Assay Detail
Functional
CHEMBL785239
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Reuptake inhibition of [3H]-labeled dopamine (DA) in rat.
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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
Oxygenated analogues of 1-[2-(Diphenylmethoxy)ethyl]- and 1-[2-[Bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines (GBR 12935 and GBR 12909) as potential extended-action cocaine-abuse therapeutic agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 8.02 | 8.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL26477 | — | — | 1 | 8.46 |
| CHEMBL26478 | — | — | 1 | 8.44 |
| CHEMBL26320 | — | — | 1 | 8.43 |
| CHEMBL148441 | — | — | 1 | 8.40 |
| CHEMBL278242 | — | — | 1 | 8.29 |
| CHEMBL149622 | — | — | 1 | 8.27 |
| CHEMBL417660 | — | — | 1 | 8.25 |
| CHEMBL146259 | — | — | 1 | 8.25 |
| CHEMBL149565 | — | — | 1 | 8.24 |
| CHEMBL356380 | — | — | 1 | 8.19 |
| CHEMBL149013 | — | — | 1 | 8.19 |
| CHEMBL146547 | — | — | 1 | 8.17 |
| CHEMBL146370 | — | — | 1 | 8.17 |
| CHEMBL28821 | — | — | 1 | 8.15 |
| CHEMBL146372 | — | — | 1 | 8.15 |
| CHEMBL145903 | — | — | 1 | 8.15 |
| CHEMBL281594 | VANOXERINE | 3.0 | 1 | 8.14 |
| CHEMBL421948 | — | — | 1 | 8.13 |
| CHEMBL149437 | — | — | 1 | 8.13 |
| CHEMBL149014 | — | — | 1 | 8.06 |
| CHEMBL356783 | — | — | 1 | 8.06 |
| CHEMBL422499 | — | — | 1 | 8.05 |
| CHEMBL146255 | — | — | 1 | 8.03 |
| CHEMBL147933 | — | — | 1 | 8.01 |
| CHEMBL43124 | — | — | 1 | 8.01 |
| CHEMBL286991 | — | — | 1 | 7.96 |
| CHEMBL358521 | — | — | 1 | 7.94 |
| CHEMBL146321 | — | — | 1 | 7.82 |
| CHEMBL145942 | — | — | 1 | 7.76 |
| CHEMBL357295 | — | — | 1 | 7.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL26477 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL26478 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL26320 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL148441 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL278242 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL149622 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL417660 | — | IC50 | = | 5.57 | nM | 8.25 |
| CHEMBL146259 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL149565 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL356380 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL149013 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL146547 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL146370 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL145903 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL146372 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL28821 | — | IC50 | = | 7.03 | nM | 8.15 |
| CHEMBL281594 | VANOXERINE | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL421948 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL149437 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL149014 | — | IC50 | = | 8.7 | nM | 8.06 |
| CHEMBL356783 | — | IC50 | = | 8.7 | nM | 8.06 |
| CHEMBL422499 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL146255 | — | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL147933 | — | IC50 | = | 9.7 | nM | 8.01 |
| CHEMBL43124 | — | IC50 | = | 9.8 | nM | 8.01 |
| CHEMBL286991 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL358521 | — | IC50 | = | 11.4 | nM | 7.94 |
| CHEMBL146321 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL145942 | — | IC50 | = | 17.4 | nM | 7.76 |
| CHEMBL357295 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL146478 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL283662 | — | IC50 | = | 41.6 | nM | 7.38 |
| CHEMBL347517 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL27907 | — | IC50 | = | 329.0 | nM | 6.48 |