Assay Detail
Binding
CHEMBL675224
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Inhibition of dopamine uptake into rat striatal tissue, using [3H]- dopamine 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 | 6.14 | 7.53 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL358368 | — | — | 2 | 7.53 |
| CHEMBL169814 | — | — | 2 | 7.47 |
| CHEMBL172524 | — | — | 4 | 7.46 |
| CHEMBL2079586 | — | — | 1 | 7.29 |
| CHEMBL172523 | — | — | 3 | 7.24 |
| CHEMBL169642 | — | — | 2 | 7.17 |
| CHEMBL170876 | — | — | 2 | 6.73 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 6.39 |
| CHEMBL172115 | — | — | 2 | 6.37 |
| CHEMBL353469 | — | — | 1 | 6.15 |
| CHEMBL353466 | — | — | 2 | 6.12 |
| CHEMBL171121 | — | — | 2 | 6.08 |
| CHEMBL355283 | — | — | 4 | 6.06 |
| CHEMBL354538 | — | — | 3 | 5.96 |
| CHEMBL170339 | — | — | 1 | 5.84 |
| CHEMBL440015 | — | — | 2 | 5.83 |
| CHEMBL173965 | — | — | 1 | 5.82 |
| CHEMBL354035 | — | — | 3 | 5.65 |
| CHEMBL171529 | — | — | 2 | 5.18 |
| CHEMBL367391 | — | — | 2 | 5.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL358368 | — | IC50 | = | 29.3 | nM | 7.53 |
| CHEMBL169814 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL172524 | — | IC50 | = | 34.9 | nM | 7.46 |
| CHEMBL2079586 | — | IC50 | = | 51.3 | nM | 7.29 |
| CHEMBL358368 | — | IC50 | = | 56.3 | nM | 7.25 |
| CHEMBL172523 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL169642 | — | IC50 | = | 68.3 | nM | 7.17 |
| CHEMBL172523 | — | IC50 | = | 93.6 | nM | 7.03 |
| CHEMBL169814 | — | IC50 | = | 97.5 | nM | 7.01 |
| CHEMBL172523 | — | IC50 | = | 98.7 | nM | 7.01 |
| CHEMBL170876 | — | IC50 | = | 186.0 | nM | 6.73 |
| CHEMBL172524 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL170876 | — | IC50 | = | 283.0 | nM | 6.55 |
| CHEMBL172524 | — | IC50 | = | 348.0 | nM | 6.46 |
| CHEMBL169642 | — | IC50 | = | 375.0 | nM | 6.43 |
| CHEMBL370805 | COCAINE | IC50 | = | 404.0 | nM | 6.39 |
| CHEMBL172115 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL172524 | — | IC50 | = | 593.0 | nM | 6.23 |
| CHEMBL353469 | — | IC50 | = | 704.0 | nM | 6.15 |
| CHEMBL353466 | — | IC50 | = | 758.0 | nM | 6.12 |
| CHEMBL353466 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL171121 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL355283 | — | IC50 | = | 875.0 | nM | 6.06 |
| CHEMBL172115 | — | IC50 | = | 960.0 | nM | 6.02 |
| CHEMBL171121 | — | IC50 | = | 980.0 | nM | 6.01 |
| CHEMBL354538 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL170339 | — | IC50 | = | 1430.0 | nM | 5.84 |
| CHEMBL440015 | — | IC50 | = | 1480.0 | nM | 5.83 |
| CHEMBL173965 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL355283 | — | IC50 | = | 2220.0 | nM | 5.65 |
| CHEMBL354035 | — | IC50 | = | 2260.0 | nM | 5.65 |
| CHEMBL354538 | — | IC50 | = | 2750.0 | nM | 5.56 |
| CHEMBL355283 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL354538 | — | IC50 | = | 4330.0 | nM | 5.36 |
| CHEMBL354035 | — | IC50 | = | 5550.0 | nM | 5.26 |
| CHEMBL440015 | — | IC50 | = | 5930.0 | nM | 5.23 |
| CHEMBL171529 | — | IC50 | = | 6560.0 | nM | 5.18 |
| CHEMBL354035 | — | IC50 | = | 7120.0 | nM | 5.15 |
| CHEMBL367391 | — | IC50 | = | 7860.0 | nM | 5.11 |
| CHEMBL355283 | — | IC50 | = | 8850.0 | nM | 5.05 |
| CHEMBL171529 | — | IC50 | = | 29300.0 | nM | 4.53 |
| CHEMBL367391 | — | IC50 | = | 36600.0 | nM | 4.44 |