Assay Detail
Binding
CHEMBL872400
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro inhibitory constant against [3H]paroxetine binding to rat frontal cortex membrane serotonin reuptake site
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Frontal cortex |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Sodium-dependent serotonin transporter (CHEMBL313) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis, structure-activity relationships, and biological properties of 1-heteroaryl-4-[omega-(1H-indol-3-yl)alkyl]piperazines, novel potential antipsychotics combining potent dopamine D2 receptor antagonism with potent serotonin reuptake inhibition.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 33 | 8.70 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL196514 | — | — | 1 | 9.70 |
| CHEMBL193501 | — | — | 1 | 9.52 |
| CHEMBL196171 | — | — | 1 | 9.40 |
| CHEMBL193854 | — | — | 1 | 9.40 |
| CHEMBL198070 | — | — | 1 | 9.40 |
| CHEMBL198107 | — | — | 1 | 9.40 |
| CHEMBL198216 | — | — | 1 | 9.30 |
| CHEMBL370359 | — | — | 1 | 9.30 |
| CHEMBL198069 | — | — | 1 | 9.22 |
| CHEMBL196893 | — | — | 1 | 9.22 |
| CHEMBL370457 | — | — | 1 | 9.15 |
| CHEMBL198224 | — | — | 1 | 9.00 |
| CHEMBL198040 | — | — | 1 | 8.96 |
| CHEMBL198812 | — | — | 1 | 8.96 |
| CHEMBL197943 | — | — | 1 | 8.85 |
| CHEMBL365605 | — | — | 1 | 8.85 |
| CHEMBL197665 | — | — | 1 | 8.82 |
| CHEMBL383396 | — | — | 1 | 8.82 |
| CHEMBL369984 | — | — | 1 | 8.80 |
| CHEMBL276520 | INDALPINE | 4.0 | 1 | 8.70 |
| CHEMBL194240 | — | — | 1 | 8.70 |
| CHEMBL196172 | — | — | 1 | 8.62 |
| CHEMBL197839 | — | — | 1 | 8.57 |
| CHEMBL199045 | — | — | 1 | 8.55 |
| CHEMBL198357 | — | — | 1 | 8.52 |
| CHEMBL198041 | — | — | 1 | 8.13 |
| CHEMBL194510 | — | — | 1 | 8.10 |
| CHEMBL372735 | — | — | 1 | 7.92 |
| CHEMBL196505 | — | — | 1 | 7.92 |
| CHEMBL196132 | — | — | 1 | 7.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL196514 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL193501 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL196171 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL193854 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL198070 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL198107 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL198216 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL370359 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL198069 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL196893 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL370457 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL198224 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL198040 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL198812 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL365605 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL197943 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL197665 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL383396 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL369984 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL276520 | INDALPINE | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL194240 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL196172 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL197839 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL199045 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL198357 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL198041 | — | Ki | = | 7.4 | nM | 8.13 |
| CHEMBL194510 | — | Ki | = | 7.9 | nM | 8.10 |
| CHEMBL372735 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL196505 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL196132 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL263329 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL194844 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL195015 | — | Ki | = | 176.0 | nM | 6.75 |