Assay Detail
Binding
CHEMBL948191
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Inhibition of rat SERT
40
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent serotonin transporter (CHEMBL313) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
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 | 40 | 7.88 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL267267 | — | — | 1 | 9.00 |
| CHEMBL272077 | — | — | 1 | 8.85 |
| CHEMBL270625 | — | — | 1 | 8.74 |
| CHEMBL272503 | — | — | 1 | 8.72 |
| CHEMBL257434 | — | — | 1 | 8.66 |
| CHEMBL257909 | — | — | 1 | 8.42 |
| CHEMBL270165 | — | — | 1 | 8.40 |
| CHEMBL409877 | — | — | 1 | 8.38 |
| CHEMBL273136 | — | — | 1 | 8.35 |
| CHEMBL408206 | — | — | 1 | 8.31 |
| CHEMBL273157 | — | — | 1 | 8.24 |
| CHEMBL258349 | — | — | 1 | 8.17 |
| CHEMBL272698 | — | — | 1 | 8.10 |
| CHEMBL256044 | — | — | 1 | 8.09 |
| CHEMBL256390 | — | — | 1 | 8.09 |
| CHEMBL272917 | — | — | 1 | 8.07 |
| CHEMBL257738 | — | — | 1 | 8.04 |
| CHEMBL402644 | — | — | 1 | 8.03 |
| CHEMBL257221 | — | — | 1 | 8.02 |
| CHEMBL404247 | — | — | 1 | 8.01 |
| CHEMBL272699 | — | — | 1 | 8.01 |
| CHEMBL257743 | — | — | 1 | 8.00 |
| CHEMBL402590 | — | — | 1 | 7.96 |
| CHEMBL403377 | — | — | 1 | 7.96 |
| CHEMBL402286 | — | — | 1 | 7.96 |
| CHEMBL258153 | — | — | 1 | 7.92 |
| CHEMBL257208 | — | — | 1 | 7.89 |
| CHEMBL272289 | — | — | 1 | 7.85 |
| CHEMBL269966 | — | — | 1 | 7.80 |
| CHEMBL403148 | — | — | 1 | 7.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL267267 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL272077 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL270625 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL272503 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL257434 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL257909 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL270165 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL409877 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL273136 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL408206 | — | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL273157 | — | Ki | = | 5.8 | nM | 8.24 |
| CHEMBL258349 | — | Ki | = | 6.7 | nM | 8.17 |
| CHEMBL272698 | — | Ki | = | 7.9 | nM | 8.10 |
| CHEMBL256044 | — | Ki | = | 8.2 | nM | 8.09 |
| CHEMBL256390 | — | Ki | = | 8.1 | nM | 8.09 |
| CHEMBL272917 | — | Ki | = | 8.5 | nM | 8.07 |
| CHEMBL257738 | — | Ki | = | 9.1 | nM | 8.04 |
| CHEMBL402644 | — | Ki | = | 9.3 | nM | 8.03 |
| CHEMBL257221 | — | Ki | = | 9.5 | nM | 8.02 |
| CHEMBL272699 | — | Ki | = | 9.7 | nM | 8.01 |
| CHEMBL404247 | — | Ki | = | 9.7 | nM | 8.01 |
| CHEMBL257743 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL402590 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL403377 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL402286 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL258153 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL257208 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL272289 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL269966 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL403148 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL404572 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL401683 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL401867 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL270411 | — | Ki | = | 102.0 | nM | 6.99 |
| CHEMBL270607 | — | Ki | = | 113.0 | nM | 6.95 |
| CHEMBL402949 | — | Ki | = | 117.0 | nM | 6.93 |
| CHEMBL270396 | — | Ki | = | 186.0 | nM | 6.73 |
| CHEMBL257009 | — | Ki | = | 238.0 | nM | 6.62 |
| CHEMBL255127 | — | Ki | = | 299.0 | nM | 6.52 |
| CHEMBL439246 | — | Ki | = | 900.0 | nM | 6.05 |