Assay Detail
Binding
CHEMBL885370
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Inhibition constant against [3H]dihydrotetrabenazine binding to vesicular monoamine transporter-2 of rat synaptic vesicle membranes
14
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Synaptic vesicular amine transporter (CHEMBL4828) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis and evaluation of a series of tropane analogues as novel vesicular monoamine transporter-2 ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 5.64 | 6.01 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL333465 | LOBELANE | — | 1 | 6.01 |
| CHEMBL370014 | — | — | 1 | 5.89 |
| CHEMBL363778 | — | — | 1 | 5.86 |
| CHEMBL122270 | LOBELINE | 2.0 | 1 | 5.56 |
| CHEMBL194212 | — | — | 1 | 5.41 |
| CHEMBL364264 | — | — | 1 | 5.40 |
| CHEMBL370052 | — | — | 1 | 5.32 |
| CHEMBL371493 | — | — | 1 | - |
| CHEMBL197250 | — | — | 1 | - |
| CHEMBL197710 | — | — | 1 | - |
| CHEMBL382976 | — | — | 2 | - |
| CHEMBL198390 | — | — | 1 | - |
| CHEMBL198391 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL333465 | LOBELANE | Ki | = | 970.0 | nM | 6.01 |
| CHEMBL370014 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL363778 | — | Ki | = | 1380.0 | nM | 5.86 |
| CHEMBL122270 | LOBELINE | Ki | = | 2760.0 | nM | 5.56 |
| CHEMBL194212 | — | Ki | = | 3880.0 | nM | 5.41 |
| CHEMBL364264 | — | Ki | = | 3950.0 | nM | 5.40 |
| CHEMBL370052 | — | Ki | = | 4800.0 | nM | 5.32 |
| CHEMBL371493 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL197250 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL197710 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL382976 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL382976 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL198390 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL198391 | — | Ki | > | 100000.0 | nM | - |