Assay Detail
Binding
CHEMBL952559
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Inhibition of dopamine transporter-mediated [3H]dopamine uptake in Wistar rat striatal synaptosomes by liquid scintillation spectrometry
40
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Subcellular | Synaptosomes |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Effects of various isoquinoline alkaloids on in vitro 3H-dopamine uptake by rat striatal synaptosomes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 40 | 5.02 | 6.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL59 | DOPAMINE | 4.0 | 1 | 6.70 |
| CHEMBL273575 | NOMIFENSINE | 4.0 | 1 | 6.70 |
| CHEMBL401798 | ANONAINE | — | 1 | 6.10 |
| CHEMBL418995 | AMINEPTINE | 4.0 | 1 | 6.00 |
| CHEMBL450147 | DIMETHYLGRISABINE | — | 1 | 5.96 |
| CHEMBL257745 | NORSTEPHALAGINE | — | 1 | 5.85 |
| CHEMBL508011 | ISOPILINE | — | 1 | 5.60 |
| CHEMBL452904 | ANTIOQUINE | — | 1 | 5.47 |
| CHEMBL464525 | OBABERINE | — | 1 | 5.41 |
| CHEMBL504757 | ISOTETRANDRINE | -1.0 | 1 | 5.38 |
| CHEMBL612 | DEXTROAMPHETAMINE | 4.0 | 1 | 5.31 |
| CHEMBL501861 | — | — | 1 | 5.24 |
| CHEMBL257746 | ANOLOBINE | — | 1 | 5.09 |
| CHEMBL509855 | HOMOAROMOLINE | — | 1 | 4.96 |
| CHEMBL508081 | SECOCULARIDINE | — | 1 | 4.87 |
| CHEMBL446211 | L-COCLAURINE | — | 1 | 4.85 |
| CHEMBL487388 | NORBOLDINE | — | 1 | 4.78 |
| CHEMBL447018 | DIMETHYLPSEUDOXANDRINE | — | 1 | 4.70 |
| CHEMBL257958 | MELOSMINE | — | 1 | 4.63 |
| CHEMBL455632 | SECOCULARINE | — | 1 | 4.55 |
| CHEMBL37736 | LIRIODENINE | — | 1 | 4.51 |
| CHEMBL486823 | — | — | 1 | 4.50 |
| CHEMBL510812 | ISOCRASSIFOLINE | — | 1 | 4.44 |
| CHEMBL453038 | NORARMEPAVINE | — | 1 | 4.43 |
| CHEMBL455633 | CULARIDINE | — | 1 | 4.38 |
| CHEMBL486824 | — | — | 1 | 4.33 |
| CHEMBL519236 | — | — | 1 | 4.33 |
| CHEMBL452510 | BREOGANINE | — | 1 | 4.25 |
| CHEMBL487016 | BELEMINE | — | 1 | 4.21 |
| CHEMBL504801 | PAMPULHAMINE | — | 1 | 4.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL59 | DOPAMINE | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL273575 | NOMIFENSINE | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL401798 | ANONAINE | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL418995 | AMINEPTINE | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL450147 | DIMETHYLGRISABINE | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL257745 | NORSTEPHALAGINE | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL508011 | ISOPILINE | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL452904 | ANTIOQUINE | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL464525 | OBABERINE | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL504757 | ISOTETRANDRINE | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL612 | DEXTROAMPHETAMINE | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL501861 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL257746 | ANOLOBINE | IC50 | = | 8100.0 | nM | 5.09 |
| CHEMBL509855 | HOMOAROMOLINE | IC50 | = | 10900.0 | nM | 4.96 |
| CHEMBL508081 | SECOCULARIDINE | IC50 | = | 13400.0 | nM | 4.87 |
| CHEMBL446211 | L-COCLAURINE | IC50 | = | 14100.0 | nM | 4.85 |
| CHEMBL487388 | NORBOLDINE | IC50 | = | 16500.0 | nM | 4.78 |
| CHEMBL447018 | DIMETHYLPSEUDOXANDRINE | IC50 | = | 20100.0 | nM | 4.70 |
| CHEMBL257958 | MELOSMINE | IC50 | = | 23600.0 | nM | 4.63 |
| CHEMBL455632 | SECOCULARINE | IC50 | = | 28200.0 | nM | 4.55 |
| CHEMBL37736 | LIRIODENINE | IC50 | = | 31200.0 | nM | 4.51 |
| CHEMBL486823 | — | IC50 | = | 31800.0 | nM | 4.50 |
| CHEMBL510812 | ISOCRASSIFOLINE | IC50 | = | 36200.0 | nM | 4.44 |
| CHEMBL453038 | NORARMEPAVINE | IC50 | = | 37000.0 | nM | 4.43 |
| CHEMBL455633 | CULARIDINE | IC50 | = | 41200.0 | nM | 4.38 |
| CHEMBL486824 | — | IC50 | = | 46600.0 | nM | 4.33 |
| CHEMBL519236 | — | IC50 | = | 46400.0 | nM | 4.33 |
| CHEMBL452510 | BREOGANINE | IC50 | = | 56500.0 | nM | 4.25 |
| CHEMBL487016 | BELEMINE | IC50 | = | 61400.0 | nM | 4.21 |
| CHEMBL504801 | PAMPULHAMINE | IC50 | = | 84200.0 | nM | 4.08 |
| CHEMBL510777 | SARCOCAPNIDINE | IC50 | = | 85500.0 | nM | 4.07 |
| CHEMBL452777 | OXOSARCOPHYLLINE | IC50 | > | 100000.0 | nM | - |
| CHEMBL488204 | SAUVEOLINE | IC50 | > | 100000.0 | nM | - |
| CHEMBL510574 | OXOCULARINE | IC50 | > | 100000.0 | nM | - |
| CHEMBL452776 | CELTISINE | IC50 | > | 100000.0 | nM | - |
| CHEMBL452512 | CLAVICULINE | IC50 | > | 100000.0 | nM | - |
| CHEMBL450834 | SECOLUCIDINE | IC50 | > | 100000.0 | nM | - |
| CHEMBL450155 | SECANTIOQUINE | IC50 | > | 100000.0 | nM | - |
| CHEMBL446266 | HETEROPSINE | IC50 | > | 100000.0 | nM | - |
| CHEMBL510090 | LYSICAMINE | IC50 | > | 100000.0 | nM | - |