Assay Detail
Binding
CHEMBL830146
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Inhibition of 3 nM [3H]NIC binding to Nicotinic acetylcholine receptor alpha4-beta2 of rat striatal membranes
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Subcellular | Membrane |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907596) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Defunctionalized lobeline analogues: structure-activity of novel ligands for the vesicular monoamine transporter.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 28 | 5.31 | 7.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL122270 | LOBELINE | 2.0 | 1 | 7.40 |
| CHEMBL372435 | — | — | 1 | 4.94 |
| CHEMBL333465 | LOBELANE | — | 1 | 4.83 |
| CHEMBL188912 | — | — | 1 | 4.79 |
| CHEMBL190113 | — | — | 1 | 4.61 |
| CHEMBL193224 | — | — | 1 | - |
| CHEMBL194053 | — | — | 1 | - |
| CHEMBL191947 | — | — | 1 | - |
| CHEMBL190870 | — | — | 1 | - |
| CHEMBL372892 | — | — | 1 | - |
| CHEMBL189788 | — | — | 1 | - |
| CHEMBL192910 | — | — | 1 | - |
| CHEMBL190555 | — | — | 1 | - |
| CHEMBL193782 | — | — | 1 | - |
| CHEMBL193571 | — | — | 1 | - |
| CHEMBL192329 | — | — | 1 | - |
| CHEMBL190319 | — | — | 1 | - |
| CHEMBL1794918 | — | — | 1 | - |
| CHEMBL193292 | — | — | 1 | - |
| CHEMBL187455 | — | — | 1 | - |
| CHEMBL192573 | — | — | 1 | - |
| CHEMBL192574 | — | — | 1 | - |
| CHEMBL190725 | — | — | 1 | - |
| CHEMBL122636 | — | — | 1 | - |
| CHEMBL192502 | — | — | 1 | - |
| CHEMBL190691 | — | — | 1 | - |
| CHEMBL424816 | — | — | 1 | - |
| CHEMBL193079 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL122270 | LOBELINE | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL372435 | — | Ki | = | 11600.0 | nM | 4.94 |
| CHEMBL333465 | LOBELANE | Ki | = | 14900.0 | nM | 4.83 |
| CHEMBL188912 | — | Ki | = | 16200.0 | nM | 4.79 |
| CHEMBL190113 | — | Ki | = | 24300.0 | nM | 4.61 |
| CHEMBL193224 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL194053 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL191947 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL190870 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL372892 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL189788 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL192910 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL190555 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL193782 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL193571 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL192329 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL190319 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL1794918 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL193292 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL187455 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL192573 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL192574 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL190725 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL122636 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL192502 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL190691 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL424816 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL193079 | — | Ki | > | 100000.0 | nM | - |