Assay Detail
Binding
CHEMBL807134
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Binding affinity was determined at the Serotonin transporter labeled with radioligand [125 I] RTI-55
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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
Heteroaromatic analogs of 1-[2-(diphenylmethoxy)ethyl]- and 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines (GBR 12935 and GBR 12909) as high-affinity dopamine reuptake inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 6.63 | 7.06 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL159320 | — | — | 1 | 7.06 |
| CHEMBL163980 | — | — | 1 | 6.98 |
| CHEMBL159967 | — | — | 1 | 6.96 |
| CHEMBL281594 | VANOXERINE | 3.0 | 1 | 6.90 |
| CHEMBL286991 | — | — | 1 | 6.87 |
| CHEMBL159319 | — | — | 1 | 6.69 |
| CHEMBL164037 | — | — | 1 | 6.48 |
| CHEMBL26320 | — | — | 1 | 6.21 |
| CHEMBL159608 | — | — | 1 | 5.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL159320 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL163980 | — | IC50 | = | 105.0 | nM | 6.98 |
| CHEMBL159967 | — | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL281594 | VANOXERINE | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL286991 | — | IC50 | = | 135.0 | nM | 6.87 |
| CHEMBL159319 | — | IC50 | = | 204.0 | nM | 6.69 |
| CHEMBL164037 | — | IC50 | = | 334.0 | nM | 6.48 |
| CHEMBL26320 | — | IC50 | = | 623.0 | nM | 6.21 |
| CHEMBL159608 | — | IC50 | = | 2800.0 | nM | 5.55 |