |
| CHEMBL81758 | — | Kd | = | 288.4 | nM | 6.54 |
| CHEMBL309659 | — | Kd | = | 316.23 | nM | 6.50 |
| CHEMBL80105 | — | Kd | = | 346.74 | nM | 6.46 |
| CHEMBL82430 | — | Kd | = | 489.78 | nM | 6.31 |
| CHEMBL311272 | — | Kd | = | 630.96 | nM | 6.20 |
| CHEMBL81520 | — | Kd | = | 630.96 | nM | 6.20 |
| CHEMBL312419 | — | Kd | = | 630.96 | nM | 6.20 |
| CHEMBL316154 | — | Kd | = | 776.25 | nM | 6.11 |
| CHEMBL80069 | — | Kd | = | 812.83 | nM | 6.09 |
| CHEMBL312601 | — | Kd | = | 1698.24 | nM | 5.77 |
| CHEMBL81597 | — | Kd | = | 2089.3 | nM | 5.68 |
| CHEMBL313060 | — | Kd | = | 2238.72 | nM | 5.65 |
| CHEMBL79507 | — | Kd | = | 4365.16 | nM | 5.36 |