Assay Detail
Binding
CHEMBL673205
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Binding affinity at the dopamine transporter using [125I]RTI-55 in rat caudate membranes.
29
Total Activities
29
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
Heteroaromatic analogs of 1-[2-(diphenylmethoxy)ethyl]- and 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines (GBR 12935 and GBR 12909) as high-affinity dopamine reuptake inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 7.77 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL160073 | — | — | 1 | 9.15 |
| CHEMBL159423 | — | — | 1 | 8.96 |
| CHEMBL351321 | — | — | 1 | 8.60 |
| CHEMBL26320 | — | — | 1 | 8.43 |
| CHEMBL159445 | — | — | 1 | 8.39 |
| CHEMBL346591 | — | — | 1 | 8.30 |
| CHEMBL164207 | — | — | 1 | 8.28 |
| CHEMBL164270 | — | — | 1 | 8.19 |
| CHEMBL159489 | — | — | 1 | 8.19 |
| CHEMBL163273 | — | — | 1 | 8.19 |
| CHEMBL162828 | — | — | 1 | 8.11 |
| CHEMBL163272 | — | — | 1 | 8.10 |
| CHEMBL349121 | — | — | 1 | 7.82 |
| CHEMBL164297 | — | — | 1 | 7.80 |
| CHEMBL162331 | — | — | 1 | 7.77 |
| CHEMBL349459 | — | — | 1 | 7.75 |
| CHEMBL159442 | — | — | 1 | 7.64 |
| CHEMBL159982 | — | — | 1 | 7.51 |
| CHEMBL159250 | — | — | 1 | 7.37 |
| CHEMBL164162 | — | — | 1 | 7.36 |
| CHEMBL163030 | — | — | 1 | 7.34 |
| CHEMBL434093 | — | — | 1 | 7.25 |
| CHEMBL163163 | — | — | 1 | 7.21 |
| CHEMBL163515 | — | — | 1 | 7.14 |
| CHEMBL159649 | — | — | 1 | 7.11 |
| CHEMBL159657 | — | — | 1 | 7.04 |
| CHEMBL346332 | — | — | 1 | 6.94 |
| CHEMBL349163 | — | — | 1 | 6.72 |
| CHEMBL350421 | — | — | 1 | 6.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL160073 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL159423 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL351321 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL26320 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL159445 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL346591 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL164207 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL164270 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL159489 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL163273 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL162828 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL163272 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL349121 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL164297 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL162331 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL349459 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL159442 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL159982 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL159250 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL164162 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL163030 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL434093 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL163163 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL163515 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL159649 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL159657 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL346332 | — | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL349163 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL350421 | — | IC50 | = | 199.0 | nM | 6.70 |