Assay Detail
Binding
CHEMBL878290
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity against dopamine transporter labelled with [125I]- RTI-55 in rat.
35
Total Activities
35
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
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 |
|---|---|---|---|
| Ki | 35 | 8.03 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL286991 | — | — | 1 | 9.05 |
| CHEMBL145903 | — | — | 1 | 9.04 |
| CHEMBL417660 | — | — | 1 | 8.67 |
| CHEMBL422499 | — | — | 1 | 8.64 |
| CHEMBL148441 | — | — | 1 | 8.60 |
| CHEMBL146370 | — | — | 1 | 8.60 |
| CHEMBL149437 | — | — | 1 | 8.57 |
| CHEMBL146372 | — | — | 1 | 8.54 |
| CHEMBL26477 | — | — | 1 | 8.52 |
| CHEMBL281594 | VANOXERINE | 3.0 | 1 | 8.43 |
| CHEMBL26320 | — | — | 1 | 8.43 |
| CHEMBL149013 | — | — | 1 | 8.42 |
| CHEMBL147933 | — | — | 1 | 8.38 |
| CHEMBL26478 | — | — | 1 | 8.36 |
| CHEMBL278242 | — | — | 1 | 8.31 |
| CHEMBL146255 | — | — | 1 | 8.31 |
| CHEMBL149565 | — | — | 1 | 8.24 |
| CHEMBL28821 | — | — | 1 | 8.21 |
| CHEMBL146259 | — | — | 1 | 8.15 |
| CHEMBL149622 | — | — | 1 | 8.08 |
| CHEMBL356783 | — | — | 1 | 8.00 |
| CHEMBL358521 | — | — | 1 | 7.94 |
| CHEMBL421948 | — | — | 1 | 7.91 |
| CHEMBL357295 | — | — | 1 | 7.86 |
| CHEMBL43124 | — | — | 1 | 7.82 |
| CHEMBL145942 | — | — | 1 | 7.82 |
| CHEMBL341692 | — | — | 1 | 7.74 |
| CHEMBL149014 | — | — | 1 | 7.72 |
| CHEMBL347517 | — | — | 1 | 7.64 |
| CHEMBL356380 | — | — | 1 | 7.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL286991 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL145903 | — | Ki | = | 0.92 | nM | 9.04 |
| CHEMBL417660 | — | Ki | = | 2.14 | nM | 8.67 |
| CHEMBL422499 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL148441 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL146370 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL149437 | — | Ki | = | 2.69 | nM | 8.57 |
| CHEMBL146372 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL26477 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL281594 | VANOXERINE | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL26320 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL149013 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL147933 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL26478 | — | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL146255 | — | Ki | = | 4.87 | nM | 8.31 |
| CHEMBL278242 | — | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL149565 | — | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL28821 | — | Ki | = | 6.09 | nM | 8.21 |
| CHEMBL146259 | — | Ki | = | 7.1 | nM | 8.15 |
| CHEMBL149622 | — | Ki | = | 8.4 | nM | 8.08 |
| CHEMBL356783 | — | Ki | = | 9.9 | nM | 8.00 |
| CHEMBL358521 | — | Ki | = | 11.6 | nM | 7.94 |
| CHEMBL421948 | — | Ki | = | 12.4 | nM | 7.91 |
| CHEMBL357295 | — | Ki | = | 13.7 | nM | 7.86 |
| CHEMBL43124 | — | Ki | = | 15.1 | nM | 7.82 |
| CHEMBL145942 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL341692 | — | Ki | = | 18.2 | nM | 7.74 |
| CHEMBL149014 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL347517 | — | Ki | = | 22.8 | nM | 7.64 |
| CHEMBL356380 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL146478 | — | Ki | = | 28.7 | nM | 7.54 |
| CHEMBL146321 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL283662 | — | Ki | = | 47.8 | nM | 7.32 |
| CHEMBL27907 | — | Ki | = | 208.0 | nM | 6.68 |
| CHEMBL146547 | — | Ki | = | 24800.0 | nM | 4.61 |