Assay Detail
Binding
CHEMBL675003
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Inhibitory potency against dopamine (DA) transporter using [3H]WIN-35428 (WIN-) binding assay.
18
Total Activities
8
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
Synthesis and pharmacology of site-specific cocaine abuse treatment agents: 2-substituted-6-amino-5-phenylbicyclo[2.2.2]octanes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 5.84 | 7.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL358368 | — | — | 1 | 7.85 |
| CHEMBL2079586 | — | — | 1 | 7.69 |
| CHEMBL827 | DEXMETHYLPHENIDATE | 4.0 | 1 | 7.08 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 6.80 |
| CHEMBL357443 | — | — | 4 | 6.57 |
| CHEMBL436211 | — | — | 4 | 5.75 |
| CHEMBL145534 | — | — | 2 | 5.40 |
| CHEMBL145732 | — | — | 4 | 5.27 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL358368 | — | IC50 | = | 14.2 | nM | 7.85 |
| CHEMBL2079586 | — | IC50 | = | 20.4 | nM | 7.69 |
| CHEMBL827 | DEXMETHYLPHENIDATE | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL370805 | COCAINE | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL357443 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL357443 | — | IC50 | = | 358.0 | nM | 6.45 |
| CHEMBL436211 | — | IC50 | = | 1770.0 | nM | 5.75 |
| CHEMBL436211 | — | IC50 | = | 2040.0 | nM | 5.69 |
| CHEMBL357443 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL357443 | — | IC50 | = | 2270.0 | nM | 5.64 |
| CHEMBL145534 | — | IC50 | = | 4010.0 | nM | 5.40 |
| CHEMBL145732 | — | IC50 | = | 5330.0 | nM | 5.27 |
| CHEMBL436211 | — | IC50 | = | 7040.0 | nM | 5.15 |
| CHEMBL436211 | — | IC50 | = | 9920.0 | nM | 5.00 |
| CHEMBL145534 | — | IC50 | = | 10300.0 | nM | 4.99 |
| CHEMBL145732 | — | IC50 | = | 12200.0 | nM | 4.91 |
| CHEMBL145732 | — | IC50 | = | 13600.0 | nM | 4.87 |
| CHEMBL145732 | — | IC50 | = | 45600.0 | nM | 4.34 |