Assay Detail
Binding
CHEMBL3887331
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition Assay: Compounds (10 mM) were also evaluated for inhibition of binding to a7 nAChR using [125I]iodoMLA as previously reported in Carroll et al. The binding assays were conducted and the Ki values calculated as described in Carroll, F. I. et al., "Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 2-exo-2-(2',3'-disubstituted 5'-pyridinyl)-7- azabicyclo[2.2.1]heptanes: epibatidine analogues." J. Med. Chem. 2002, 45, 4755-4761.
13
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor subunit alpha-7 (CHEMBL4980) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Nicotinic receptor compounds
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 5.90 | 6.06 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3963157 | — | — | 1 | 6.06 |
| CHEMBL2164667 | — | — | 1 | 5.73 |
| CHEMBL58935 | — | — | 3 | - |
| CHEMBL185061 | — | — | 1 | - |
| CHEMBL185591 | — | — | 1 | - |
| CHEMBL361465 | — | — | 1 | - |
| CHEMBL2164663 | — | — | 1 | - |
| CHEMBL2164664 | — | — | 1 | - |
| CHEMBL372638 | — | — | 1 | - |
| CHEMBL2164666 | — | — | 1 | - |
| CHEMBL2164665 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3963157 | — | Ki | = | 870.0 | nM | 6.06 |
| CHEMBL2164667 | — | Ki | = | 1870.0 | nM | 5.73 |
| CHEMBL58935 | — | Ki | > | 2000.0 | nM | - |
| CHEMBL58935 | — | Ki | > | 2000.0 | nM | - |
| CHEMBL58935 | — | Ki | > | 2000.0 | nM | - |
| CHEMBL185061 | — | Ki | > | 2000.0 | nM | - |
| CHEMBL185591 | — | Ki | > | 2000.0 | nM | - |
| CHEMBL361465 | — | Ki | > | 2000.0 | nM | - |
| CHEMBL2164663 | — | Ki | > | 2000.0 | nM | - |
| CHEMBL2164664 | — | Ki | > | 2000.0 | nM | - |
| CHEMBL372638 | — | Ki | > | 2000.0 | nM | - |
| CHEMBL2164666 | — | Ki | > | 2000.0 | nM | - |
| CHEMBL2164665 | — | Ki | > | 2000.0 | nM | - |