Assay Detail
Binding
CHEMBL671002
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Binding against Dopamine transporter using radioligand as [3H]GBR 12935
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Development of novel, potent, and selective dopamine reuptake inhibitors through alteration of the piperazine ring of 1-[2-(diphenylmethoxy)ethyl]-and 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines (GBR 12935 and GBR 12909).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 7.49 | 8.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL143823 | — | — | 1 | 8.59 |
| CHEMBL26320 | — | — | 1 | 8.39 |
| CHEMBL142674 | — | — | 1 | 8.36 |
| CHEMBL281594 | VANOXERINE | 3.0 | 1 | 8.26 |
| CHEMBL102119 | — | — | 1 | 8.14 |
| CHEMBL143612 | — | — | 1 | 8.03 |
| CHEMBL140054 | — | — | 1 | 7.68 |
| CHEMBL344083 | — | — | 1 | 7.64 |
| CHEMBL142545 | — | — | 1 | 7.40 |
| CHEMBL140104 | — | — | 1 | 7.10 |
| CHEMBL141251 | — | — | 1 | 6.98 |
| CHEMBL142617 | — | — | 1 | 6.98 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 6.18 |
| CHEMBL346409 | — | — | 1 | 5.11 |
| CHEMBL143407 | — | — | 1 | - |
| CHEMBL143750 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL143823 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL26320 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL142674 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL281594 | VANOXERINE | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL102119 | — | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL143612 | — | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL140054 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL344083 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL142545 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL140104 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL141251 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL142617 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL370805 | COCAINE | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL346409 | — | IC50 | = | 7760.0 | nM | 5.11 |
| CHEMBL143407 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL143750 | — | IC50 | > | 30000.0 | nM | - |