Assay Detail
Binding
CHEMBL1176113
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Inhibition of [3H]dopamine reuptake at human DAT expressed in HEK293 cells after 90 mins by scintillation counting
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent dopamine transporter (CHEMBL238) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and characterization of in vitro and in vivo profiles of hydroxybupropion analogues: aids to smoking cessation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 5.88 | 7.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1173597 | — | — | 1 | 7.52 |
| CHEMBL1173428 | — | — | 1 | 7.16 |
| CHEMBL1173772 | — | — | 1 | 6.69 |
| CHEMBL1173354 | — | — | 1 | 6.54 |
| CHEMBL1173771 | — | — | 1 | 6.34 |
| CHEMBL1172929 | — | — | 1 | 6.20 |
| CHEMBL894 | BUPROPION | 4.0 | 1 | 6.18 |
| CHEMBL1170441 | — | — | 1 | 6.08 |
| CHEMBL1173429 | — | — | 1 | 5.99 |
| CHEMBL1173274 | — | — | 1 | 5.97 |
| CHEMBL1173275 | — | — | 1 | 5.86 |
| CHEMBL1173427 | — | — | 1 | 5.67 |
| CHEMBL1173277 | — | — | 1 | 5.58 |
| CHEMBL1173598 | — | — | 1 | 5.54 |
| CHEMBL1173276 | — | — | 1 | 5.48 |
| CHEMBL1171260 | — | — | 1 | 5.47 |
| CHEMBL1173353 | — | — | 1 | 5.38 |
| CHEMBL1173430 | — | — | 1 | 5.08 |
| CHEMBL1173770 | — | — | 1 | 5.00 |
| CHEMBL1173280 | — | — | 1 | 4.92 |
| CHEMBL1173279 | — | — | 1 | 4.80 |
| CHEMBL1173599 | — | — | 1 | - |
| CHEMBL1173701 | — | — | 1 | - |
| CHEMBL1173600 | — | — | 1 | - |
| CHEMBL1173355 | — | — | 1 | - |
| CHEMBL1172928 | RADAFAXINE | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1173597 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL1173428 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL1173772 | — | IC50 | = | 204.0 | nM | 6.69 |
| CHEMBL1173354 | — | IC50 | = | 285.0 | nM | 6.54 |
| CHEMBL1173771 | — | IC50 | = | 453.0 | nM | 6.34 |
| CHEMBL1172929 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL894 | BUPROPION | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL1170441 | — | IC50 | = | 832.0 | nM | 6.08 |
| CHEMBL1173429 | — | IC50 | = | 1020.0 | nM | 5.99 |
| CHEMBL1173274 | — | IC50 | = | 1065.0 | nM | 5.97 |
| CHEMBL1173275 | — | IC50 | = | 1380.0 | nM | 5.86 |
| CHEMBL1173427 | — | IC50 | = | 2140.0 | nM | 5.67 |
| CHEMBL1173277 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL1173598 | — | IC50 | = | 2870.0 | nM | 5.54 |
| CHEMBL1173276 | — | IC50 | = | 3340.0 | nM | 5.48 |
| CHEMBL1171260 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL1173353 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL1173430 | — | IC50 | = | 8250.0 | nM | 5.08 |
| CHEMBL1173770 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL1173280 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL1173279 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL1173599 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1173701 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1173600 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1173355 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1172928 | RADAFAXINE | IC50 | > | 100000.0 | nM | - |