Assay Detail
Binding
CHEMBL948189
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Inhibition of human histamine H3 receptor
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 |
|---|---|---|---|
| Ki | 43 | 8.56 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL272077 | — | — | 1 | 9.30 |
| CHEMBL257208 | — | — | 1 | 9.15 |
| CHEMBL235614 | — | — | 1 | 9.15 |
| CHEMBL401683 | — | — | 1 | 9.10 |
| CHEMBL258349 | — | — | 1 | 9.10 |
| CHEMBL272699 | — | — | 1 | 9.05 |
| CHEMBL273136 | — | — | 1 | 9.00 |
| CHEMBL402949 | — | — | 1 | 9.00 |
| CHEMBL401867 | — | — | 1 | 9.00 |
| CHEMBL257009 | — | — | 1 | 9.00 |
| CHEMBL272289 | — | — | 1 | 9.00 |
| CHEMBL403148 | — | — | 1 | 8.96 |
| CHEMBL256044 | — | — | 1 | 8.96 |
| CHEMBL257909 | — | — | 1 | 8.96 |
| CHEMBL404572 | — | — | 1 | 8.96 |
| CHEMBL267267 | — | — | 1 | 8.96 |
| CHEMBL272503 | — | — | 1 | 8.92 |
| CHEMBL272698 | — | — | 1 | 8.85 |
| CHEMBL257434 | — | — | 1 | 8.85 |
| CHEMBL272917 | — | — | 1 | 8.82 |
| CHEMBL257738 | — | — | 1 | 8.74 |
| CHEMBL439246 | — | — | 1 | 8.70 |
| CHEMBL403377 | — | — | 1 | 8.70 |
| CHEMBL255127 | — | — | 1 | 8.68 |
| CHEMBL270625 | — | — | 1 | 8.66 |
| CHEMBL408206 | — | — | 1 | 8.62 |
| CHEMBL257743 | — | — | 1 | 8.62 |
| CHEMBL256390 | — | — | 1 | 8.47 |
| CHEMBL257221 | — | — | 1 | 8.39 |
| CHEMBL273157 | — | — | 1 | 8.37 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL272077 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL257208 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL235614 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL401683 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL258349 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL272699 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL273136 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL402949 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL401867 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL257009 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL272289 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL257909 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL403148 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL256044 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL267267 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL404572 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL272503 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL272698 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL257434 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL272917 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL257738 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL439246 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL403377 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL255127 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL270625 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL408206 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL257743 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL256390 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL257221 | — | Ki | = | 4.1 | nM | 8.39 |
| CHEMBL273157 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL402286 | — | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL270396 | — | Ki | = | 6.8 | nM | 8.17 |
| CHEMBL258153 | — | Ki | = | 7.7 | nM | 8.11 |
| CHEMBL257917 | — | Ki | = | 10.6 | nM | 7.97 |
| CHEMBL236046 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL404247 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL270607 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL270411 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL402590 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL409877 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL402644 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL270165 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL269966 | — | Ki | = | 37.0 | nM | 7.43 |