Assay Detail
Binding
CHEMBL899542
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Binding affinity at human histamine H3
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Sodium-dependent serotonin transporter (CHEMBL228) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Dual serotonin transporter inhibitor/histamine H3 antagonists: development of rigidified H3 pharmacophores.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 20 | 7.44 | 9.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL438490 | — | — | 1 | 9.14 |
| CHEMBL394861 | — | — | 1 | 8.70 |
| CHEMBL238051 | — | — | 1 | 8.60 |
| CHEMBL237862 | — | — | 1 | 8.09 |
| CHEMBL238052 | — | — | 1 | 7.92 |
| CHEMBL400629 | — | — | 1 | 7.75 |
| CHEMBL238055 | — | — | 1 | 7.68 |
| CHEMBL238054 | — | — | 1 | 7.68 |
| CHEMBL237861 | — | — | 1 | 7.64 |
| CHEMBL400831 | — | — | 1 | 7.61 |
| CHEMBL236784 | — | — | 1 | 7.46 |
| CHEMBL236604 | — | — | 1 | 7.29 |
| CHEMBL236783 | — | — | 1 | 6.96 |
| CHEMBL238053 | — | — | 1 | 6.96 |
| CHEMBL399014 | — | — | 1 | 6.70 |
| CHEMBL236605 | — | — | 1 | 6.60 |
| CHEMBL236782 | — | — | 1 | 6.58 |
| CHEMBL237863 | — | — | 1 | 6.58 |
| CHEMBL236606 | — | — | 1 | 6.49 |
| CHEMBL400830 | — | — | 1 | 6.29 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL438490 | — | Ki | = | 0.72 | nM | 9.14 |
| CHEMBL394861 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL238051 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL237862 | — | Ki | = | 8.2 | nM | 8.09 |
| CHEMBL238052 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL400629 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL238055 | — | Ki | = | 20.7 | nM | 7.68 |
| CHEMBL238054 | — | Ki | = | 20.7 | nM | 7.68 |
| CHEMBL237861 | — | Ki | = | 22.7 | nM | 7.64 |
| CHEMBL400831 | — | Ki | = | 24.3 | nM | 7.61 |
| CHEMBL236784 | — | Ki | = | 34.3 | nM | 7.46 |
| CHEMBL236604 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL236783 | — | Ki | = | 109.0 | nM | 6.96 |
| CHEMBL238053 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL399014 | — | Ki | = | 201.0 | nM | 6.70 |
| CHEMBL236605 | — | Ki | = | 253.0 | nM | 6.60 |
| CHEMBL236782 | — | Ki | = | 265.0 | nM | 6.58 |
| CHEMBL237863 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL236606 | — | Ki | = | 323.0 | nM | 6.49 |
| CHEMBL400830 | — | Ki | = | 511.0 | nM | 6.29 |