Assay Detail
Functional
CHEMBL789207
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of dopamine (DA) uptake into rat brain synaptosomes
23
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Subcellular | Synaptosomes |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Pyrroloisoquinoline antidepressants. Potent, enantioselective inhibition of tetrabenazine-induced ptosis and neuronal uptake of norepinephrine, dopamine, and serotonin.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 23 | 7.61 | 9.07 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2093944 | — | — | 1 | 9.07 |
| CHEMBL171474 | — | — | 1 | 9.00 |
| CHEMBL540617 | — | — | 1 | 8.77 |
| CHEMBL558387 | — | — | 1 | 8.36 |
| CHEMBL539081 | — | — | 1 | 8.29 |
| CHEMBL538310 | — | — | 1 | 8.28 |
| CHEMBL553692 | — | — | 1 | 8.00 |
| CHEMBL131724 | — | — | 1 | 7.95 |
| CHEMBL287257 | DICLOFENSINE | 2.0 | 1 | 7.84 |
| CHEMBL1743811 | — | — | 1 | 7.52 |
| CHEMBL284305 | — | — | 1 | 7.43 |
| CHEMBL2093945 | — | — | 1 | 7.26 |
| CHEMBL556545 | — | — | 1 | 7.14 |
| CHEMBL273575 | NOMIFENSINE | 4.0 | 1 | 7.10 |
| CHEMBL536947 | — | — | 1 | 7.03 |
| CHEMBL2093943 | — | — | 2 | 6.80 |
| CHEMBL1696 | DESIPRAMINE HYDROCHLORIDE | 4.0 | 1 | 5.18 |
| CHEMBL2094040 | — | — | 1 | - |
| CHEMBL172809 | — | — | 1 | - |
| CHEMBL1692 | IMIPRAMINE HYDROCHLORIDE | 4.0 | 1 | - |
| CHEMBL537398 | — | — | 1 | - |
| CHEMBL6437 | MIANSERIN | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2093944 | — | Ki | = | 0.86 | nM | 9.07 |
| CHEMBL171474 | — | Ki | = | 0.99 | nM | 9.00 |
| CHEMBL540617 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL558387 | — | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL539081 | — | Ki | = | 5.1 | nM | 8.29 |
| CHEMBL538310 | — | Ki | = | 5.2 | nM | 8.28 |
| CHEMBL553692 | — | Ki | = | 10.1 | nM | 8.00 |
| CHEMBL131724 | — | Ki | = | 11.3 | nM | 7.95 |
| CHEMBL287257 | DICLOFENSINE | Ki | = | 14.6 | nM | 7.84 |
| CHEMBL1743811 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL284305 | — | Ki | = | 36.8 | nM | 7.43 |
| CHEMBL2093945 | — | Ki | = | 54.3 | nM | 7.26 |
| CHEMBL556545 | — | Ki | = | 71.9 | nM | 7.14 |
| CHEMBL273575 | NOMIFENSINE | Ki | = | 79.0 | nM | 7.10 |
| CHEMBL536947 | — | Ki | = | 94.2 | nM | 7.03 |
| CHEMBL2093943 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL2093943 | — | Ki | = | 1345.0 | nM | 5.87 |
| CHEMBL1696 | DESIPRAMINE HYDROCHLORIDE | Ki | = | 6532.0 | nM | 5.18 |
| CHEMBL2094040 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL172809 | — | Ki | > | 500.0 | nM | - |
| CHEMBL1692 | IMIPRAMINE HYDROCHLORIDE | Ki | > | 10000.0 | nM | - |
| CHEMBL537398 | — | Ki | > | 100.0 | nM | - |
| CHEMBL6437 | MIANSERIN | Ki | > | 10000.0 | nM | - |