Assay Detail
Binding
CHEMBL670593
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of dopamine DA reuptake
40
Total Activities
40
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 | 40 | 7.39 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL344080 | — | — | 1 | 9.22 |
| CHEMBL423372 | — | — | 1 | 9.15 |
| CHEMBL142674 | — | — | 1 | 8.47 |
| CHEMBL143823 | — | — | 1 | 8.47 |
| CHEMBL26320 | — | — | 1 | 8.43 |
| CHEMBL281594 | VANOXERINE | 3.0 | 1 | 8.37 |
| CHEMBL142953 | — | — | 1 | 8.14 |
| CHEMBL357008 | — | — | 1 | 8.03 |
| CHEMBL140054 | — | — | 1 | 8.02 |
| CHEMBL143612 | — | — | 1 | 7.92 |
| CHEMBL142545 | — | — | 1 | 7.82 |
| CHEMBL344990 | — | — | 1 | 7.77 |
| CHEMBL142041 | — | — | 1 | 7.75 |
| CHEMBL143591 | — | — | 1 | 7.70 |
| CHEMBL344083 | — | — | 1 | 7.55 |
| CHEMBL141251 | — | — | 1 | 7.54 |
| CHEMBL142518 | — | — | 1 | 7.52 |
| CHEMBL142159 | — | — | 1 | 7.51 |
| CHEMBL342120 | — | — | 1 | 7.46 |
| CHEMBL140104 | — | — | 1 | 7.46 |
| CHEMBL102119 | — | — | 1 | 7.40 |
| CHEMBL141876 | — | — | 1 | 7.24 |
| CHEMBL142617 | — | — | 1 | 7.15 |
| CHEMBL356790 | — | — | 1 | 7.08 |
| CHEMBL142337 | — | — | 1 | 7.07 |
| CHEMBL143039 | — | — | 1 | 7.06 |
| CHEMBL342121 | — | — | 1 | 7.03 |
| CHEMBL142522 | — | — | 1 | 6.91 |
| CHEMBL142500 | — | — | 1 | 6.90 |
| CHEMBL358758 | — | — | 1 | 6.86 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL344080 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL423372 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL143823 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL142674 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL26320 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL281594 | VANOXERINE | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL142953 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL357008 | — | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL140054 | — | IC50 | = | 9.6 | nM | 8.02 |
| CHEMBL143612 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL142545 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL344990 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL142041 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL143591 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL344083 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL141251 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL142518 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL142159 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL342120 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL140104 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL102119 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL141876 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL142617 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL356790 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL142337 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL143039 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL342121 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL142522 | — | IC50 | = | 124.0 | nM | 6.91 |
| CHEMBL142500 | — | IC50 | = | 127.0 | nM | 6.90 |
| CHEMBL358758 | — | IC50 | = | 138.0 | nM | 6.86 |
| CHEMBL142861 | — | IC50 | = | 252.0 | nM | 6.60 |
| CHEMBL141882 | — | IC50 | = | 453.0 | nM | 6.34 |
| CHEMBL370805 | COCAINE | IC50 | = | 478.0 | nM | 6.32 |
| CHEMBL143846 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL143648 | — | IC50 | = | 545.0 | nM | 6.26 |
| CHEMBL142642 | — | IC50 | = | 651.0 | nM | 6.19 |
| CHEMBL348432 | — | IC50 | = | 1330.0 | nM | 5.88 |
| CHEMBL346409 | — | IC50 | = | 1640.0 | nM | 5.79 |
| CHEMBL143407 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL143750 | — | IC50 | > | 30000.0 | nM | - |