Assay Detail
Binding
CHEMBL675002
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Inhibitory potency against [3H]DA uptake 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 | 5.60 | 7.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL827 | DEXMETHYLPHENIDATE | 4.0 | 1 | 7.62 |
| CHEMBL358368 | — | — | 1 | 7.53 |
| CHEMBL2079586 | — | — | 1 | 7.29 |
| CHEMBL357443 | — | — | 4 | 6.43 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 6.39 |
| CHEMBL436211 | — | — | 4 | 5.55 |
| CHEMBL145732 | — | — | 4 | 5.31 |
| CHEMBL145534 | — | — | 2 | 5.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL827 | DEXMETHYLPHENIDATE | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL358368 | — | IC50 | = | 29.3 | nM | 7.53 |
| CHEMBL2079586 | — | IC50 | = | 51.3 | nM | 7.29 |
| CHEMBL357443 | — | IC50 | = | 372.0 | nM | 6.43 |
| CHEMBL370805 | COCAINE | IC50 | = | 404.0 | nM | 6.39 |
| CHEMBL357443 | — | IC50 | = | 687.0 | nM | 6.16 |
| CHEMBL436211 | — | IC50 | = | 2810.0 | nM | 5.55 |
| CHEMBL436211 | — | IC50 | = | 4450.0 | nM | 5.35 |
| CHEMBL357443 | — | IC50 | = | 4840.0 | nM | 5.32 |
| CHEMBL145732 | — | IC50 | = | 4930.0 | nM | 5.31 |
| CHEMBL357443 | — | IC50 | = | 8240.0 | nM | 5.08 |
| CHEMBL145534 | — | IC50 | = | 9140.0 | nM | 5.04 |
| CHEMBL436211 | — | IC50 | = | 10900.0 | nM | 4.96 |
| CHEMBL145732 | — | IC50 | = | 16300.0 | nM | 4.79 |
| CHEMBL436211 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL145534 | — | IC50 | = | 24700.0 | nM | 4.61 |
| CHEMBL145732 | — | IC50 | = | 25800.0 | nM | 4.59 |
| CHEMBL145732 | — | IC50 | = | 75000.0 | nM | 4.12 |