Assay Detail
Binding
CHEMBL806550
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In vitro inhibition of [3H]5-HT transporter uptake in rat brain synaptosomes
9
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Subcellular | Synaptosomes |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Sodium-dependent serotonin transporter (CHEMBL313) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Antihypertensive activity in a series of 1-piperazino-3-phenylindans with potent 5-HT2-antagonistic activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 5.88 | 7.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1237326 | — | — | 1 | 7.38 |
| CHEMBL1237336 | — | — | 1 | 6.40 |
| CHEMBL305905 | — | — | 1 | 6.21 |
| CHEMBL1237338 | — | — | 1 | 6.14 |
| CHEMBL1237328 | — | — | 1 | 5.66 |
| CHEMBL70887 | — | — | 1 | 5.41 |
| CHEMBL1237344 | — | — | 1 | 5.01 |
| CHEMBL73461 | IRINDALONE | 2.0 | 2 | 4.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1237326 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL1237336 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL305905 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL1237338 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL1237328 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL70887 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL1237344 | — | IC50 | = | 9700.0 | nM | 5.01 |
| CHEMBL73461 | IRINDALONE | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL73461 | IRINDALONE | IC50 | > | 100000.0 | nM | - |