Assay Detail
Binding
CHEMBL944162
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Displacement of [3H]DA from rat DAT
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Sodium-dependent dopamine transporter (CHEMBL338) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Advances in development of dopaminergic aporphinoids.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 4.81 | 6.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL401798 | ANONAINE | — | 1 | 6.10 |
| CHEMBL257745 | NORSTEPHALAGINE | — | 1 | 5.85 |
| CHEMBL508011 | ISOPILINE | — | 1 | 5.60 |
| CHEMBL257746 | ANOLOBINE | — | 1 | 5.09 |
| CHEMBL487388 | NORBOLDINE | — | 1 | 4.78 |
| CHEMBL257958 | MELOSMINE | — | 1 | 4.61 |
| CHEMBL37736 | LIRIODENINE | — | 1 | 4.51 |
| CHEMBL257956 | — | — | 1 | 4.50 |
| CHEMBL257747 | — | — | 1 | 4.40 |
| CHEMBL455633 | CULARIDINE | — | 1 | 4.39 |
| CHEMBL258370 | PUKATEINE | — | 1 | 4.34 |
| CHEMBL452510 | BREOGANINE | — | 1 | 4.24 |
| CHEMBL510777 | SARCOCAPNIDINE | — | 1 | 4.07 |
| CHEMBL452776 | CELTISINE | — | 1 | - |
| CHEMBL452512 | CLAVICULINE | — | 1 | - |
| CHEMBL257957 | SUAVEOLINE | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL401798 | ANONAINE | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL257745 | NORSTEPHALAGINE | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL508011 | ISOPILINE | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL257746 | ANOLOBINE | IC50 | = | 8100.0 | nM | 5.09 |
| CHEMBL487388 | NORBOLDINE | IC50 | = | 16500.0 | nM | 4.78 |
| CHEMBL257958 | MELOSMINE | IC50 | = | 24600.0 | nM | 4.61 |
| CHEMBL37736 | LIRIODENINE | IC50 | = | 31000.0 | nM | 4.51 |
| CHEMBL257956 | — | IC50 | = | 32000.0 | nM | 4.50 |
| CHEMBL257747 | — | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL455633 | CULARIDINE | IC50 | = | 41000.0 | nM | 4.39 |
| CHEMBL258370 | PUKATEINE | IC50 | = | 46000.0 | nM | 4.34 |
| CHEMBL452510 | BREOGANINE | IC50 | = | 57000.0 | nM | 4.24 |
| CHEMBL510777 | SARCOCAPNIDINE | IC50 | = | 86000.0 | nM | 4.07 |
| CHEMBL452776 | CELTISINE | IC50 | > | 100000.0 | nM | - |
| CHEMBL452512 | CLAVICULINE | IC50 | > | 10000.0 | nM | - |
| CHEMBL257957 | SUAVEOLINE | IC50 | > | 100000.0 | nM | - |