Assay Detail
Binding
CHEMBL806539
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Inhibition of [3H]5-HT reuptake at rat serotonin transporter
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 serotonin transporter (CHEMBL313) ↗| 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 | 5.80 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL142861 | — | — | 1 | 7.70 |
| CHEMBL281594 | VANOXERINE | 3.0 | 1 | 7.14 |
| CHEMBL142674 | — | — | 1 | 6.95 |
| CHEMBL143823 | — | — | 1 | 6.63 |
| CHEMBL102119 | — | — | 1 | 6.56 |
| CHEMBL26320 | — | — | 1 | 6.54 |
| CHEMBL370805 | COCAINE | 4.0 | 1 | 6.52 |
| CHEMBL143750 | — | — | 1 | 6.44 |
| CHEMBL140104 | — | — | 1 | 6.42 |
| CHEMBL142545 | — | — | 1 | 6.34 |
| CHEMBL344080 | — | — | 1 | 6.30 |
| CHEMBL142159 | — | — | 1 | 6.07 |
| CHEMBL423372 | — | — | 1 | 6.01 |
| CHEMBL344083 | — | — | 1 | 5.93 |
| CHEMBL346409 | — | — | 1 | 5.87 |
| CHEMBL142617 | — | — | 1 | 5.85 |
| CHEMBL357008 | — | — | 1 | 5.83 |
| CHEMBL342121 | — | — | 1 | 5.80 |
| CHEMBL143612 | — | — | 1 | 5.77 |
| CHEMBL140054 | — | — | 1 | 5.76 |
| CHEMBL356790 | — | — | 1 | 5.72 |
| CHEMBL344990 | — | — | 1 | 5.68 |
| CHEMBL142041 | — | — | 1 | 5.61 |
| CHEMBL348432 | — | — | 1 | 5.60 |
| CHEMBL143591 | — | — | 1 | 5.57 |
| CHEMBL141876 | — | — | 1 | 5.54 |
| CHEMBL143039 | — | — | 1 | 5.50 |
| CHEMBL142500 | — | — | 1 | 5.49 |
| CHEMBL142337 | — | — | 1 | 5.37 |
| CHEMBL342120 | — | — | 1 | 5.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL142861 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL281594 | VANOXERINE | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL142674 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL143823 | — | IC50 | = | 234.0 | nM | 6.63 |
| CHEMBL102119 | — | IC50 | = | 278.0 | nM | 6.56 |
| CHEMBL26320 | — | IC50 | = | 289.0 | nM | 6.54 |
| CHEMBL370805 | COCAINE | IC50 | = | 304.0 | nM | 6.52 |
| CHEMBL143750 | — | IC50 | = | 361.0 | nM | 6.44 |
| CHEMBL140104 | — | IC50 | = | 376.0 | nM | 6.42 |
| CHEMBL142545 | — | IC50 | = | 459.0 | nM | 6.34 |
| CHEMBL344080 | — | IC50 | = | 503.0 | nM | 6.30 |
| CHEMBL142159 | — | IC50 | = | 857.0 | nM | 6.07 |
| CHEMBL423372 | — | IC50 | = | 986.0 | nM | 6.01 |
| CHEMBL344083 | — | IC50 | = | 1180.0 | nM | 5.93 |
| CHEMBL346409 | — | IC50 | = | 1340.0 | nM | 5.87 |
| CHEMBL142617 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL357008 | — | IC50 | = | 1480.0 | nM | 5.83 |
| CHEMBL342121 | — | IC50 | = | 1590.0 | nM | 5.80 |
| CHEMBL143612 | — | IC50 | = | 1710.0 | nM | 5.77 |
| CHEMBL140054 | — | IC50 | = | 1730.0 | nM | 5.76 |
| CHEMBL356790 | — | IC50 | = | 1890.0 | nM | 5.72 |
| CHEMBL344990 | — | IC50 | = | 2080.0 | nM | 5.68 |
| CHEMBL142041 | — | IC50 | = | 2450.0 | nM | 5.61 |
| CHEMBL348432 | — | IC50 | = | 2530.0 | nM | 5.60 |
| CHEMBL143591 | — | IC50 | = | 2680.0 | nM | 5.57 |
| CHEMBL141876 | — | IC50 | = | 2860.0 | nM | 5.54 |
| CHEMBL143039 | — | IC50 | = | 3150.0 | nM | 5.50 |
| CHEMBL142500 | — | IC50 | = | 3210.0 | nM | 5.49 |
| CHEMBL142337 | — | IC50 | = | 4240.0 | nM | 5.37 |
| CHEMBL342120 | — | IC50 | = | 6220.0 | nM | 5.21 |
| CHEMBL143846 | — | IC50 | = | 6830.0 | nM | 5.17 |
| CHEMBL142518 | — | IC50 | = | 8940.0 | nM | 5.05 |
| CHEMBL142522 | — | IC50 | = | 9570.0 | nM | 5.02 |
| CHEMBL143407 | — | IC50 | = | 12200.0 | nM | 4.91 |
| CHEMBL142642 | — | IC50 | = | 14300.0 | nM | 4.84 |
| CHEMBL141251 | — | IC50 | = | 20100.0 | nM | 4.70 |
| CHEMBL358758 | — | IC50 | = | 25300.0 | nM | 4.60 |
| CHEMBL142953 | — | IC50 | = | 34100.0 | nM | 4.47 |
| CHEMBL143648 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL141882 | — | IC50 | > | 10000.0 | nM | - |