Assay Detail
Functional
CHEMBL800887
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro binding affinity was determined against serotonin reuptake site of rat in presence of [3H]paroxetine radioligand
51
Total Activities
51
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Sodium-dependent serotonin transporter (CHEMBL313) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Potential antidepressants displayed combined alpha(2)-adrenoceptor antagonist and monoamine uptake inhibitor properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 51 | 7.24 | 8.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL436234 | — | — | 1 | 8.80 |
| CHEMBL354611 | — | — | 1 | 8.70 |
| CHEMBL166690 | — | — | 1 | 8.30 |
| CHEMBL166648 | — | — | 1 | 8.00 |
| CHEMBL166748 | — | — | 1 | 8.00 |
| CHEMBL41 | FLUOXETINE | 4.0 | 1 | 8.00 |
| CHEMBL354072 | — | — | 1 | 7.90 |
| CHEMBL352643 | — | — | 1 | 7.90 |
| CHEMBL167394 | — | — | 1 | 7.80 |
| CHEMBL352636 | — | — | 1 | 7.80 |
| CHEMBL165529 | — | — | 1 | 7.80 |
| CHEMBL168205 | — | — | 1 | 7.70 |
| CHEMBL168022 | — | — | 1 | 7.70 |
| CHEMBL353200 | — | — | 1 | 7.70 |
| CHEMBL165467 | — | — | 1 | 7.60 |
| CHEMBL90997 | — | — | 1 | 7.60 |
| CHEMBL353910 | — | — | 1 | 7.60 |
| CHEMBL168168 | — | — | 1 | 7.50 |
| CHEMBL354112 | — | — | 1 | 7.50 |
| CHEMBL168153 | — | — | 1 | 7.40 |
| CHEMBL407509 | — | — | 1 | 7.40 |
| CHEMBL262777 | VANCOMYCIN | 4.0 | 1 | 7.30 |
| CHEMBL167578 | — | — | 1 | 7.30 |
| CHEMBL353212 | — | — | 1 | 7.30 |
| CHEMBL167515 | — | — | 1 | 7.20 |
| CHEMBL353843 | — | — | 1 | 7.20 |
| CHEMBL164118 | — | — | 1 | 7.20 |
| CHEMBL167437 | — | — | 1 | 7.20 |
| CHEMBL353139 | — | — | 1 | 7.10 |
| CHEMBL168063 | — | — | 1 | 7.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL436234 | — | Ki | = | 1.585 | nM | 8.80 |
| CHEMBL354611 | — | Ki | = | 1.995 | nM | 8.70 |
| CHEMBL166690 | — | Ki | = | 5.012 | nM | 8.30 |
| CHEMBL166648 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL166748 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL41 | FLUOXETINE | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL354072 | — | Ki | = | 12.59 | nM | 7.90 |
| CHEMBL352643 | — | Ki | = | 12.59 | nM | 7.90 |
| CHEMBL167394 | — | Ki | = | 15.85 | nM | 7.80 |
| CHEMBL352636 | — | Ki | = | 15.85 | nM | 7.80 |
| CHEMBL165529 | — | Ki | = | 15.85 | nM | 7.80 |
| CHEMBL168205 | — | Ki | = | 19.95 | nM | 7.70 |
| CHEMBL168022 | — | Ki | = | 19.95 | nM | 7.70 |
| CHEMBL353200 | — | Ki | = | 19.95 | nM | 7.70 |
| CHEMBL353910 | — | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL90997 | — | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL165467 | — | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL168168 | — | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL354112 | — | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL168153 | — | Ki | = | 39.81 | nM | 7.40 |
| CHEMBL407509 | — | Ki | = | 39.81 | nM | 7.40 |
| CHEMBL262777 | VANCOMYCIN | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL167578 | — | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL353212 | — | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL167437 | — | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL353843 | — | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL167515 | — | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL164118 | — | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL353139 | — | Ki | = | 79.43 | nM | 7.10 |
| CHEMBL168063 | — | Ki | = | 79.43 | nM | 7.10 |
| CHEMBL166448 | — | Ki | = | 79.43 | nM | 7.10 |
| CHEMBL355467 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL166852 | — | Ki | = | 158.49 | nM | 6.80 |
| CHEMBL352704 | — | Ki | = | 158.49 | nM | 6.80 |
| CHEMBL165645 | — | Ki | = | 158.49 | nM | 6.80 |
| CHEMBL167493 | NAPAMEZOLE | Ki | = | 199.53 | nM | 6.70 |
| CHEMBL167665 | — | Ki | = | 199.53 | nM | 6.70 |
| CHEMBL424557 | — | Ki | = | 251.19 | nM | 6.60 |
| CHEMBL168000 | — | Ki | = | 251.19 | nM | 6.60 |
| CHEMBL166683 | — | Ki | = | 398.11 | nM | 6.40 |
| CHEMBL166501 | — | Ki | = | 501.19 | nM | 6.30 |
| CHEMBL168201 | — | Ki | = | 630.96 | nM | 6.20 |
| CHEMBL164070 | — | Ki | = | 630.96 | nM | 6.20 |
| CHEMBL167644 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL167649 | — | Ki | = | 1258.93 | nM | 5.90 |
| CHEMBL167795 | — | Ki | = | 6309.57 | nM | 5.20 |
| CHEMBL166226 | — | Ki | < | 1000.0 | nM | - |
| CHEMBL3037826 | — | Ki | < | 3162.28 | nM | - |
| CHEMBL353705 | — | Ki | < | 10000.0 | nM | - |
| CHEMBL353972 | ATIPAMEZOLE | Ki | < | 3162.28 | nM | - |