Assay Detail
Functional
CHEMBL948192
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Antagonist activity at human histamine H3 receptor
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and biological activity of piperazine and diazepane amides that are histamine H3 antagonists and serotonin reuptake inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 29 | 9.63 | 10.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL272077 | — | — | 1 | 10.72 |
| CHEMBL401683 | — | — | 1 | 10.70 |
| CHEMBL258349 | — | — | 1 | 10.65 |
| CHEMBL257208 | — | — | 1 | 10.44 |
| CHEMBL272699 | — | — | 1 | 10.40 |
| CHEMBL273136 | — | — | 1 | 10.37 |
| CHEMBL257009 | — | — | 1 | 10.37 |
| CHEMBL272917 | — | — | 1 | 10.32 |
| CHEMBL272698 | — | — | 1 | 10.32 |
| CHEMBL404572 | — | — | 1 | 10.30 |
| CHEMBL257909 | — | — | 1 | 10.10 |
| CHEMBL401867 | — | — | 1 | 10.00 |
| CHEMBL272289 | — | — | 1 | 9.98 |
| CHEMBL257221 | — | — | 1 | 9.98 |
| CHEMBL267267 | — | — | 1 | 9.95 |
| CHEMBL257434 | — | — | 1 | 9.76 |
| CHEMBL257738 | — | — | 1 | 9.76 |
| CHEMBL403377 | — | — | 1 | 9.68 |
| CHEMBL255127 | — | — | 1 | 9.60 |
| CHEMBL439246 | — | — | 1 | 9.41 |
| CHEMBL402286 | — | — | 1 | 9.23 |
| CHEMBL272503 | — | — | 1 | 8.86 |
| CHEMBL256044 | — | — | 1 | 8.63 |
| CHEMBL270625 | — | — | 1 | 8.57 |
| CHEMBL403148 | — | — | 1 | 8.53 |
| CHEMBL258153 | — | — | 1 | 8.35 |
| CHEMBL408206 | — | — | 1 | 8.17 |
| CHEMBL273157 | — | — | 1 | 8.15 |
| CHEMBL402644 | — | — | 1 | 8.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL272077 | — | Kd | = | 0.01905 | nM | 10.72 |
| CHEMBL401683 | — | Kd | = | 0.01995 | nM | 10.70 |
| CHEMBL258349 | — | Kd | = | 0.02239 | nM | 10.65 |
| CHEMBL257208 | — | Kd | = | 0.03631 | nM | 10.44 |
| CHEMBL272699 | — | Kd | = | 0.03981 | nM | 10.40 |
| CHEMBL273136 | — | Kd | = | 0.04266 | nM | 10.37 |
| CHEMBL257009 | — | Kd | = | 0.04266 | nM | 10.37 |
| CHEMBL272917 | — | Kd | = | 0.04786 | nM | 10.32 |
| CHEMBL272698 | — | Kd | = | 0.04786 | nM | 10.32 |
| CHEMBL404572 | — | Kd | = | 0.05012 | nM | 10.30 |
| CHEMBL257909 | — | Kd | = | 0.07943 | nM | 10.10 |
| CHEMBL401867 | — | Kd | = | 0.1 | nM | 10.00 |
| CHEMBL272289 | — | Kd | = | 0.1047 | nM | 9.98 |
| CHEMBL257221 | — | Kd | = | 0.1047 | nM | 9.98 |
| CHEMBL267267 | — | Kd | = | 0.1122 | nM | 9.95 |
| CHEMBL257434 | — | Kd | = | 0.1738 | nM | 9.76 |
| CHEMBL257738 | — | Kd | = | 0.1738 | nM | 9.76 |
| CHEMBL403377 | — | Kd | = | 0.2089 | nM | 9.68 |
| CHEMBL255127 | — | Kd | = | 0.2512 | nM | 9.60 |
| CHEMBL439246 | — | Kd | = | 0.389 | nM | 9.41 |
| CHEMBL402286 | — | Kd | = | 0.5888 | nM | 9.23 |
| CHEMBL272503 | — | Kd | = | 1.38 | nM | 8.86 |
| CHEMBL256044 | — | Kd | = | 2.344 | nM | 8.63 |
| CHEMBL270625 | — | Kd | = | 2.692 | nM | 8.57 |
| CHEMBL403148 | — | Kd | = | 2.951 | nM | 8.53 |
| CHEMBL258153 | — | Kd | = | 4.467 | nM | 8.35 |
| CHEMBL408206 | — | Kd | = | 6.761 | nM | 8.17 |
| CHEMBL273157 | — | Kd | = | 7.079 | nM | 8.15 |
| CHEMBL402644 | — | Kd | = | 7.943 | nM | 8.10 |