Assay Detail
Binding
CHEMBL670108
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Inhibition of 3[H] WIN-35 428 binding to Dopamine transporter (DAT)
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Expansion of structure-activity studies of piperidine analogues of 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazine (GBR 12935) compounds by altering substitutions in the N-benzyl moiety and behavioral pharmacology of selected molecules.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 7.80 | 9.02 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL36074 | — | — | 1 | 9.02 |
| CHEMBL158427 | — | — | 1 | 8.53 |
| CHEMBL348100 | — | — | 1 | 8.39 |
| CHEMBL159128 | — | — | 1 | 8.35 |
| CHEMBL423061 | — | — | 1 | 8.09 |
| CHEMBL157757 | — | — | 1 | 7.94 |
| CHEMBL160812 | — | — | 1 | 7.84 |
| CHEMBL440191 | — | — | 1 | 7.71 |
| CHEMBL159184 | — | — | 1 | 7.57 |
| CHEMBL158832 | — | — | 1 | 7.20 |
| CHEMBL160897 | — | — | 1 | 7.19 |
| CHEMBL160559 | — | — | 1 | 6.95 |
| CHEMBL160488 | — | — | 1 | 6.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL36074 | — | IC50 | = | 0.96 | nM | 9.02 |
| CHEMBL158427 | — | IC50 | = | 2.96 | nM | 8.53 |
| CHEMBL348100 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL159128 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL423061 | — | IC50 | = | 8.23 | nM | 8.09 |
| CHEMBL157757 | — | IC50 | = | 11.6 | nM | 7.94 |
| CHEMBL160812 | — | IC50 | = | 14.3 | nM | 7.84 |
| CHEMBL440191 | — | IC50 | = | 19.6 | nM | 7.71 |
| CHEMBL159184 | — | IC50 | = | 26.9 | nM | 7.57 |
| CHEMBL158832 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL160897 | — | IC50 | = | 65.1 | nM | 7.19 |
| CHEMBL160559 | — | IC50 | = | 113.0 | nM | 6.95 |
| CHEMBL160488 | — | IC50 | = | 240.0 | nM | 6.62 |