Assay Detail
Binding
CHEMBL675530
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Binding affinity towards dopamine transporter (DAT) by using [125I]RTI-55 radioligand
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent dopamine transporter (CHEMBL238) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Piperidine analogues of 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine (GBR 12909): high affinity ligands for the dopamine transporter.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 8.84 | 9.35 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL137718 | — | — | 1 | 9.35 |
| CHEMBL416409 | — | — | 1 | 9.15 |
| CHEMBL538405 | — | — | 1 | 9.14 |
| CHEMBL136057 | — | — | 1 | 9.00 |
| CHEMBL136154 | — | — | 1 | 9.00 |
| CHEMBL77867 | — | — | 1 | 8.96 |
| CHEMBL343534 | — | — | 1 | 8.89 |
| CHEMBL137020 | — | — | 1 | 8.79 |
| CHEMBL136249 | — | — | 1 | 8.28 |
| CHEMBL35411 | — | — | 1 | 7.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL137718 | — | Ki | = | 0.45 | nM | 9.35 |
| CHEMBL416409 | — | Ki | = | 0.71 | nM | 9.15 |
| CHEMBL538405 | — | Ki | = | 0.73 | nM | 9.14 |
| CHEMBL136057 | — | Ki | = | 0.99 | nM | 9.00 |
| CHEMBL136154 | — | Ki | = | 1.01 | nM | 9.00 |
| CHEMBL77867 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL343534 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL137020 | — | Ki | = | 1.61 | nM | 8.79 |
| CHEMBL136249 | — | Ki | = | 5.3 | nM | 8.28 |
| CHEMBL35411 | — | Ki | = | 16.0 | nM | 7.80 |