Assay Detail
Binding
CHEMBL672114
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Tested for inhibition of radioligand [3H]dopamine (DA) uptake in rat synaptosomes
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Further studies of the structure-activity relationships of 1-[1-(2-benzo[b]thienyl)cyclohexyl]piperidine. Synthesis and evaluation of 1-(2-benzo[b]thienyl)-N,N-dialkylcyclohexylamines at dopamine uptake and phencyclidine binding sites.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 7.32 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL131389 | — | — | 1 | 8.40 |
| CHEMBL340059 | — | — | 1 | 8.30 |
| CHEMBL335006 | — | — | 1 | 8.15 |
| CHEMBL130749 | — | — | 1 | 8.15 |
| CHEMBL439796 | — | — | 1 | 7.96 |
| CHEMBL279556 | — | — | 1 | 7.96 |
| CHEMBL336359 | — | — | 1 | 7.92 |
| CHEMBL132044 | — | — | 1 | 7.85 |
| CHEMBL336193 | — | — | 1 | 7.77 |
| CHEMBL338121 | — | — | 1 | 7.66 |
| CHEMBL130224 | — | — | 1 | 7.54 |
| CHEMBL336575 | — | — | 1 | 7.48 |
| CHEMBL336154 | — | — | 1 | 7.48 |
| CHEMBL335901 | — | — | 1 | 7.48 |
| CHEMBL335957 | — | — | 1 | 7.47 |
| CHEMBL339868 | — | — | 1 | 7.29 |
| CHEMBL335982 | — | — | 1 | 7.24 |
| CHEMBL18618 | — | — | 1 | 7.11 |
| CHEMBL335531 | — | — | 1 | 7.09 |
| CHEMBL133223 | — | — | 1 | 7.06 |
| CHEMBL336153 | — | — | 1 | 7.05 |
| CHEMBL339243 | — | — | 1 | 6.86 |
| CHEMBL130383 | — | — | 1 | 6.76 |
| CHEMBL335829 | — | — | 1 | 6.71 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 6.53 |
| CHEMBL128887 | — | — | 1 | 6.02 |
| CHEMBL335905 | — | — | 1 | 5.87 |
| CHEMBL336535 | — | — | 1 | 5.67 |
| CHEMBL339896 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL131389 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL340059 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL335006 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL130749 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL439796 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL279556 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL336359 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL132044 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL336193 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL338121 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL130224 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL336575 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL336154 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL335901 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL335957 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL339868 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL335982 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL18618 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL335531 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL133223 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL336153 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL339243 | — | IC50 | = | 138.0 | nM | 6.86 |
| CHEMBL130383 | — | IC50 | = | 174.0 | nM | 6.76 |
| CHEMBL335829 | — | IC50 | = | 196.0 | nM | 6.71 |
| CHEMBL370805 | COCAINE | IC50 | = | 296.0 | nM | 6.53 |
| CHEMBL128887 | — | IC50 | = | 947.0 | nM | 6.02 |
| CHEMBL335905 | — | IC50 | = | 1363.0 | nM | 5.87 |
| CHEMBL336535 | — | IC50 | = | 2124.0 | nM | 5.67 |
| CHEMBL339896 | — | IC50 | > | 5000.0 | nM | - |