Assay Detail
Binding
CHEMBL675225
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Inhibitory binding activity against rat striatal tissue using [3H]WIN-35248 as the radioligand.
42
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Striatum |
| 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-(aminomethyl)-3-phenylbicyclo[2.2.2]- and -[2.2.1]alkane dopamine uptake inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 42 | 6.70 | 8.11 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL172524 | — | — | 4 | 8.11 |
| CHEMBL172523 | — | — | 3 | 7.94 |
| CHEMBL169642 | — | — | 2 | 7.89 |
| CHEMBL358368 | — | — | 2 | 7.85 |
| CHEMBL2079586 | — | — | 1 | 7.69 |
| CHEMBL169814 | — | — | 2 | 7.67 |
| CHEMBL170876 | — | — | 2 | 7.43 |
| CHEMBL172115 | — | — | 2 | 6.93 |
| CHEMBL353466 | — | — | 2 | 6.83 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 6.80 |
| CHEMBL353469 | — | — | 1 | 6.80 |
| CHEMBL171121 | — | — | 2 | 6.72 |
| CHEMBL355283 | — | — | 4 | 6.60 |
| CHEMBL173965 | — | — | 1 | 6.60 |
| CHEMBL440015 | — | — | 2 | 6.57 |
| CHEMBL170339 | — | — | 1 | 6.42 |
| CHEMBL354035 | — | — | 3 | 6.30 |
| CHEMBL354538 | — | — | 3 | 6.29 |
| CHEMBL367391 | — | — | 2 | 5.83 |
| CHEMBL171529 | — | — | 2 | 5.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL172524 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL172523 | — | IC50 | = | 11.6 | nM | 7.94 |
| CHEMBL169642 | — | IC50 | = | 12.9 | nM | 7.89 |
| CHEMBL358368 | — | IC50 | = | 14.2 | nM | 7.85 |
| CHEMBL2079586 | — | IC50 | = | 20.4 | nM | 7.69 |
| CHEMBL358368 | — | IC50 | = | 21.3 | nM | 7.67 |
| CHEMBL172523 | — | IC50 | = | 21.3 | nM | 7.67 |
| CHEMBL169814 | — | IC50 | = | 21.5 | nM | 7.67 |
| CHEMBL172523 | — | IC50 | = | 32.7 | nM | 7.49 |
| CHEMBL169814 | — | IC50 | = | 37.5 | nM | 7.43 |
| CHEMBL170876 | — | IC50 | = | 36.8 | nM | 7.43 |
| CHEMBL172524 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL172524 | — | IC50 | = | 65.3 | nM | 7.18 |
| CHEMBL169642 | — | IC50 | = | 71.4 | nM | 7.15 |
| CHEMBL170876 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL172115 | — | IC50 | = | 117.0 | nM | 6.93 |
| CHEMBL353466 | — | IC50 | = | 149.0 | nM | 6.83 |
| CHEMBL353469 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL370805 | COCAINE | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL171121 | — | IC50 | = | 191.0 | nM | 6.72 |
| CHEMBL172115 | — | IC50 | = | 204.0 | nM | 6.69 |
| CHEMBL172524 | — | IC50 | = | 207.0 | nM | 6.68 |
| CHEMBL353466 | — | IC50 | = | 239.0 | nM | 6.62 |
| CHEMBL173965 | — | IC50 | = | 249.0 | nM | 6.60 |
| CHEMBL355283 | — | IC50 | = | 251.0 | nM | 6.60 |
| CHEMBL440015 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL171121 | — | IC50 | = | 313.0 | nM | 6.50 |
| CHEMBL355283 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL170339 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL354035 | — | IC50 | = | 495.0 | nM | 6.30 |
| CHEMBL354538 | — | IC50 | = | 515.0 | nM | 6.29 |
| CHEMBL355283 | — | IC50 | = | 816.0 | nM | 6.09 |
| CHEMBL354035 | — | IC50 | = | 1160.0 | nM | 5.94 |
| CHEMBL440015 | — | IC50 | = | 1195.0 | nM | 5.92 |
| CHEMBL367391 | — | IC50 | = | 1480.0 | nM | 5.83 |
| CHEMBL354035 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL171529 | — | IC50 | = | 2010.0 | nM | 5.70 |
| CHEMBL354538 | — | IC50 | = | 2140.0 | nM | 5.67 |
| CHEMBL354538 | — | IC50 | = | 2510.0 | nM | 5.60 |
| CHEMBL355283 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL171529 | — | IC50 | = | 8820.0 | nM | 5.05 |
| CHEMBL367391 | — | IC50 | = | 11600.0 | nM | 4.94 |