Assay Detail
Binding
CHEMBL670042
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Binding affinity against dopamine transporter using radioligand as [3H]GBR 12935
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Development of novel, potent, and selective dopamine reuptake inhibitors through alteration of the piperazine ring of 1-[2-(diphenylmethoxy)ethyl]-and 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines (GBR 12935 and GBR 12909).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 6.72 | 8.29 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL423372 | — | — | 1 | 8.29 |
| CHEMBL142953 | — | — | 1 | 8.10 |
| CHEMBL344080 | — | — | 1 | 8.07 |
| CHEMBL357008 | — | — | 1 | 7.70 |
| CHEMBL142041 | — | — | 1 | 7.57 |
| CHEMBL342120 | — | — | 1 | 7.48 |
| CHEMBL142337 | — | — | 1 | 7.44 |
| CHEMBL141876 | — | — | 1 | 7.13 |
| CHEMBL143591 | — | — | 1 | 6.99 |
| CHEMBL142518 | — | — | 1 | 6.97 |
| CHEMBL142522 | — | — | 1 | 6.96 |
| CHEMBL344990 | — | — | 1 | 6.84 |
| CHEMBL356790 | — | — | 1 | 6.77 |
| CHEMBL142159 | — | — | 1 | 6.65 |
| CHEMBL143039 | — | — | 1 | 6.54 |
| CHEMBL142500 | — | — | 1 | 6.13 |
| CHEMBL143648 | — | — | 1 | 6.08 |
| CHEMBL342121 | — | — | 1 | 6.06 |
| CHEMBL358758 | — | — | 1 | 6.00 |
| CHEMBL142642 | — | — | 1 | 5.87 |
| CHEMBL141882 | — | — | 1 | 5.84 |
| CHEMBL142861 | — | — | 1 | 5.76 |
| CHEMBL143846 | — | — | 1 | 5.01 |
| CHEMBL348432 | — | — | 1 | 5.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL423372 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL142953 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL344080 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL357008 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL142041 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL342120 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL142337 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL141876 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL143591 | — | IC50 | = | 103.0 | nM | 6.99 |
| CHEMBL142518 | — | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL142522 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL344990 | — | IC50 | = | 143.0 | nM | 6.84 |
| CHEMBL356790 | — | IC50 | = | 169.0 | nM | 6.77 |
| CHEMBL142159 | — | IC50 | = | 222.0 | nM | 6.65 |
| CHEMBL143039 | — | IC50 | = | 286.0 | nM | 6.54 |
| CHEMBL142500 | — | IC50 | = | 747.0 | nM | 6.13 |
| CHEMBL143648 | — | IC50 | = | 834.0 | nM | 6.08 |
| CHEMBL342121 | — | IC50 | = | 864.0 | nM | 6.06 |
| CHEMBL358758 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL142642 | — | IC50 | = | 1360.0 | nM | 5.87 |
| CHEMBL141882 | — | IC50 | = | 1460.0 | nM | 5.84 |
| CHEMBL142861 | — | IC50 | = | 1730.0 | nM | 5.76 |
| CHEMBL143846 | — | IC50 | = | 9780.0 | nM | 5.01 |
| CHEMBL348432 | — | IC50 | = | 9940.0 | nM | 5.00 |