Assay Detail
Binding
CHEMBL3887330
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Inhibition Assay: The Ki values for the inhibition of [3H]epibatidine binding at the α4β2 nAChR in male rat cerebral cortex for compounds are listed in Table A. 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.
17
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907589) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Nicotinic receptor compounds
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 9.85 | 10.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL361465 | — | — | 3 | 10.68 |
| CHEMBL2164666 | — | — | 1 | 10.52 |
| CHEMBL185061 | — | — | 1 | 10.14 |
| CHEMBL2164664 | — | — | 3 | 10.10 |
| CHEMBL2164667 | — | — | 1 | 9.92 |
| CHEMBL372638 | — | — | 1 | 9.72 |
| CHEMBL58935 | — | — | 3 | 9.62 |
| CHEMBL3963157 | — | — | 1 | 9.44 |
| CHEMBL2164663 | — | — | 1 | 9.36 |
| CHEMBL185591 | — | — | 1 | 9.28 |
| CHEMBL2164665 | — | — | 1 | 9.03 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL361465 | — | Ki | = | 0.021 | nM | 10.68 |
| CHEMBL361465 | — | Ki | = | 0.022 | nM | 10.66 |
| CHEMBL2164666 | — | Ki | = | 0.03 | nM | 10.52 |
| CHEMBL185061 | — | Ki | = | 0.073 | nM | 10.14 |
| CHEMBL2164664 | — | Ki | = | 0.08 | nM | 10.10 |
| CHEMBL2164664 | — | Ki | = | 0.082 | nM | 10.09 |
| CHEMBL2164667 | — | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL2164664 | — | Ki | = | 0.17 | nM | 9.77 |
| CHEMBL372638 | — | Ki | = | 0.19 | nM | 9.72 |
| CHEMBL58935 | — | Ki | = | 0.24 | nM | 9.62 |
| CHEMBL58935 | — | Ki | = | 0.24 | nM | 9.62 |
| CHEMBL58935 | — | Ki | = | 0.26 | nM | 9.59 |
| CHEMBL3963157 | — | Ki | = | 0.36 | nM | 9.44 |
| CHEMBL2164663 | — | Ki | = | 0.44 | nM | 9.36 |
| CHEMBL185591 | — | Ki | = | 0.53 | nM | 9.28 |
| CHEMBL2164665 | — | Ki | = | 0.94 | nM | 9.03 |
| CHEMBL361465 | — | Ki | = | 0.009 | nM | - |