Assay Detail
Functional
CHEMBL789206
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Inhibition of norepinephrine (NE) 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 |
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 | 8.50 | 9.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL540617 | — | — | 1 | 9.80 |
| CHEMBL2093944 | — | — | 1 | 9.70 |
| CHEMBL558387 | — | — | 1 | 9.43 |
| CHEMBL131724 | — | — | 1 | 9.22 |
| CHEMBL1696 | DESIPRAMINE HYDROCHLORIDE | 4.0 | 1 | 9.19 |
| CHEMBL171474 | — | — | 1 | 9.17 |
| CHEMBL539081 | — | — | 1 | 9.13 |
| CHEMBL538310 | — | — | 1 | 9.10 |
| CHEMBL553692 | — | — | 1 | 9.09 |
| CHEMBL2093945 | — | — | 1 | 9.02 |
| CHEMBL284305 | — | — | 1 | 8.54 |
| CHEMBL536947 | — | — | 1 | 8.47 |
| CHEMBL556545 | — | — | 1 | 8.47 |
| CHEMBL273575 | NOMIFENSINE | 4.0 | 1 | 8.42 |
| CHEMBL287257 | DICLOFENSINE | 2.0 | 1 | 8.36 |
| CHEMBL1743811 | — | — | 1 | 8.00 |
| CHEMBL1692 | IMIPRAMINE HYDROCHLORIDE | 4.0 | 1 | 7.92 |
| CHEMBL172809 | — | — | 1 | 7.70 |
| CHEMBL6437 | MIANSERIN | 4.0 | 1 | 7.58 |
| CHEMBL2093943 | — | — | 2 | 7.19 |
| CHEMBL537398 | — | — | 1 | 7.00 |
| CHEMBL2094040 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL540617 | — | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL2093944 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL558387 | — | Ki | = | 0.37 | nM | 9.43 |
| CHEMBL131724 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL1696 | DESIPRAMINE HYDROCHLORIDE | Ki | = | 0.65 | nM | 9.19 |
| CHEMBL171474 | — | Ki | = | 0.68 | nM | 9.17 |
| CHEMBL539081 | — | Ki | = | 0.74 | nM | 9.13 |
| CHEMBL538310 | — | Ki | = | 0.79 | nM | 9.10 |
| CHEMBL553692 | — | Ki | = | 0.81 | nM | 9.09 |
| CHEMBL2093945 | — | Ki | = | 0.95 | nM | 9.02 |
| CHEMBL284305 | — | Ki | = | 2.89 | nM | 8.54 |
| CHEMBL536947 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL556545 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL273575 | NOMIFENSINE | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL287257 | DICLOFENSINE | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL1743811 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL1692 | IMIPRAMINE HYDROCHLORIDE | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL172809 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL6437 | MIANSERIN | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL2093943 | — | Ki | = | 64.9 | nM | 7.19 |
| CHEMBL537398 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL2093943 | — | Ki | = | 411.0 | nM | 6.39 |
| CHEMBL2094040 | — | Ki | > | 100.0 | nM | - |