Assay Detail
Binding
CHEMBL963862
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Displacement of [3H]dihydrotetrabenazine from vesicular monoamine transporter-2 in rat brain synaptosome
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Synaptic vesicular amine transporter (CHEMBL4828) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis and evaluation of a series of homologues of lobelane at the vesicular monoamine transporter-2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 20 | 5.25 | 6.06 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL455666 | — | — | 1 | 6.06 |
| CHEMBL333465 | LOBELANE | — | 1 | 6.01 |
| CHEMBL453650 | — | — | 1 | 6.00 |
| CHEMBL453701 | — | — | 1 | 5.95 |
| CHEMBL500548 | — | — | 1 | 5.79 |
| CHEMBL192329 | — | — | 1 | 5.64 |
| CHEMBL454769 | — | — | 1 | 5.56 |
| CHEMBL122270 | LOBELINE | 2.0 | 1 | 5.56 |
| CHEMBL509644 | — | — | 1 | 5.34 |
| CHEMBL455665 | — | — | 1 | 5.34 |
| CHEMBL508711 | — | — | 1 | 5.12 |
| CHEMBL454111 | — | — | 1 | 4.98 |
| CHEMBL455200 | — | — | 1 | 4.91 |
| CHEMBL455197 | — | — | 1 | 4.87 |
| CHEMBL455198 | — | — | 1 | 4.79 |
| CHEMBL447962 | — | — | 1 | 4.62 |
| CHEMBL500510 | — | — | 1 | 4.55 |
| CHEMBL455199 | — | — | 1 | 4.54 |
| CHEMBL455145 | — | — | 1 | 4.20 |
| CHEMBL455327 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL455666 | — | Ki | = | 880.0 | nM | 6.06 |
| CHEMBL333465 | LOBELANE | Ki | = | 970.0 | nM | 6.01 |
| CHEMBL453650 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL453701 | — | Ki | = | 1130.0 | nM | 5.95 |
| CHEMBL500548 | — | Ki | = | 1620.0 | nM | 5.79 |
| CHEMBL192329 | — | Ki | = | 2310.0 | nM | 5.64 |
| CHEMBL454769 | — | Ki | = | 2770.0 | nM | 5.56 |
| CHEMBL122270 | LOBELINE | Ki | = | 2760.0 | nM | 5.56 |
| CHEMBL509644 | — | Ki | = | 4560.0 | nM | 5.34 |
| CHEMBL455665 | — | Ki | = | 4600.0 | nM | 5.34 |
| CHEMBL508711 | — | Ki | = | 7680.0 | nM | 5.12 |
| CHEMBL454111 | — | Ki | = | 10500.0 | nM | 4.98 |
| CHEMBL455200 | — | Ki | = | 12200.0 | nM | 4.91 |
| CHEMBL455197 | — | Ki | = | 13600.0 | nM | 4.87 |
| CHEMBL455198 | — | Ki | = | 16100.0 | nM | 4.79 |
| CHEMBL447962 | — | Ki | = | 24100.0 | nM | 4.62 |
| CHEMBL500510 | — | Ki | = | 28400.0 | nM | 4.55 |
| CHEMBL455199 | — | Ki | = | 28600.0 | nM | 4.54 |
| CHEMBL455145 | — | Ki | = | 62500.0 | nM | 4.20 |
| CHEMBL455327 | — | Ki | > | 100000.0 | nM | - |