Assay Detail
Functional
CHEMBL672113
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Reuptake inhibition at the dopamine transporter labeled with radioligand [3H]dopamine on synaptosomes obtained from rat caudate.
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Tissue | Brain |
| 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 | 37 | 7.60 | 8.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL26320 | — | — | 1 | 8.43 |
| CHEMBL163980 | — | — | 1 | 8.21 |
| CHEMBL159967 | — | — | 1 | 8.14 |
| CHEMBL281594 | VANOXERINE | 3.0 | 1 | 8.14 |
| CHEMBL159319 | — | — | 1 | 8.10 |
| CHEMBL351321 | — | — | 1 | 8.09 |
| CHEMBL163273 | — | — | 1 | 8.07 |
| CHEMBL159423 | — | — | 1 | 8.06 |
| CHEMBL346591 | — | — | 1 | 8.02 |
| CHEMBL164207 | — | — | 1 | 8.01 |
| CHEMBL159489 | — | — | 1 | 8.00 |
| CHEMBL286991 | — | — | 1 | 7.96 |
| CHEMBL159320 | — | — | 1 | 7.89 |
| CHEMBL160073 | — | — | 1 | 7.89 |
| CHEMBL164037 | — | — | 1 | 7.84 |
| CHEMBL159442 | — | — | 1 | 7.77 |
| CHEMBL164270 | — | — | 1 | 7.73 |
| CHEMBL349459 | — | — | 1 | 7.72 |
| CHEMBL159608 | — | — | 1 | 7.70 |
| CHEMBL349121 | — | — | 1 | 7.70 |
| CHEMBL162331 | — | — | 1 | 7.66 |
| CHEMBL162828 | — | — | 1 | 7.60 |
| CHEMBL163272 | — | — | 1 | 7.52 |
| CHEMBL159250 | — | — | 1 | 7.50 |
| CHEMBL159445 | — | — | 1 | 7.47 |
| CHEMBL163030 | — | — | 1 | 7.43 |
| CHEMBL159657 | — | — | 1 | 7.38 |
| CHEMBL164162 | — | — | 1 | 7.19 |
| CHEMBL159649 | — | — | 1 | 7.16 |
| CHEMBL163163 | — | — | 1 | 7.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL26320 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL163980 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL281594 | VANOXERINE | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL159967 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL159319 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL351321 | — | IC50 | = | 8.1 | nM | 8.09 |
| CHEMBL163273 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL159423 | — | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL346591 | — | IC50 | = | 9.6 | nM | 8.02 |
| CHEMBL164207 | — | IC50 | = | 9.7 | nM | 8.01 |
| CHEMBL159489 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL286991 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL159320 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL160073 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL164037 | — | IC50 | = | 14.5 | nM | 7.84 |
| CHEMBL159442 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL164270 | — | IC50 | = | 18.6 | nM | 7.73 |
| CHEMBL349459 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL159608 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL349121 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL162331 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL162828 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL163272 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL159250 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL159445 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL163030 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL159657 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL164162 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL159649 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL163163 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL164297 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL434093 | — | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL163515 | — | IC50 | = | 111.0 | nM | 6.96 |
| CHEMBL349163 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL350421 | — | IC50 | = | 192.0 | nM | 6.72 |
| CHEMBL159982 | — | IC50 | = | 312.0 | nM | 6.51 |
| CHEMBL346332 | — | IC50 | = | 406.0 | nM | 6.39 |