Assay Detail
Binding
CHEMBL946207
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Inhibition of dopamine uptake at cloned DAT in rat brain synaptosome
39
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Studies on the structure-activity relationship of bicifadine analogs as monoamine transporter inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 39 | 5.78 | 6.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL448714 | — | — | 1 | 6.75 |
| CHEMBL452045 | — | — | 1 | 6.72 |
| CHEMBL592374 | AMITIFADINE | 2.0 | 2 | 6.58 |
| CHEMBL488638 | — | — | 1 | 6.48 |
| CHEMBL509158 | — | — | 1 | 6.48 |
| CHEMBL451785 | — | — | 1 | 6.44 |
| CHEMBL448893 | — | — | 1 | 6.40 |
| CHEMBL444992 | — | — | 1 | 6.38 |
| CHEMBL521058 | — | — | 1 | 6.30 |
| CHEMBL453327 | — | — | 1 | 6.11 |
| CHEMBL508171 | — | — | 1 | 5.82 |
| CHEMBL505313 | — | — | 1 | 5.64 |
| CHEMBL508156 | — | — | 1 | 5.62 |
| CHEMBL506040 | — | — | 1 | 5.62 |
| CHEMBL509214 | — | — | 1 | 5.60 |
| CHEMBL503383 | — | — | 1 | 5.57 |
| CHEMBL444247 | — | — | 1 | 5.48 |
| CHEMBL453576 | — | — | 1 | 5.47 |
| CHEMBL503444 | — | — | 1 | 5.41 |
| CHEMBL449514 | — | — | 1 | 5.21 |
| CHEMBL500739 | — | — | 1 | 5.12 |
| CHEMBL503805 | — | — | 1 | 5.09 |
| CHEMBL505382 | — | — | 1 | 5.09 |
| CHEMBL488473 | — | — | 1 | 5.06 |
| CHEMBL519552 | — | — | 1 | 5.05 |
| CHEMBL449052 | — | — | 1 | 5.04 |
| CHEMBL451504 | — | — | 1 | 5.02 |
| CHEMBL180101 | ESREBOXETINE | 3.0 | 1 | - |
| CHEMBL519717 | — | — | 1 | - |
| CHEMBL488639 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL448714 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL452045 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL592374 | AMITIFADINE | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL488638 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL509158 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL451785 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL592374 | AMITIFADINE | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL448893 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL444992 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL521058 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL453327 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL508171 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL505313 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL508156 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL506040 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL509214 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL503383 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL444247 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL453576 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL503444 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL449514 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL500739 | — | IC50 | = | 7500.0 | nM | 5.12 |
| CHEMBL503805 | — | IC50 | = | 8200.0 | nM | 5.09 |
| CHEMBL505382 | — | IC50 | = | 8200.0 | nM | 5.09 |
| CHEMBL488473 | — | IC50 | = | 8700.0 | nM | 5.06 |
| CHEMBL519552 | — | IC50 | = | 8900.0 | nM | 5.05 |
| CHEMBL449052 | — | IC50 | = | 9100.0 | nM | 5.04 |
| CHEMBL451504 | — | IC50 | = | 9500.0 | nM | 5.02 |
| CHEMBL486255 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL505812 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL454285 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL508896 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL449825 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL505742 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL452543 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL453328 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL488639 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL519717 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL180101 | ESREBOXETINE | IC50 | > | 10000.0 | nM | - |