Assay Detail
Binding
CHEMBL829579
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Displacement of [3H]paroxetine from Serotonin transporter of rat caudate putamen
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Caudate-putamen |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Sodium-dependent serotonin transporter (CHEMBL313) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis and pharmacology of 6-substituted benztropines: discovery of novel dopamine uptake inhibitors possessing low binding affinity to the dopamine transporter.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 6.57 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL370805 | COCAINE | 4.0 | 1 | 9.30 |
| CHEMBL425907 | — | — | 1 | 6.55 |
| CHEMBL361277 | — | — | 1 | 5.46 |
| CHEMBL425008 | — | — | 1 | 4.96 |
| CHEMBL363814 | — | — | 1 | - |
| CHEMBL192672 | — | — | 1 | - |
| CHEMBL365397 | — | — | 1 | - |
| CHEMBL191722 | — | — | 1 | - |
| CHEMBL192317 | — | — | 1 | - |
| CHEMBL2113360 | — | — | 1 | - |
| CHEMBL534927 | — | — | 1 | - |
| CHEMBL2113359 | — | — | 1 | - |
| CHEMBL558788 | — | — | 1 | - |
| CHEMBL2113366 | — | — | 1 | - |
| CHEMBL541630 | — | — | 1 | - |
| CHEMBL189989 | — | — | 1 | - |
| CHEMBL192040 | — | — | 1 | - |
| CHEMBL365353 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL370805 | COCAINE | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL425907 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL361277 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL425008 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL363814 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL192672 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL365397 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL191722 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL192317 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2113360 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL534927 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2113359 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL558788 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2113366 | — | IC50 | > | 10.0 | nM | - |
| CHEMBL541630 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL189989 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL192040 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL365353 | — | IC50 | > | 100000.0 | nM | - |